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tetradecanoylphorbol acetate

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Description

Tetradecanoylphorbol acetate (TPA) is a potent tumor promoter and a highly active phorbol ester. It is a diterpene ester found in the latex of the plant Croton tiglium. TPA acts as a strong activator of protein kinase C (PKC), a family of serine/threonine kinases that play critical roles in cellular signaling pathways. TPA promotes cell proliferation and differentiation, and it has been extensively studied for its effects on various cellular processes, including inflammation, immunity, and carcinogenesis. The molecule consists of a phorbol ester core and a tetradecanoyl chain attached at the 12-position. The synthesis of TPA involves several steps, including the isolation of phorbol from Croton tiglium latex, followed by chemical modification to introduce the tetradecanoyl chain. TPA has been used as a research tool to study the role of PKC in various cellular functions and to investigate the mechanisms of tumor promotion. It is also used as a model compound for developing new anti-cancer drugs.'

Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
CrotongenusA plant genus of the family EUPHORBIACEAE. The common name of dragon's blood is also used for DRACAENA and Daemonorops (ARECACEAE). Croton tiglium is the source of CROTON OIL.[MeSH]EuphorbiaceaeThe spurge family of flowering plants in the order Malpighiales. The family consists of annual and perennial herbs and woody shrubs or trees. Members contain securinine.[MeSH]
CrotongenusA plant genus of the family EUPHORBIACEAE. The common name of dragon's blood is also used for DRACAENA and Daemonorops (ARECACEAE). Croton tiglium is the source of CROTON OIL.[MeSH]EuphorbiaceaeThe spurge family of flowering plants in the order Malpighiales. The family consists of annual and perennial herbs and woody shrubs or trees. Members contain securinine.[MeSH]

Cross-References

ID SourceID
PubMed CID27924
CHEMBL ID279115
CHEBI ID37537
SCHEMBL ID115567
MeSH IDM0021224
PubMed CID122634
CHEMBL ID2373592
MeSH IDM0021224

Synonyms (183)

Synonym
BIDD:PXR0145
CBIOL_002014
pma (phorbol ester)
CHEMBL279115 ,
tpa (phorbol ester)
nsc-262244
phorbol 12-myristate 13-acetate diester
c36h56o8
BRD-K68552125-001-03-8
tetradecanoyl-beta-phorbol acetate
gtpl2341
(1s,2s,6r,10s,11r,13s,14r,15r)-13-(acetyloxy)-1,6-dihydroxy-8-(hydroxymethyl)-4,12,12,15-tetramethyl-5-oxotetracyclo[8.5.0.0^{2,6}.0^{11,13}]pentadeca-3,8-dien-14-yl tetradecanoate
nsc-626496
nsc626496
phorbol-12-myristate-13-acetate
p1585 ,
phorbol-12-tetradecanoyl-13-acetate
nsc-262644
nsc262644
DIVK1C_006897
tetradecanoic acid, (1ar,1bs,4ar,7as,7bs,8r,9r,9as)-9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa[3,4]benz[1,2-e]azulen-9
nsc 262244
tpa (phorbol derivative)
ccris 716
-yl ester
13-o-acetylphorbol 12-myristate
phorbol 12-tetradecanoate 13-acetate
5h-cyclopropa(3,4)benz(1,2-e)azulen-5-one, 1,1a-beta,1b-alpha,4,4a,7a-beta,7b,8,9,9a-decahydro-4a-alpha,7b-beta,9-alpha,9a-beta-tetrahydroxy-3-(hydroxymethyl)-1,1,6,8-beta-tetramethyl-, 9a-acetate 9-m
pma (tumor promoter)
1h-cyclopropa[3,4]benz[1,2-e]azulene, tetradecanoic acid deriv.
12-tetradecanoylphorbol 13-monoacetate
-one 9a-acetate, (+)- (8ci)
phorbol monoacetate monomyristate
tetradecanoic acid, 9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa[3,4]benz[1,2-e]azulen-9-yl ester, [1ar-(1aalpha,1bbeta,
beta-phorbol 12-myristate 13-acetate
phorbol ester
hsdb 3542
4abeta,7aalpha,7balpha,8alpha,9beta,9aalpha)]-
yristate
myristic acid, 9-ester with 1,1aalpha,1bbeta,4,4a,7aalpha,7b,8,9,9a-decahydro-4abeta,7balpha,9beta,9aalpha-tetrahydroxy-3-(hydroxymethyl)-1,1,6,8alpha-tetramethyl-5h-cyclopropa[3,4]benz[1,2-e]azulen-5
4beta-phorbol 12-myristate 13-acetate
12-o-tetradecanoyl phorbol acetate
CHEBI:37537 ,
phorbol 13-acetate 12-myristate
phorbol 12-myristate 13-acetate, >=99% (tlc), film or powder
BIO2_000352
BIO1_000300
BIO1_001278
BIO1_000789
BIO2_000832
BCBCMAP01_000182
IDI1_002107
BSPBIO_001024
phorbol myristate acetate
4-.beta.-phorbol 12-myristate 13-oac
12-o-tetradecanoylphorbol-13-acetate
nsc262244
tetradecanoic acid, (1ar,1bs,4ar,7as,7bs,8r,9r,9as)-9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa[3,4]benz[1,2-e]azulen-9-yl ester
factor a1
[acetoxy-dihydroxy-(hydroxymethyl)-tetramethyl-oxo-[?]yl] tetradecanoate
UPCMLD-DP069:001
brn 2407201
12-tetradecanoylphorbol-13-acetate
13-tetradecanoylphorbol acetate
phorbol-12-myristate 13-acetate
phorbol-myristate acetate
tetradecanoylphorbol acetate
phorbol acetate, myristate
4beta-phorbol-12-myristate-13-acetate
pentahydroxy-tigliadienone-monoacetate(c)monomyristate(b)
myristic acid, 9-ester with 1,1aalpha,1bbeta,4,4a,7aalpha,7b,8,9,9a-decahydro-4abeta,7balpha,9beta,9aalpha-tetrahydroxy-3-(hydroxymethyl)-1,1,6,8alpha-tetramethyl-5h-cyclopropa(3,4)benz(1,2-e)azulen-5-one 9a-acetate, (+)-
tetradecanoic acid, 9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa(3,4)benz(1,2-e)azulen-9-yl ester, (1ar-(1aalpha,1bbeta,4abeta,7aalpha,7balpha,8alpha,9beta,9aalpha))-
12-o-tetradekanoylphorbol-13-acetat [german]
myristic acid, 9-ester with 1,1a-alpha,1b-beta,4,4a,7a-alpha,7b,8,9,9a-decahydro-4a-beta,7b-alpha,9-beta,9a-alpha-tetrahydroxy-3-(hydroxymethyl)-1,1,6,8-alpha-tetramethyl-5h-cyclopropa(3,4)benz(1,2-e)azulen-5-one, 9a-acetate
C05151
12-o-tetradecanoylphorbol 13-acetate
12-tetradecanoylphorbol 13-acetate
phorbol 12-myristate 13-acetate
16561-29-8
phorbol 13 acetate 12 myristate
pma, for use in molecular biology applications, >=99% (tlc)
UPCMLD-DP069
UPCMLD-DP069:002
NCGC00161633-01
KBIO1_001841
KBIOGR_000364
MOLMAP_000041
KBIO2_000364
KBIOSS_000364
KBIO2_002932
KBIOGR_001298
KBIO3_000708
KBIO3_000707
KBIO2_005500
SPECTRUM4_000889
SPBIO_001902
SPECTRUM2_001911
SPECPLUS_000801
SPECTRUM330004
SPECTRUM5_001855
NCGC00161633-04
phorbol 12-myristate 13-acetate, synthetic, >=98.0% (tlc)
HMS1990D05
HMS1362D05
HMS1792D05
bdbm50099066
LMPR0104330002
NCGC00161633-05
unii-ni40jaq945
ni40jaq945 ,
tetradecanoic acid, 9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9, 9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa(3,4)benz(1,2-e)azulen-9-yl ester, (1ar-(1aa,1bb,4ab,7aa,7ba, 8a,9b,9aa))-
12-o-tetradekanoylphorbol-13-acetat
CCG-39863
S7791
phorbol 12-myristate 13-acetate diester [mi]
12-o-tetradecanoylphorbol-13-acetate [hsdb]
SCHEMBL115567
BRD-K68552125-001-04-6
(1ar,1bs,4ar,7as,7bs,8r,9r,9as)-9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa[3,4]benz[1,2-e]azulen-9-yl tetradecanoate
W-201494
AKOS024418767
AC-33957
phorbol 12-myristate 13-acetate (pma)
HB0502
(1ar,1bs,4ar,7as,7bs,8r,9r,9as)-9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a ,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa[3,4]benz[1,2-e]azulen-9-yl tetradecanoate
HMS3403D05
mfcd00036736
DTXSID5023798
12-o-tetradecanoyl-phorbol-13-acetate
CS-6053
HY-18739
12-o-tetradecanoylphorbol-13-acetate (tpa)
PHEDXBVPIONUQT-RGYGYFBISA-N
Q416716
phorbol-12-myristate-13-acetate - cas 16561-29-8
phorbol12-myristate13-acetate
(1ar,1bs,4ar,7as,7bs,8r,9r,9as)-9a-acetoxy-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-1h-cyclopropa[3,4]benzo[1,2-e]azulen-9-yl tetradecanoate
11016-13-0
cocarcinogen c3
cocarcinogen a1
FS-4842
12-o-tetradecanoyl phorbol-13-acetate;cocarcinogen a1; cocarcinogen c3
EX-A6920
[(1s,2s,6r,10s,11r,13s,14r,15r)-13-acetyloxy-1,6-dihydroxy-8-(hydroxymethyl)-4,12,12,15-tetramethyl-5-oxo-14-tetracyclo[8.5.0.02,6.011,13]pentadeca-3,8-dienyl] tetradecanoate
EU-0101032
LOPAC0_001032
.alpha.-tpa
63597-44-4
4-.alpha.-phorbol 13 acetate
tetradecanoic acid, (1ar,1bs,4as,7as,7bs,8r,9r,9as)-9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa[3,4]benz[1,2-e]azulen-9-yl ester
4.alpha.-tpa
4.alpha.-phorbol 12-myristate 13-acetate
4alpha-phorbol 12-myristate 13-acetate, solid, >=95% (tlc)
NCGC00094321-02
NCGC00094321-01
P 8139
NCGC00094321-03
4alpha-phorbol 12-myristate 13-acetate
HMS3263O05
CHEMBL2373592
CCG-205110
4alpha-phorbol-12-myristate-13-acetate
tetradecanoic acid, 9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa(3,4)benz(1,2-e)azulen-9-yl ester, (1ar-(1aalpha,1bbeta,4aalpha,7aalpha,7balpha,8alpha,9beta,9aalpha))-
LP01032
NCGC00261717-01
tox21_501032
4alpha-phorbol12-myristate13-acetate
4alpha-pma
6357-44-4
SR-01000076082-1
SR-01000076082-6
SR-01000076082-7
sr-01000076082
tetradecanoic acid,(1ar,1bs,4as,7as,7bs,8r,9r,9as)-9a-(acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1h-cyclopropa[3,4]benz[1,2-e]azulen-9-
4-alpha-phorbol 12-myristate 13-acetate >99%
SDCCGSBI-0051003.P002
NCGC00094321-05
[(1s,2s,6s,10s,11r,13s,14r,15r)-13-acetyloxy-1,6-dihydroxy-8-(hydroxymethyl)-4,12,12,15-tetramethyl-5-oxo-14-tetracyclo[8.5.0.02,6.011,13]pentadeca-3,8-dienyl] tetradecanoate
4,4-dianilino-1,1-binaphthyl-5,5-disulfonicaciddipotassiumsalt
4 alpha -phorbol 12-myristate 13-acetate
HY-106029
4|a-tpa
CS-0024660

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Starch particles with covalently bound glucose oxidase resembled macrophages in their spatial relation to the target cells and in the flux of H2O2 they generated from their surface, but were not expected to produce any other potentially toxic products."( Extracellular cytolysis by activated macrophages and granulocytes. II. Hydrogen peroxide as a mediator of cytotoxicity.
Brukner, LH; Cohn, ZA; Nathan, CF; Silverstein, SC, 1979
)
0.26
" The oligodendroglial damage coincided with the release of toxic compounds by the stimulated macrophages, since treatment of the cultures with the anti-GalC antibody and a variety of other macrophage stimulating agents led to secretion of reactive oxygen species and--in some experiments--tumor necrosis factor, both known to be toxic for oligodendrocytes."( Antibody-dependent cellular cytotoxicity in antimyelin antibody-induced oligodendrocyte damage in vitro.
Griot, C; Griot-Wenk, M; Pfister, H; Vandevelde, M, 1991
)
0.28
" Neutrophil-induced hepatocyte toxicity could not be explained by the production of reactive oxygen intermediates since: (a) hepatocyte toxicity was not prevented by either superoxide dismutase or by catalase; (b) PMN obtained from a subject with chronic granulomatous disease were as toxic as PMN obtained from a normal subject."( Toxicity of phorbol myristate acetate-stimulated polymorphonuclear neutrophils against rat hepatocytes. Demonstration and mechanism.
Dhumeaux, D; Guigui, B; Martin, N; Mavier, P; Préaux, AM; Rosenbaum, J; Zafrani, ES, 1988
)
0.27
"Several mechanisms have been postulated to be responsible for the pleiotropic effects of toxic chemicals."( Inhibition of gap junctional-mediated intercellular communication in vitro by aldrin, dieldrin, and toxaphene: a possible cellular mechanism for their tumor-promoting and neurotoxic effects.
Chang, CC; Jone, C; Trosko, JE,
)
0.13
" Reactive oxygen species are not involved in NK-cell mediated cytotoxicity, while PMA stimulated the monocytes to exert cytolysis and suppressed NK cells by the generation of these highly toxic oxygen products."( Cytotoxicity by human adherent cells: oxygen-dependent and -independent cytotoxic reactions by different cell populations.
van Kats-Renaud, JH; van Kessel, KP; van Strijp, JA; Verhoef, J; Visser, MR, 1986
)
0.27
"Human monomorphonuclear leukocytes (MMNs) stimulated with 12-O-tetradecanoylphorbol-13-acetate (TPA) were found to be toxic towards human A549 lung carcinoma cells which have been desensitized against the direct growth-inhibitory effect of TPA."( Oxidative properties of 12-O-tetradecanoylphorbol-13-acetate-stimulated human blood monomorphonuclear leukocytes and their toxicity against a human lung carcinoma cell line.
Brodie, AE; Gescher, A; Reed, DJ, 1985
)
0.27
" This suggests that the effect of PMA is not due to its nonspecific toxic effect; instead, it is dependent on the reactive oxygen species produced by the normal neutrophils."( Phorbol myristate acetate induced neutrophil autotoxicity.
Tsan, MF, 1980
)
0.26
" However, all five dihydroxylated pro-oxidant coumarins were toxic to NS20Y neuroblastoma cells in 24 hr culture, whereas the other eleven coumarins were nontoxic."( Superoxide scavenging activity in leukocytes and absence of cellular toxicity of a series of coumarins.
De Las Heras, B; Goodwin, PA; Hoult, JR; Paya, M, 1994
)
0.29
"In the past several years there has been a great deal of interest in the antioxidant beta-carotene and other micronutrients for their protective potential against various toxic insults."( beta-Carotene inhibition of chemically induced toxicity in vivo and in vitro.
Kornhauser, A; Lambert, LA; Wamer, WG; Wei, RR, 1994
)
0.29
" Previously we showed that in primary thyroid follicular cells, expression of mutant p21ras conferred a striking sensitivity to the toxic effects of phorbol esters."( Toxicity of phorbol esters for human epithelial cells expressing a mutant ras oncogene.
Bond, J; Dawson, T; Eccles, N; Wynford-Thomas, D, 1993
)
0.29
" The toxic effect of cationic liposomes was very limited with uninfected cells, although concentrations of liposomes that were not toxic within a few days of treatment could cause toxicity at later times."( Human immunodeficiency virus type-1 (HIV-1) infection increases the sensitivity of macrophages and THP-1 cells to cytotoxicity by cationic liposomes.
Düzgüneş, N; Felgner, PL; Konopka, K; Pretzer, E, 1996
)
0.29
" Ethanol was toxic to HepG2 E9 cells, which express CYP2E1, but not to HepG2 MV5 cells, which do not express CYP2E1."( Ethanol cytotoxicity to a transfected HepG2 cell line expressing human cytochrome P4502E1.
Cederbaum, AI; Wu, D, 1996
)
0.29
" Preincubation of Hep G2 cells with low, nontoxic concentrations of menadione increased the viability of the cells against toxic doses of menadione or H2O2."( Menadione cytotoxicity to Hep G2 cells and protection by activation of nuclear factor-kappaB.
Cederbaum, AI; Chen, Q, 1997
)
0.3
" dose of TPA, but these adverse effects became less intense or disappeared when a lower dose of TPA was used."( Effect of intravenous infusions of 12-O-tetradecanoylphorbol-13-acetate (TPA) in patients with myelocytic leukemia: preliminary studies on therapeutic efficacy and toxicity.
Cao, GS; Chang, RL; Conney, AH; Han, ZT; Liu, XJ; Newmark, HL; Sun, JZ; Tian, GF; Yang, RY; Zhu, XX, 1998
)
0.3
" Furthermore, inhibition of the PKC pathway neither significantly affected TNF-alpha-induced MKP-1 expression nor made cells susceptible to toxic effect of TNF-alpha."( Resistance to TNF-alpha cytotoxicity can be achieved through different signaling pathways in rat mesangial cells.
Guo, YL; Kang, B; Williamson, JR, 1999
)
0.3
"1 mM SIN-1 were not toxic to MAC-T cells."( Cytotoxic effects of peroxynitrite, polymorphonuclear neutrophils, free-radical scavengers, inhibitors of myeloperoxidase, and inhibitors of nitric oxide synthase on bovine mammary secretory epithelial cells.
Douglass, LW; Ledbetter, TK; Paape, MJ, 2001
)
0.31
"Peroxynitrite, MPO, and histidine are toxic to mammary secretory epithelial cells."( Cytotoxic effects of peroxynitrite, polymorphonuclear neutrophils, free-radical scavengers, inhibitors of myeloperoxidase, and inhibitors of nitric oxide synthase on bovine mammary secretory epithelial cells.
Douglass, LW; Ledbetter, TK; Paape, MJ, 2001
)
0.31
" The results of these studies suggest that the mechanism of L-canavanine toxicity is mediated through L-arginine-utilizing mechanisms and that the L-canavanine metabolite, L-canaline, is toxic to human PBMCs by disrupting polyamine biosynthesis."( The antiproliferative and immunotoxic effects of L-canavanine and L-canaline.
Adams, VR; Bence, AK; Crooks, PA; Worthen, DR, 2002
)
0.31
"To evaluate the adverse effects of exogenously induced reactive oxygen species (ROS) on mouse embryo development by using the 12-phorbol 13-myristate acetate (PMA)-activated leukocyte model as a source of ROS, and to examine the protective effect of antioxidant supplementation (vitamin C and vitamin E)."( Vitamin C and vitamin E supplementation reduce oxidative stress-induced embryo toxicity and improve the blastocyst development rate.
Agarwal, A; Attaran, M; Falcone, T; Goldberg, JM; Sharma, RK; Wang, X, 2002
)
0.31
"Chlorhexidine, even at low concentrations, is toxic for a variety of eukaryotic cells; however, its effects on host immune cells are not well known."( Cytotoxicity of chlorhexidine digluconate to murine macrophages and its effect on hydrogen peroxide and nitric oxide induction.
Bonacorsi, C; Carlos, IZ; Raddi, MS, 2004
)
0.32
" Of the total 13 adverse events (n = 12), 11 were mild, 2 were moderate, and none were severe, and only 5 were considered by the investigator as possibly related to treatment."( The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of RO5068760, an MEK inhibitor, in healthy volunteers: assessment of target suppression.
Barrett, J; Blotner, S; Busse-Reid, R; DeSchepper, S; Deutsch, J; Goelzer, P; Lee, L; Niu, H; Peck, R; Rueger, R; Weissgerber, G, 2010
)
0.36
"We examined the utility of respiratory burst measurements in alveolar macrophages to assess adverse cellular changes following exposure to urban particles."( Respiratory burst in alveolar macrophages exposed to urban particles is not a predictor of cytotoxicity.
Breznan, D; Brook, JR; Cakmak, S; Chauhan, V; Goegan, P; Karthikeyan, S; Kumarathasan, P; Nadeau, D; Vincent, R, 2013
)
0.39
" PAMNPs could be metabolized rapidly in mice and were not observed to cause any toxic or adverse effect."( Low toxicity and long circulation time of polyampholyte-coated magnetic nanoparticles for blood pool contrast agents.
Duan, Y; Gu, H; Lin, J; Shen, M; Wang, Q; Xu, Y; Zhao, T, 2015
)
0.42
" Possible adverse effects were evaluated after multiple treatments with the extract in a skin atrophy model."( Corticoid-like anti-inflammatory effect of Vochysia bifalcata Warm.: Preclinical evidence of efficacy and safety.
Assreuy, J; Bresolin, TMB; Cabrini, DA; Farias, IV; Ferreira, BGA; Horinouchi, CDDS; Krueger, CMA; Mendes, DAGB; Meyre-Silva, C; Otuki, MF; Soley, BDS; Zuffellato-Ribas, KC, 2020
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
" The development of potent anti-cancer agents that target this pathway prompts the need for analytical methods that allow pharmacodynamic monitoring of drug effects in patients during early phase clinical trial."( Measurement of MAP kinase activation by flow cytometry using phospho-specific antibodies to MEK and ERK: potential for pharmacodynamic monitoring of signal transduction inhibitors.
Chow, S; Hedley, DW; Patel, H, 2001
)
0.31
"We previously reported a flow cytometry technique to monitor pharmacodynamic effects of the raf kinase inhibitor BAY 43-9006 based on the ability of phorbol ester (PMA) to phosphorylate extracellular-regulated kinase (ERK) in peripheral blood (Chow et al."( Pharmacodynamic monitoring of BAY 43-9006 (Sorafenib) in phase I clinical trials involving solid tumor and AML/MDS patients, using flow cytometry to monitor activation of the ERK pathway in peripheral blood cells.
Chow, S; Hedley, D; Tong, FK, 2006
)
0.33
" Time kinetic analysis of NFAT1 inhibition in plasma from stable renal transplant recipients before and after an in vivo dose with tacrolimus correlated with the expected pharmacokinetic profile of tacrolimus."( Nuclear translocation of nuclear factor of activated T cells (NFAT) as a quantitative pharmacodynamic parameter for tacrolimus.
Maguire, O; Minderman, H; O'Loughlin, KL; Tornatore, KM; Venuto, RC, 2013
)
0.39

Compound-Compound Interactions

ExcerptReferenceRelevance
" Therefore, the effects of the anthracycline antibiotics on skin tumor promotion were evaluated in combination with the Ca2+ antagonist verapamil (VRP) and the protein kinase C (PKC) inhibitor palmitoylcarnitine (PC), compounds known to circumvent drug resistance."( Inhibition of mouse skin tumor promotion by adriamycin and daunomycin in combination with verapamil or palmitoylcarnitine.
Perchellet, JP; Satyamoorthy, K, 1990
)
0.28
" RAR-gamma selectively binding retinoids are potent inhibitors of breast cancer cell proliferation, alone and in combination with IFN-gamma."( Activity of retinoic acid receptor-gamma selectively binding retinoids alone and in combination with interferon-gamma in breast cancer cell lines.
Culig, Z; Daxenbichler, G; Marth, C; Michel, S; Mörtl, MG; Widschwendter, A; Widschwendter, M; Zeimet, AG, 1997
)
0.3
" Since the family of protein kinases C (PKC) takes part in these processes by interacting with signal transduction pathways at several levels including the activation of transcription factors, we evaluated in the present study the effects of exposure of human amniotic fluid cells (AFC) to 50 Hz, 1 mT electromagnetic fields (EMF) alone and in combination with the tumour promoting phorbol ester 12-O-tetradecanoylphorbol 13-acetate (TPA) on the subcellular localization of PKC protein, on PKC enzyme activity, and on the cell cycle distribution."( Influence of 50 Hz electromagnetic fields in combination with a tumour promoting phorbol ester on protein kinase C and cell cycle in human cells.
Kriehuber, R; Lange, S; Myrtill, S; Richard, D; Viergutz, T; Weiss, DG, 2002
)
0.31
" Because the dose of TPA used in this study was effective and resulted in clinically achievable blood levels, clinical trials with TPA alone or in combination with ATRA in patients with prostate cancer may be warranted."( Inhibitory effect of 12-O-tetradecanoylphorbol-13-acetate alone or in combination with all-trans-retinoic acid on the growth of LNCaP prostate tumors in immunodeficient mice.
Avila, GE; Chang, RL; Conney, AH; Cui, XX; Lee, S; Lin, Y; Lou, YR; Lu, YP; Newmark, H; Rabson, A; Reuhl, K; Shih, WJ; Zheng, X, 2004
)
0.32
"To investigate the effects of 12-O-tetradecanoylphorbol-13-acetate (TPA) in combination with paclitaxel (Taxol) on prostate cancer cells cultured in vitro or grown as tumors in immunodeficient mice."( Effects of 12-O-tetradecanoylphorbol-13-acetate (TPA) in combination with paclitaxel (Taxol) on prostate Cancer LNCaP cells cultured in vitro or grown as xenograft tumors in immunodeficient mice.
Avila, GE; Chang, RL; Conney, AH; Cui, XX; Garzotto, M; Hebbar, V; Kong, AN; Lin, Y; Lu, SE; Rabson, AB; Shih, WJ; Zheng, X, 2006
)
0.33
"Human prostate cancer LNCaP cells in culture were treated with TPA alone or in combination with paclitaxel."( Effects of 12-O-tetradecanoylphorbol-13-acetate (TPA) in combination with paclitaxel (Taxol) on prostate Cancer LNCaP cells cultured in vitro or grown as xenograft tumors in immunodeficient mice.
Avila, GE; Chang, RL; Conney, AH; Cui, XX; Garzotto, M; Hebbar, V; Kong, AN; Lin, Y; Lu, SE; Rabson, AB; Shih, WJ; Zheng, X, 2006
)
0.33
" Clinical trials with TPA alone or in combination with paclitaxel in patients with prostate cancer may be warranted."( Effects of 12-O-tetradecanoylphorbol-13-acetate (TPA) in combination with paclitaxel (Taxol) on prostate Cancer LNCaP cells cultured in vitro or grown as xenograft tumors in immunodeficient mice.
Avila, GE; Chang, RL; Conney, AH; Cui, XX; Garzotto, M; Hebbar, V; Kong, AN; Lin, Y; Lu, SE; Rabson, AB; Shih, WJ; Zheng, X, 2006
)
0.33
" In this in vivo study, the mammary glands of mature female rats were treated with TPA, and then the effects of genistein alone or in combination with capsaicin on suppression of inflammatory responses were examined."( Anti-inflammatory and anticarcinogenic effect of genistein alone or in combination with capsaicin in TPA-treated rat mammary glands or mammary cancer cell line.
Hwang, JT; Lee, YK; Park, OJ; Shin, JI, 2009
)
0.35
" These studies provide evidence for potential use of GNKG168 in combination with PWM and PMA in karyotypic analysis of CLL patient samples to better identify chromosomal abnormalities for risk stratification."( Enhanced detection of chromosomal abnormalities in chronic lymphocytic leukemia by conventional cytogenetics using CpG oligonucleotide in combination with pokeweed mitogen and phorbol myristate acetate.
Andritsos, L; Breidenbach, H; Byrd, JC; Flynn, J; Heerema, NA; Jarjoura, D; Jones, J; Mo, X; Muthusamy, N; Ramanunni, A, 2011
)
0.37
"In the present study, the effects of 12-O-tetra-decanoylphorbol-13-acetate (TPA) alone or in combination with gemcitabine on the growth of Panc-1 pancreatic cancer cells cultured in vitro or grown in NCr immunodeficient nude mice were investigated."( Effects of 12-O-tetradecanoylphorbol-13-acetate in combination with gemcitabine on Panc-1 pancreatic cancer cells cultured in vitro or Panc-1 tumors grown in immunodeficient mice.
Conney, AH; Cui, XX; Gao, Z; Huang, MT; Liu, Y; Rabson, AB; Verano, M; Zheng, X, 2012
)
0.38
"This study was aimed to investigate the effects of arsenic trioxide (As2O3) combined with TPA on cell cycle, cell differentiation and apoptosis of K562 cell line, and their possible mechanisms."( [Effects of As2O3 in combination with TPA on K562 cells].
Fan, RH; Mi, RH; Wei, XD; Yin, QS; Yuan, FF; Zhang, XH, 2014
)
0.4

Bioavailability

ExcerptReferenceRelevance
" The IGFBPs modulate the bioavailability of the IGFs and may enhance or inhibit IGF actions."( Regulation of insulin-like growth factor-binding protein messenger ribonucleic acid levels in sheep thyroid cells.
Bachrach, LK; Burrow, GN; Eggo, MC; Liu, F; Powell, DR; Tram, T, 1991
)
0.28
" Because AA may be poorly absorbed cutaneously, we evaluated the effect of dietary AA."( Effect of ascorbic acid and its synthetic lipophilic derivative ascorbyl palmitate on phorbol ester-induced skin-tumor promotion in mice.
Crawford, CL; Smart, RC, 1991
)
0.28
" Its high content in soybeans and relatively high bioavailability favor genistein as a promising candidate for the prevention of human cancers."( Antioxidant and antipromotional effects of the soybean isoflavone genistein.
Barnes, S; Bowen, R; Cai, Q; Wang, Y; Wei, H, 1995
)
0.29
"The effects of daily supplementation of 1000 IU of d-alpha- or dl-alpha-tocopherol acetate to Holstein cows from drying off to 8 wk after calving were studied 1) to compare the bioavailability of d-alpha- and dl-alpha-tocopherol acetate by monitoring vitamin E concentrations in plasma, red blood cells, and neutrophils and 2) to determine the effect of d-alpha- and dl-alpha-tocopherol acetate supplementation on O2- and H2O2 release by neutrophils."( Bioavailability of vitamin E compounds and the effect of supplementation on release of superoxide and hydrogen peroxide by bovine neutrophils.
Batra, TR; Hidiroglou, M; Zhao, X, 1997
)
0.3
" Our results support the hypothesis that intracellular tetrahydrobiopterin levels are tightly linked to tyrosine hydroxylation and that tetrahydrobiopterin bioavailability modulates catecholamine synthesis."( Vasoactive intestinal peptide induces both tyrosine hydroxylase activity and tetrahydrobiopterin biosynthesis in PC12 cells.
Anastasiadis, PZ; Bezin, L; Blitz, J; Gordon, LJ; Imerman, B; Kuhn, DM; Levine, RA, 1998
)
0.3
" CRF-binding protein (CRF-BP) regulates the bioavailability of CRF, and knowledge of the regulation of CRF-BP synthesis is an integral component of understanding the actions of CRF."( Coordinate and divergent regulation of corticotropin-releasing factor (CRF) and CRF-binding protein expression in an immortalized amygdalar neuronal cell line.
Balasubramaniam, A; Kasckow, JW; Mulchahey, JJ; Regmi, A; Sheriff, S, 1999
)
0.3
" This enzyme is a major source for arterial ROS generation and affects the bioavailability of endothelium-derived NO."( A gp91phox containing NADPH oxidase selectively expressed in endothelial cells is a major source of oxygen radical generation in the arterial wall.
Amidi, M; Brandes, RP; Busse, R; Dehghani, F; Görlach, A; Nguyen, K, 2000
)
0.31
" These data establish a general strategy for enhancing delivery of poorly absorbed drugs across tissue barriers and provide a new topical approach to the treatment of inflammatory skin disorders."( Conjugation of arginine oligomers to cyclosporin A facilitates topical delivery and inhibition of inflammation.
Garlington, S; Khavari, PA; Kirschberg, T; Kreider, E; Lin, Q; McGrane, PL; Rothbard, JB; Wender, PA, 2000
)
0.31
" The systemic bioavailability of curcumin is low, so that its pharmacological activity may be mediated, in part, by curcumin metabolites."( Characterization of metabolites of the chemopreventive agent curcumin in human and rat hepatocytes and in the rat in vivo, and evaluation of their ability to inhibit phorbol ester-induced prostaglandin E2 production.
Gescher, A; Howells, L; Ireson, C; Jones, DJ; Jukes, R; Lim, CK; Luo, JL; Orr, S; Plummer, S; Steward, WP; Verschoyle, R; Williams, M, 2001
)
0.31
" It has been proposed that the lipid phosphate phosphatases exhibit ecto activity that may function to limit bioavailability of these lipid agonists at their receptors."( G-protein-coupled receptor stimulation of the p42/p44 mitogen-activated protein kinase pathway is attenuated by lipid phosphate phosphatases 1, 1a, and 2 in human embryonic kidney 293 cells.
Ahmed, IS; Alderton, F; Darroch, P; McKie, A; Pyne, N; Pyne, S; Sambi, B, 2001
)
0.31
" Thus, microglial NADPH oxidase can regulate the bioavailability of NO and the production of peroxynitrite."( Stimulation of the NADPH oxidase in activated rat microglia removes nitric oxide but induces peroxynitrite production.
Bal-Price, A; Brown, GC; Matthias, A, 2002
)
0.31
" This may have practical applications in drug delivery and bioavailability of hydrophobic peptides."( Lipidation and glycosylation of a T cell antigen receptor (TCR) transmembrane hydrophobic peptide dramatically enhances in vitro and in vivo function.
Ali, M; Amon, MA; Bender, V; Chan, YN; Manolios, N; Toth, I, 2006
)
0.33
" D3 is highly expressed in brain, placenta, pregnant uterus, and fetal tissues and plays an important role in regulating thyroid hormone bioavailability during fetal development."( Regulation of type III iodothyronine deiodinase expression in human cell lines.
Kester, MH; Kuiper, GG; Versteeg, R; Visser, TJ, 2006
)
0.33
")NO bioavailability was reflected in decreased cellular cGMP content, associated with increased superoxide anion radical (O(2)(-."( Hydrogen peroxide promotes endothelial dysfunction by stimulating multiple sources of superoxide anion radical production and decreasing nitric oxide bioavailability.
Ellis, NA; Rayner, BS; Stocker, R; Witting, PK; Wu, BJ, 2007
)
0.34
" Curcumin is characterized by poor bioavailability as it is water-insoluble, is poorly absorbed and is systemically eliminated."( Influence of particle size on the in vitro and in vivo anti-inflammatory and anti-allergic activities of a curcumin lipid nanoemulsion.
Andoh, T; Ichikawa, H; Kuriyama, I; Lee-Hiraiwa, E; Mizushina, Y; Onodera, T; Sakamoto, Y, 2015
)
0.42
" Here a caveolae-targeting glycosylphosphatidylinositol (GPI)-anchored EPCR (EPCR-GPI) was engineered to restore EPCR's bioavailability via "cell painting."( Cell painting with an engineered EPCR to augment the protein C system.
Bouwens, EA; Mosnier, LO; Stavenuiter, F, 2015
)
0.42
" This enhanced the therapeutic bioavailability of resveratrol."( Enhancement of the cancer inhibitory effect of the bioactive food component resveratrol by nanoparticle based delivery.
Ahmed, F; Bano, S; Chaudhary, SC; Khan, F; Samim, M, 2020
)
0.56
"Fetal growth restriction (FGR) is associated with decreased nutrient availability and reduced insulin-line growth factor (IGF)-I bioavailability via increased IGF binding protein (IGFBP)-1 phosphorylation."( IGFBP-1 hyperphosphorylation in response to nutrient deprivation is mediated by activation of protein kinase Cα (PKCα).
Biggar, K; Chen, AW; Gupta, MB; Jansson, T; Li, C; Nathanielsz, PW; Nygard, K; Singal, S; Zhao, T, 2021
)
0.62

Dosage Studied

ExcerptRelevanceReference
" The dose-response curve for triggering of H2O2 release by PMA was identical to that for triggering cytotoxicity."( Extracellular cytolysis by activated macrophages and granulocytes. I. Pharmacologic triggering of effector cells and the release of hydrogen peroxide.
Brukner, LH; Cohn, ZA; Nathan, CF; Silverstein, SC, 1979
)
0.26
"The dose-response effects of phorbol myristate acetate and cytochalasin B on secretion of azurophil and specific granule enzymes from viable human polymorphonuclear leukocytes have been examined."( Cytochalasin B-dependent release of azurophil granule enzymes from human polymorphonuclear leukocytes.
Yurewicz, EC; Zimmerman, M, 1977
)
0.26
" A similar dose-response relation was observed for the ability of PdiC8 to stimulate epidermal hyperplasia."( Epidermal cell proliferation and promoting ability of phorbol esters.
Scribner, JD; Slaga, TJ; Viaje, A, 1976
)
0.26
" A single application of 50 to 200 nmoles of (+)- or (-)-trans-7,8-dihydroxy-7,8-dihydrobenzo(a)pyrene to the backs of CD-1 mice followed by twice-weekly applications of 12-O-tetradecanoyl-phorbol-13-acetate revealed that the (-)-enantiomer was 5- to 10-fold more potent than was the (+)-enantiomer as a tumor initiator at the three dosage levels tested."( Marked differences in the tumor-initiating activity of optically pure (+)- and (-)-trans-7,8-dihydroxy-7,8-dihydrobenzo(a)pyrene on mouse skin.
Chang, RL; Conney, AH; Jerina, DM; Levin, W; Slaga, TJ; Wood, AW; Yagi, H, 1977
)
0.26
" A dose-response relationship between the amount of acetic acid and the rate of DNA synthesis was found between the dose levels of 33 to 833 mumoles of acetic acid per application."( Acetic acid, a potent stimulator of mouse epidermal macromolecular synthesis and hyperplasia but with weak tumor-promoting ability.
Boutwell, RK; Bowden, GT; Slaga, TJ, 1975
)
0.25
" The dose-response curves to PMA for decreasing the activities of PKC 1 and 2 were shifted to the right by the potent and selective PKC inhibitors, staurosporine and calphostin-C."( Staurosporine and calphostin-C inhibit the phorbol ester-induced decrease of protein kinase C activity in rat hepatocytes.
García-Sáinz, JA; López-Gómez, FJ; Robles-Flores, M, 1992
)
0.28
" The dose-response curve for this suppression was very similar to that for stimulation of inositol monophosphate (IP1) formation and for stimulation of the initial rise of [Ca2+]i elicited by carbachol."( Suppressive effect of carbachol on forskolin-stimulated neurite outgrowth in human neuroblastoma NB-OK1 cells.
Nakagawa-Yagi, Y; Nakamura, H; Saito, Y; Takada, Y, 1992
)
0.28
" Similar dose-response relationships for the effects of NGF and of FGF on the activation of the kinase and on the outgrowth of neurites were observed."( Activation of microtubule-associated protein kinase in PC12D cells in response to both fibroblast growth factor and epidermal growth factor and concomitant stimulation of the outgrowth of neurites.
Kitajima, S; Sano, M, 1992
)
0.28
" Genistein (10-200 microM) inhibited in a dose-response fashion the PRL stimulation of casein, lipid and lactose synthesis as well as ODC activation."( Effect of a tyrosine kinase inhibitor, genistein, on the actions of prolactin in cultured mouse mammary tissues.
Fan, G; Rillema, JA, 1992
)
0.28
" This effect was rapid (t1/2 less than 5 min) and had a similar dose-response relationship as the effect on glucose transport."( Insulin can rapidly increase cell surface insulin binding capacity in rat adipocytes. A novel mechanism related to insulin sensitivity.
Eriksson, J; Lönnroth, P; Smith, U, 1992
)
0.28
" An increase in intracellular Ca2+ concentration depressed the amplitude of current induced by application of acetylcholine in neurons with ouabain-sensitive responses and shifted the dose-response relationship to the right."( The effects of cAMP, Ca2+, and phorbol esters on ouabain-induced depression of acetylcholine responses in Helix neurons.
Arvanov, VL; Ayrapetyan, SN; Stepanyan, AS, 1992
)
0.28
" These results indicate that differences in MHC gene dosage are associated with differences in chicken macrophage activation for the acquisition of selected antibacterial functions."( Macrophage antimicrobial functions in a chicken MHC chromosome dosage model.
Bloom, SE; Dietert, RR; Lin, HK, 1992
)
0.28
" Dose-response curves of PMA and of forskolin for the inhibition of PLC-gamma 1 tyrosine phosphorylation and of PtdIns 4,5-P2 hydrolysis were similar."( Inhibition of CD3-linked phospholipase C by phorbol ester and by cAMP is associated with decreased phosphotyrosine and increased phosphoserine contents of PLC-gamma 1.
Min, HK; Park, DJ; Rhee, SG, 1992
)
0.28
" By using Northern blot analysis and dosage of the IL-2 release in cell supernatants, we show that SP can act as cosignal with PHA + PMA to enhance the expression of specific IL-2 mRNA and IL-2 secretion in T cells."( Substance P enhances IL-2 expression in activated human T cells.
Calvo, CF; Chavanel, G; Senik, A, 1992
)
0.28
" Dose-response studies with several mutagens indicated that the number of foci increased with concentration to the point where excessive cytotoxicity developed."( Development of an in vitro model to study carcinogen-induced neoplastic progression of initiated mouse epidermal cells.
Glick, A; Greenhalgh, D; Hennings, H; Morgan, D; Welty, D; Yuspa, SH, 1992
)
0.28
" The dose-response of [3H]thymidine incorporation induced by IGF-I and TPA indicated that 10 nM was the lowest concentration producing a maximal effect for both agents."( Involvement of protein kinase-C in the mitogenic effect of insulin-like growth factor-I on rat astrocytes.
Calle, R; Naftolin, F; Robbins, R; Tranque, PA, 1992
)
0.28
" Dose-response relationships showed 10 nM- and 100 nM-EGF to be maximally effective in HeLa cells and A431 cells respectively."( Epidermal-growth-factor-induced production of phosphatidylalcohols by HeLa cells and A431 cells through activation of phospholipase D.
Kast, R; Kaszkin, M; Kinzel, V; Seidler, L, 1992
)
0.28
" Dose-response and time-course studies revealed that TPA (10(-8) M) acutely increased GnRH secretion 3-fold at 3-6 h, which then declined to baseline at 24 h, while it progressively decreased GnRH mRNA levels by 50% and 70% at 6 and 24 h, respectively."( Phorbol ester activation of the protein kinase C pathway inhibits gonadotropin-releasing hormone gene expression.
Bruder, JM; Krebs, WD; Nett, TM; Wierman, ME, 1992
)
0.28
" To provide adequate cell numbers for kinetic and dose-response studies, the in vitro model of phorbol ester (TPA)-induced differentiation of HL60 cells to macrophage-like cells was used."( Dexamethasone-induced increase in platelet-derived growth factor (B) mRNA in human alveolar macrophages and myelomonocytic HL60 macrophage-like cells.
Haynes, AR; Shaw, RJ, 1992
)
0.28
" Before AOS exposure, the opioid peptides suppressed the PMA-stimulated respiratory burst in human PMNs and a U-shaped dose-response relationship was observed."( Reciprocal effects between opioid peptides and human polymorphonuclear leukocytes--II. Enhancement of phorbol myristate acetate-induced respiratory burst in human polymorphonuclear leukocyte by opioid peptides previously exposed to activated oxygen specie
Guerin, MC; Le Doucen, C; Loubatiere, J; Slaoui-Hasnaoui, A; Torreilles, J, 1992
)
0.28
"8% LA diet group, and a positive dose-response relationship between dietary LA and mammary-tumor incidence was observed."( Differential effects of dietary linoleic acid on mouse skin-tumor promotion and mammary carcinogenesis.
Bechtel, DH; Belury, MA; Fischer, SM; Lee, ML; Leyton, J; Locniskar, M; Maldve, RE; Slaga, TJ, 1992
)
0.28
" Dose-response relationships were established for skin tumor promotion by TPA following initiation with 7,12-dimethylbenz[a]anthracene in C3H/He and B6C3F1, as well as several other mouse stocks and strains included for comparison."( Further genetic analyses of skin tumor promoter susceptibility using inbred and recombinant inbred mice.
Beltrán, L; Chenicek, KJ; DiGiovanni, J; Imamoto, A; Naito, M; Skow, L; Walker, SE, 1992
)
0.28
" Similarly, dose-response curves for pepsinogen secretion and the increase in membrane-associated PKC activity induced by a membrane-permeant DAG (1-oleoyl-2-acetylglycerol) were superimposable."( Cellular distribution of gastric chief cell protein kinase C activity: differential effects of diacylglycerol, phorbol esters, carbachol, and cholecystokinin.
Raffaniello, RD; Raufman, JP, 1992
)
0.28
" Dose-response experiments indicated that interleukin-4 is more potent than interleukin-1 alpha and interleukin-2 in inhibiting dexamethasone-induced apoptosis."( Interleukins modulate glucocorticoid-induced thymocyte apoptosis.
Crocicchio, F; Migliorati, G; Moraca, R; Nicoletti, I; Pagliacci, C; Riccardi, C, 1992
)
0.28
" Treatment with TPA leads to a marked transformation yield in all plates scored even at the lowest assayed dosage of 1,1,2,2-TTCE, without performing amplification of transformation."( Initiating activity of 1,1,2,2-tetrachloroethane in two-stage BALB/c 3T3 cell transformation.
Bartoli, S; Colacci, A; Da Via, C; Grilli, S; Perocco, P; Silingardi, P; Vaccari, M, 1992
)
0.28
" Dose-response studies revealed that the most effective TPA concentration for stimulation of DNA synthesis and growth of melanocytes (10 ng/ml TPA) also supported a relatively high level of PKC enzyme activity, increased membrane association of the PKC alpha and PKC epsilon isoforms, and led to a high level of phosphorylation of a major PKC substrate, the myristoylated alanine-rich C kinase substrate (MARCKS) protein."( Growth of human melanocyte cultures supported by 12-O-tetradecanoylphorbol-13-acetate is mediated through protein kinase C activation.
Arita, Y; O'Driscoll, KR; Weinstein, IB, 1992
)
0.28
" Bradykinin increased the two second messengers via independent mechanisms: (a) dose-response curves with different incubation media demonstrated that each second messenger could be generated independently of the other; (b) phorbol ester inhibited InsP production but stimulated arachidonic acid release; (c) for polarized cultures, submucosal bradykinin stimulated production of both second messengers but mucosal bradykinin stimulated only arachidonic acid release."( Polarized distribution of bradykinin receptors on airway epithelial cells and independent coupling to second messenger pathways.
Denning, GM; Welsh, MJ, 1991
)
0.28
" Normal functional coupling of m2, m4, alpha 2, and D2 receptors was demonstrated by their ability to inhibit forskolin-stimulated cAMP accumulation with dose-response activities consistent with previous reports for these Gi-coupled receptors."( A transduction pathway associated with receptors coupled to the inhibitory guanine nucleotide binding protein Gi that amplifies ATP-mediated arachidonic acid release.
Axelrod, J; Felder, CC; Williams, HL, 1991
)
0.28
" Oral dosing of nilvadipine suppressed carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen."( Inhibition by nilvadipine of ischemic and carrageenan paw edema as well as of superoxide radical production from neutrophils and xanthine oxidase.
Oyanagui, Y; Sato, S, 1991
)
0.28
" The dose-response curve characterizing the dependence of ROI production on the concentration of platelet-activating factor (PAF) showed that stimulation occurred within a concentration range of 2 x 10(-9)M to 5 x 10(-6)M."( Platelet-activating factor stimulates receptor-mediated formation of reactive oxygen intermediates in human monocytes.
Kozyukov, AV; Makarova, OV; Porodenko, NV; Pustynnikov, MG; Severin, ES; Sokolovsky, AA, 1991
)
0.28
" Further, dose-response studies showed that sodium fluoride (NaF), activator of G-binding proteins, and ouabain, inhibitor of Na+/H+ pump, increased levels of IL-6 mRNA."( Role of lymphotoxin in expression of interleukin 6 in human fibroblasts. Stimulation and regulation.
Adelman, DC; Akashi, M; Koeffler, HP; Loussararian, AH; Saito, M, 1990
)
0.28
" Time-course kinetics and dose-response curves of RNA and DNA synthesis induced by bryostatin 1 or PMA were comparable, albeit the phorbol ester was significantly more potent."( Synergistic action of calcium ionophore A23187 and protein kinase C activator bryostatin 1 on human B cell activation and proliferation.
Drexler, HG; Gignac, SM; Hoffbrand, AV; Pettit, GR, 1990
)
0.28
" However, in the presence of ionomycin the dose-response of 8-bromo-cAMP (Br-cAMP) with respect to uPA mRNA accumulation was shifted toward the lower concentrations of Br-cAMP."( Ca2+ potentiates cAMP-dependent expression of urokinase-type plasminogen activator gene through a calmodulin- and protein kinase C-independent mechanism.
Hagmann, J; Kiefer, B; Nagamine, Y; Ziegler, A, 1990
)
0.28
" An insulin dosage as low as 10(-10) M was inhibitory to PEPCK activity, suggesting the involvement of insulin receptors."( Insulin and other regulatory factors modulate the growth and the phosphoenolpyruvate carboxykinase (PEPCK) activity of primary rabbit kidney proximal tubule cells in serum free medium.
Taub, M; Wang, Y, 1991
)
0.28
" PDGF displays a steep dose-response relationship in the 1-5 ng/ml range."( Activation of signal transduction pathways protects quiescent Balb/c-3T3 fibroblasts against death due to serum deprivation.
Kikuchi, T; Tamm, I, 1991
)
0.28
" In contrast, PR mRNA in the K3 subline, as in the parental K1 cells, is still up-regulated by E2, and ER mRAN content and the ER mRNA transcription rate are still down-regulated by E2 and show normal E2 dose-response relationships, implying that the ER in this subline is functional."( Differential regulation of gene expression by estrogen in estrogen growth-independent and -dependent MCF-7 human breast cancer cell sublines.
Cho, HS; Katzenellenbogen, BS; NG, PA, 1991
)
0.28
" Dose-response curves for the inhibitory effects of the anti-oxidants on DNA synthesis and ODC activity at 48 h after mitogen addition were very similar."( Effects of anti-oxidants on ornithine decarboxylase in mitogenically-activated T lymphocytes.
Fragonas, JC; Hunt, NH, 1992
)
0.28
"7 mmol/l) led to a potentiation of both phase 1 and phase 2 of glucose-induced insulin secretion, and caused a shift in the dose-response curve with 10 mmol/l and 16."( Role of protein kinase C and Ca2+ in glucose-induced sensitization/desensitization of insulin secretion.
Thams, P, 1991
)
0.28
" The dose-response curve showed a peak action at 1 mM (Bu)2cAMP."( The mechanism of parathyroid hormone action on calcium reabsorption by the distal tubule.
Bouhtiauy, I; Brunette, MG; Lajeunesse, D, 1991
)
0.28
" Dose-response curves for the inhibition of inositol 1,4,5-trisphosphate formation and Ca2+ mobilization reveal 50% inhibitory concentrations of 2 or 5 microM, respectively."( Hexadecylphosphocholine inhibits inositol phosphate formation and protein kinase C activity.
Demuth, L; Grunicke, HH; Maly, K; Oberhuber, H; Uberall, F; Zaknun, J, 1991
)
0.28
" The dose-response relation with AVP thus shifted to the right."( Inhibition by phorbol ester of cellular adenosine 3',5'-monophosphate production and cellular free calcium mobilization in response to arginine vasopressin in rat renal papillary collecting tubule cells in culture.
Ishikawa, S; Saito, T, 1991
)
0.28
" Inhibition by cAMP was achieved by shifting the Ca2+ dose-response curve for secretion to the right; this was observed for the release of both specific granules (vitamin B12 binding protein) and azurophil granules (B-glucuronidase)."( Cyclic AMP inhibits secretion from electroporated human neutrophils.
Kuczynski, B; Smolen, JE; Stoehr, SJ, 1991
)
0.28
" Inhibition of specific-granule release by GTP[S] was observed at low Ca2+ concentrations and resulted from shifting the Ca2+ dose-response curves to the right."( Dual effects of guanosine 5'-[gamma-thio]triphosphate on secretion by electroporated human neutrophils.
Koh, EK; Kuczynski, B; Omann, GM; Smolen, JE; Stoehr, SJ, 1991
)
0.28
" There was a clear dose-response effect, with the optimal antimelanoma dose being 100 micrograms/kg/day, but even low doses of bryostatin 1 of 1 micrograms/kg/day resulted in a 53% reduction in the number of metastases."( Successful treatment of murine melanoma with bryostatin 1.
Esa, AH; Hess, AD; Laulis, MK; May, S; Pettit, GR; Schuchter, LM, 1991
)
0.28
" Prior to each TPA application groups were dosed with 0, 1 mumol, or 10 mumol citral."( Modulation of tumor promotion in mouse skin by the food additive citral (3,7-dimethyl-2,6-octadienal).
Connor, MJ, 1991
)
0.28
" However, no dose-response data related directly to carcinogenesis have been published."( Neoplastic transformation of C3H/10T1/2 cells following exposure to 120-Hz modulated 2.45-GHz microwaves and phorbol ester tumor promoter.
Balcer-Kubiczek, EK; Harrison, GH, 1991
)
0.28
" The dose-response curve for FMLP was biphasic; low concentrations were stimulatory, and the response was reduced at higher concentrations."( The involvement of calcium and protein kinase C in modulating agonist-stimulated chemotaxis of human neutrophils.
Greener, M; Hallam, TJ; Merritt, JE; Swayne, GT, 1991
)
0.28
" The substantial cell killing and regenerative proliferation, and the correspondence between the dose-response patterns for epidermal damage and tumors, together with the initial appearance of tumors in the benign form, a characteristic of the action of promoting agents, provided evidence that the tissue damage associated with the high dose levels of B[a]P used in this study reflected tumor-promoting activity in this mouse epidermal tumorigenesis model."( Benzo[a]pyrene-induced skin damage and tumor promotion in the mouse.
Albert, RE; Andringa, A; Baxter, CS; Cody, T; Miller, ML; Shukla, R, 1991
)
0.28
" The time course and dose-response curves for the effects of phorbol 12-myristate 13-acetate (PMA) on S6 kinase activity were similar to those for its effects on protein kinase C binding to the membrane fraction, indicating that S6 kinase activation was correlated with protein kinase C activation."( Regulation of S6 kinase activity in Madin-Darby canine kidney renal epithelial cells.
Bloom, TJ; Krebs, EG; Meier, KE; Weiel, JE, 1990
)
0.28
" The number of colonies which developed during promoter exposure in cocultures showed a dose-response curve which differed from the dose-response curve for stimulation of growth of 308 colonies in the absence of normal keratinocytes."( Development of an in vitro analogue of initiated mouse epidermis to study tumor promoters and antipromoters.
Hennings, H; Jung, R; Michael, DM; Pettit, GR; Robinson, VA; Yuspa, SH, 1990
)
0.28
" This study was designed to examine the dose-response nature and time-dependent effect of 4 beta-phorbol-12-myristate-13-acetate (PMA) on the rates of bicarbonate absorption (JHCO3) and fluid absorption (Jv) in the proximal convoluted tubule (PCT) of rat kidney."( Time- and dose-dependent effects of protein kinase C on proximal bicarbonate transport.
Chan, YL; Wang, T, 1990
)
0.28
" Dose-response studies, also reported here, indicate that the detergent insolubility of the complexes does not correlate with secretion."( Antigen-dependent transition of IgE to a detergent-insoluble form is associated with reduced IgE receptor-dependent secretion from RBL-2H3 mast cells.
Oliver, JM; Seagrave, J, 1990
)
0.28
" Dose-response and time-course considerations make it unlikely that these effects are mediated via the glucocorticoid receptor, a concept further supported by the ability of sex steroids to work similar effects."( Steroids decrease granulocyte membrane fluidity, while phorbol ester increases membrane fluidity. Studies using electron paramagnetic resonance.
Hammerschmidt, DE; Jacob, HS; Knabe, AC; Lamche, HR; Silberstein, PT; Thomas, DD, 1990
)
0.28
" The activation of the three cascades induced the expression of the protooncogenes c-fos and c-myc with dose-response curves similar to those for DNA synthesis."( Regulation of protooncogenes c-fos and c-myc expressions by protein tyrosine kinase, protein kinase C, and cyclic AMP mitogenic pathways in dog primary thyrocytes: a positive and negative control by cyclic AMP on c-myc expression.
Dumont, JE; Maenhaut, C; Reuse, S, 1990
)
0.28
"Phorbol myristate acetate (PMA) inhibits glucagon-stimulated cyclic AMP accumulation and shifts to the right the dose-response curve to glucagon for ureagenesis."( Modulation of glucagon actions by phorbol myristate acetate in isolated hepatocytes. Effect of hypothyroidism.
García-Sáinz, JA; Hernández-Sotomayor, SM; Hruby, VJ; Macías-Silva, M; Torres-Márquez, ME; Trivedi, D, 1990
)
0.28
" The amount of dye extracted from the paw showed a clear dose-response relationship to the dose of each agonist injected into the paw."( Assessment of vascular permeability increase in the mouse by dye leakage during paw edema.
Hayashi, M; Oh-ishi, S; Qu, XF; Yamaki, K, 1990
)
0.28
" Dose-response curves revealed that PHA-induced production of inositol phosphates correlated closely with PKC activities, whereas only a partial correlation between these parameters was observed with GTP[S]."( A method for measuring protein kinase C activity in permeabilized T lymphocytes by using peptide substrates. Evidence for multiple pathways of kinase activation.
Alexander, DR; Cantrell, DA; Crumpton, MJ; Graves, JD; Lucas, SC, 1990
)
0.28
" Additional dosing regimens were examined to determine whether the down-regulation of particulate PKC activity was associated with hyperplasia and tumor promotion."( Differential down-regulation of epidermal protein kinase C by 12-O-tetradecanoylphorbol-13-acetate and diacylglycerol: association with epidermal hyperplasia and tumor promotion.
Hansen, LA; Monteiro-Riviere, NA; Smart, RC, 1990
)
0.28
" Extracellular calcium, 1 mM produced a slight shift of the histone dose-response curve to the right."( Histamine release induced by histone and phorbol ester from rat peritoneal mast cells.
Foreman, JC; Sagi-Eisenberg, R; Shelly, R, 1985
)
0.27
" In dose-response studies, PMA stimulated amylase release independently of db-cAMP, but potentiated the effect of carbachol."( Phorbol ester stimulates amylase secretion from rat parotid cells.
Ichida, T; Takuma, T, 1986
)
0.27
" This enhancement is particularly striking at decreased effector:target ratios (as low as one effector per five targets) and is also demonstrated by a shift to lower concentrations of the phorbol diester dose-response curve."( Enhancement of phorbol diester-induced HL-60-mediated cytotoxicity by retinoic acid, dimethyl sulfoxide, and 5-azacytidine.
Hall, RE; Leftwich, JA, 1986
)
0.27
" In the presence of TMB-8 the dose-response curve for carbachol-induced amylase release shifts to the right, suggesting competitive antagonism at the muscarinic receptor."( Stimulatory and inhibitory effects of TMB-8 on pancreatic enzyme secretion.
De Pont, JJ; Van Nooij, IG; Willems, PH, 1986
)
0.27
" Acini preexposed to concentrations of carbamylcholine of 10(-6) M or greater showed shifts to the right in the subsequent carbamylcholine dose-response curves of amylase release."( Short-term cholinergic desensitization of rat pancreatic secretory response.
Asselin, J; Larose, L; Morisset, J, 1987
)
0.27
" Thus, palytoxin exhibited a biphasic dose-response curve for enhanced bone resorption, with stimulation at low concentrations (0."( Palytoxin: an extraordinarily potent stimulator of prostaglandin production and bone resorption in cultured mouse calvariae.
Fujiki, H; Lazzaro, M; Levine, L; Tashjian, AH, 1987
)
0.27
" Dose-response curves for CCK-8- or CCh-stimulated amylase release in TPA-pretreated acini revealed attenuation of both maximal efficacy and sensitivity."( Downregulation of protein kinase C in guinea pig pancreatic acini: effects on secretion.
Hootman, SR; Kuroiwa, C; Stuenkel, EL; Sung, CK; Williams, JA, 1988
)
0.27
" Further, the maximal' dose-response curve to VIP shifted 2 log units to the left (3 x 10(-9) versus 3 x 10(-7) M)."( Phorbol ester potentiates VIP-stimulated amylase release in rat pancreatic acini.
Firmansyah, A; Lebenthal, E; Lee, PC; Leung, YK; Suwandito, L, 1989
)
0.28
" The most effective inhibitory dosage with maximal carbachol (10(-5) M; 30."( Prostaglandin E analogue inhibition of pancreatic enzyme secretion.
Adrian, TE; Bilchik, AJ; Modlin, IM; Zucker, KA, 1989
)
0.28
" The diacylglycerols OAG and diC8 produced biphasic dose-response curves leading to rounding up of cells at very high stimulant concentrations."( Diacylglycerols and PMA induce actin polymerization and distinct shape changes in lymphocytes: relation to fluid pinocytosis and locomotion.
Keller, HU; Niggli, V; Zimmermann, A, 1989
)
0.28
" Chlordiazepoxide shifted the dose-response curves for TRH stimulation of PRL release and synthesis to the right, and did not change PRL release alone."( Pituitary thyrotropin-releasing hormone (TRH) receptors: effects of TRH, drugs mimicking TRH action, and chlordiazepoxide.
Hinkle, PM; Shanshala, ED, 1989
)
0.28
" At each fixed frequency of TPA application, there was a good dose-response of TPA in mouse skin papilloma incidence."( Dose and frequency effect in mouse skin tumor promotion.
Becher, H; Chouroulinkov, I; Day, NE; Lasne, C; Lowy, R; Wahrendorf, J; Yamasaki, H, 1989
)
0.28
" The dosage of OHM for inducing a comparable degree of acute and chronic hyperplasia to that induced by mezerein was 3- to 10-fold higher."( Comparison of octahydromezerein and mezerein as protein kinase C activators and as mouse skin tumor promoters.
Blumberg, PM; Hennings, H; Sharkey, NA; Yuspa, SH, 1989
)
0.28
" The dose-response curve for 0-10% CO2 was S-shaped."( Regulation of lung surfactant secretion by intracellular pH.
Chander, A, 1989
)
0.28
" A U-shaped dose-response relation was observed."( Beta-endorphin and related peptides suppress phorbol myristate acetate-induced respiratory burst in human polymorphonuclear leukocytes.
de Wied, D; Diamant, M; Henricks, PA; Nijkamp, FP, 1989
)
0.28
" Dose-response studies indicate that the desensitization was associated with a major reduction in the maximal extent of agonist-induced responses."( Homologous desensitization of muscarinic cholinergic, histaminergic, adrenergic, and serotonergic receptors coupled to phospholipase C in cerebellar granule cells.
Chuang, DM; Dillon-Carter, O, 1989
)
0.28
" In contrast, ecto-5'-NT-positive and -negative T cells showed markedly different dose-response curves for proliferation in response to PMA."( Functional characterization of ecto-5'-nucleotidase-positive and -negative human T lymphocytes.
Ruedi, JM; Thompson, LF, 1989
)
0.28
" The OAG effect on testosterone production was inhibitory throughout the dose-response curve of 8-bromo-cAMP."( Effects of protein kinase C activation on cyclic AMP and testosterone production of rat Leydig cells in vitro.
Huhtaniemi, I; Nikula, H, 1989
)
0.28
" The time course and dose-response for the effect of PMA at 23 degrees C closely correlate with the phosphorylation of a set of relatively "slowly" phosphorylated proteins (P20, P35, P41, P60), but not the rapidly phosphorylated P47 protein."( Synergistic release of arachidonic acid from platelets by activators of protein kinase C and Ca2+ ionophores. Evidence for the role of protein phosphorylation in the activation of phospholipase A2 and independence from the Na+/H+ exchanger.
Banga, HS; Feinstein, MB; Halenda, SP; Lau, LF; Zavoico, GB, 1989
)
0.28
" Dose-response curves for agonist-induced pHi increases were shifted to the right by a factor of 10 for segments suspended in KHB + HCO3."( The presence of HCO3- does not inhibit alpha-adrenergic increases in proximal tubular intracellular pH.
Gesek, FA; Schoolwerth, AC,
)
0.13
" Additionally, on this dosing regimen, the peak of ODC activity shifted to approximately 4 h after the last treatment, so that the time-course of ODC induction resembled that after multiple applications of TPA."( Characterization of the induction of ornithine decarboxylase activity by benzoyl peroxide in SENCAR mouse epidermis.
Binder, RL; Motz, AA; Volpenhein, ME, 1989
)
0.28
" The dose-response relationships for activation of phospholipase D and stimulation of thymidine incorporation by PDGF and TPA were comparable."( Phospholipase D activation by the mitogens platelet-derived growth factor and 12-O-tetradecanoylphorbol 13-acetate in NIH-3T3 cells.
Ben-Av, P; Liscovitch, M, 1989
)
0.28
" The phosphorylation of pp63 and pp66, in particular, correlated with the mitogenic dose-response curve."( Mitogen-induced phosphorylation of human B-lymphocyte proteins. Relationship to protein kinase C activation.
Finney, M; Gordon, J; Guy, GR; Michell, RH, 1989
)
0.28
" The dose-response curves for enhancement of MNNG-induced transformation and induction of aryl hydrocarbon hydroxylase activity by TCDD were similar."( 2,3,7,8-Tetrachlorodibenzo-p-dioxin enhancement of N-methyl-N'-nitro-N-nitrosoguanidine-induced transformation of rat tracheal epithelial cells in culture.
Barrett, JC; Gray, T; Nelson, K; Nettesheim, P; Tanaka, N, 1989
)
0.28
" sn-1,2-Didecanoylglycerol was evaluated as a complete skin tumor promoter in CD-1 mice utilizing a dosing regimen demonstrated to produce epidermal hyperplasia."( Synthetic lipid second messenger sn-1,2-didecanoylglycerol: a complete tumor promoter in mouse skin.
Conney, AH; Hansen, LA; Mills, KJ; Smart, RC, 1989
)
0.28
" The neutrophil dose-response curve for increase in XO paralleled closely the curve for neutrophil-mediated RPAEC cytotoxicity."( Xanthine oxidase activity in rat pulmonary artery endothelial cells and its alteration by activated neutrophils.
Gannon, DE; Phan, SH; Ryan, US; Varani, J; Ward, PA, 1989
)
0.28
" To resolve this discrepancy, we investigated the dose-response to phorbol esters of both baseline and potentiated granule cell responses elicited with perforant path stimulation."( Dose-dependent phorbol ester facilitation or blockade of hippocampal long-term potentiation: relation to membrane/cytosol distribution of protein kinase C activity.
Colley, PA; Routtenberg, A; Sheu, FS, 1989
)
0.28
" Noteworthy is that TFP in the dosage range used in SLDT experiments showed inhibitory effect on cell growth and DNA synthesis of MGC-803 cells documented in parallel experiments."( [Studies on the gap junctional intercellular communication (GJIC) of human stomach carcinoma cells in comparison with normal cells and the effect of the tumor promoter, TPA].
Han, YL; Lin, ZX; Trosko, JE; Zhang, RF; Zhau, YL, 1989
)
0.28
" The dose-response relationship between TPA concentration and induced differentiation is relatively steep."( Induction of HL-60 monocytic cell differentiation promoted by a perturbation of DNA synthesis: hydroxyurea promotes action of TPA.
Fishbaugh, J; Freeman, L; Yen, A, 1988
)
0.27
" Co-incubation of cells with 1 microM A23187 caused parallel upward shift of the TPA dose-response curve, and the further addition of 10 microM forskolin led to further upward shift."( Mechanisms of TSH release: studies with forskolin, phorbol ester and A23187.
Davis, JR; Sheppard, MC, 1987
)
0.27
" This decrease paralleled the time course and dose-response of the inhibition of cytocidal activity."( Tumor necrosis factor receptors and cytocidal activity are down-regulated by activators of protein kinase C.
Baglioni, C; Johnson, SE, 1988
)
0.27
" The dose-response curves for triggering of O2- release and membrane depolarization by each of receptor-mediated agonists in phorbol myristate acetate-pretreated or control cells were identical."( Phorbol myristate acetate potentiates superoxide release and membrane depolarization without affecting an increase in cytoplasmic free calcium in human granulocytes stimulated by the chemotactic peptide, lectins and the calcium ionophore.
Kitagawa, S; Miura, Y; Ohsaka, A; Saito, M; Suzuki, I; Takaku, F, 1988
)
0.27
" alpha 2-Adrenergic agonist preincubation also resulted in desensitization as indicated by a shift to the right in the dose-response curve of a subsequent challenge by an alpha 2-adrenergic agonist."( Characterization and possible mechanisms of alpha 2-adrenergic receptor-mediated sensitization of forskolin-stimulated cyclic AMP production in HT29 cells.
Bylund, DB; Jones, SB, 1988
)
0.27
" Using digitonin-permeabilized cells we showed that adenylate cyclase activity was stimulated by prostaglandin E1 with the same dose-response relationship as was cyclic AMP accumulation in intact cells, but the permeabilized cells showed no response to angiotensin II."( Angiotensin II potentiates prostaglandin stimulation of cyclic AMP levels in intact bovine adrenal medulla cells but not adenylate cyclase in permeabilized cells.
Boarder, MR; Marriott, DB; Plevin, R, 1988
)
0.27
" ANP stimulated production of cyclic GMP (cGMP), and inhibited aldosterone secretion with a similar dose-response relationship."( Regulation of aldosterone secretion by avian adrenocortical cells.
Hurwitz, S; Pines, M; Rosenberg, J, 1988
)
0.27
" The phorbol ester was shown to affect the dose-response relationship between the cAMP concentration and the relative amplitude of the light-scattering change, more by decreasing the number of cAMP receptors than by decreasing their apparent affinity for cAMP."( Phorbol 12-myristate 13-acetate modulates the cAMP-induced light-scattering response of a Dictyostelium discoïdeum cell population.
Klein, R; Tatischeff, I; Thiery, R, 1988
)
0.27
" There was a significant tumor incidence after the higher doses of TPA and a clear dose-response relationship."( TPA (12-O-tetradecanoyl-phorbol-13-acetate) as a carcinogen for mouse skin. A positive dose-response relationship.
Iversen, OH, 1985
)
0.27
" Our results indicate that dose protraction does not change the shape the dose-response curve for transformation, and that the shape change induced by TPA is also independent of dose protraction."( Effect of X-ray dose protraction and a tumor promoter on transformation induction in vitro.
Balcer-Kubiczek, EK; Harrison, GH, 1988
)
0.27
" Protein kinase C activators increased the apparent maximum of the ionophoretic dose-response curve for glutamate-induced depolarization, without affecting the reversal potential and the voltage-dependent decay rate for the excitatory postsynaptic current (EPSC) under voltage-clamp conditions."( Activation of protein kinase C promotes glutamate-mediated transmission at the neuromuscular junction of the mealworm.
Yamamoto, D, 1988
)
0.27
" The dose-response curves for the natural and recombinant factors were similar, with half-maximal responses at 2-3 ng/ml and maximal responses at approx."( Bombesin and platelet-derived growth factor stimulate formation of inositol phosphates and Ca2+ mobilization in Swiss 3T3 cells by different mechanisms.
Blakeley, DM; Brown, KD; Corps, AN, 1989
)
0.28
" Significantly, studies in this laboratory indicated that B6C3F1 mice dosed with BZP demonstrated increased NK activity in the spleen as was observed after dosing with TPA."( Modulation of natural killer activity by 12-O-tetradecanoylphorbol-13-acetate and benzoyl peroxide in phorbol ester-sensitive (SENCAR) and resistant (B6C3F1) mice.
Chuthaputti, A; Pfeifer, RW; Updyke, LW; Yim, GK, 1988
)
0.27
" Incubation of the neutrophils with cholera toxin, unlike pertussis toxin, did not inhibit the fMet-Leu-Phe induced rise in the intracellular concentration of free calcium, and caused only a shift to the right of the dose-response curve of N-acetyl-beta-glucosaminidase release."( Pertussis but not cholera toxin inhibits the stimulated increase in actin association with the cytoskeleton in rabbit neutrophils: role of the "G proteins" in stimulus-response coupling.
Becker, EL; Feinstein, MB; Molski, TF; Munoz, JJ; Naccache, PH; Sha'afi, RI; Shefcyk, J; Volpi, M; Yassin, R, 1985
)
0.27
" The effect of viable P haemolytica on macrophage viability was related to bacterial dosage and the presence of opsonizing antibody."( Production of superoxide anion by bovine pulmonary macrophages challenged with soluble and particulate stimuli.
Benson, CE; Boy, MG; Dyer, RM, 1985
)
0.27
" The dose-response curves for triggering of membrane potential changes and O2- release by PMA were identical."( Relationship between membrane potential changes and superoxide-releasing capacity in resident and activated mouse peritoneal macrophages.
Johnston, RB; Kitagawa, S, 1985
)
0.27
" The ACTH dose-response curves for steroidogenic activity and for polyamine uptake were similar."( Hormonal control of polyamine levels in bovine adrenocortical cells.
Chambaz, EM; Feige, JJ; Madani, C, 1986
)
0.27
" The dose-response curve for ODC induction by PTH was parallel to that of PTH-stimulated proteoglycan synthesis both in TPA-treated chondrocytes and in normal chondrocytes."( Comparison of inhibition by a tumor promoter (12-O-tetradecanoylphorbol-13-acetate) of expression of the differentiated phenotype of chondrocytes in rabbit costal chondrocytes in culture with inhibition by retinoic acid.
Enomoto, M; Fukuo, K; Kumahara, Y; Suzuki, F; Tajima, K; Takigawa, M, 1986
)
0.27
" Dose-response studies indicate the beta-adrenergic component of cyclic AMP stimulation is enhanced and the alpha 1-adrenergic component of cyclic GMP stimulation is diminished in LL pinealocytes."( See-saw signal processing in pinealocytes involves reciprocal changes in the alpha 1-adrenergic component of the cyclic GMP response and the beta-adrenergic component of the cyclic AMP response.
Klein, DC; Sugden, D; Vanecek, J; Weller, JL, 1986
)
0.27
" Dose-response studies indicated that phosphorylation of the 67 kilodalton protein was particularly sensitive to inhibition by quercetin at concentrations that also inhibit neutrophil degranulation and superoxide production."( The bioflavonoid quercetin inhibits neutrophil degranulation, superoxide production, and the phosphorylation of specific neutrophil proteins.
Blackburn, WD; Heck, LW; Wallace, RW, 1987
)
0.27
" This increase was not due to a shift in the PMA dose-response curve, a change in the time course of the PMA response, or an effect of decreased cell density on the assay system."( Exposure to gamma-irradiation increases phorbol myristate acetate-induced H2O2 production in human macrophages.
Gallin, EK; Green, SW, 1987
)
0.27
" Inhibition by topical retinoic acid of ODC induction by TPA was partially overcome in a dose-response fashion by PGE."( The role of prostaglandin E1 in ornithine decarboxylase induction by tumor promoters.
Boutwell, RK; Cleaveland, JS; Ordman, AB; Simsiman, RC, 1986
)
0.27
" The lymphocyte adhesion to the EC and the expression of DR antigens on the EC were well correlated in terms of both kinetics and the dose-response pattern of rIFN-gamma."( Mechanisms of lymphocyte adhesion to human vascular endothelial cells in culture. T lymphocyte adhesion to endothelial cells through endothelial HLA-DR antigens induced by gamma interferon.
Kano, S; Masuyama, J; Minato, N, 1986
)
0.27
" Phorbol ester dose-response curves for growth arrest and enzymatic markers of differentiation were shifted to lower concentrations when the ionophore was present."( Ca2+ and phorbol ester synergistically induce HL-60 differentiation.
Harley, CB; Tyers, M, 1986
)
0.27
" The SENCAR mouse model provides a good dose-response relationship for many carcinogens used as tumor initiators and for many compounds used as tumor promoter."( SENCAR mouse skin tumorigenesis model versus other strains and stocks of mice.
Slaga, TJ, 1986
)
0.27
" Furthermore, the magnitude of the translocation of protein kinase C from cytosol to plasma membrane corresponded to the physiologic IL 2 dose-response for IFN-gamma secretion."( Interleukin 2 induction of interferon-gamma mRNA synthesis.
Birchenall-Sparks, MC; Farrar, WL; Young, HB, 1986
)
0.27
" A similar dose-response relationship for papilloma and carcinoma formation was observed when chrysarobin was applied once weekly."( Characterization of skin tumor promotion and progression by chrysarobin in SENCAR mice.
Conti, CJ; DiGiovanni, J; Kruszewski, FH, 1987
)
0.27
" Overall the results show, in terms of the numbers of animals with tumours, the total numbers of tumours produced and the numbers of malignant tumours formed all in dose-response relationship, that the Swiss mice were the most sensitive and the B57B1/6 mice the least sensitive to the tumour-promoting effects of TPA with the DBA/2 mice occupying and intermediate position."( Sensitivity of the skin of different mouse strains to the promoting effect of 12-0-tetradecanoyl-phorbol-13-acetate.
Chouroulinkov, I; Grover, P; Lasne, C; Phillips, D, 1988
)
0.27
" Dose-response curves comparing 45Ca efflux and insulin secretion suggested that AA also stimulates hormone release by at least one other mechanism in addition to Ca2+ mobilization."( Exogenous arachidonic acid promotes insulin release from intact or permeabilized rat islets by dual mechanisms. Putative activation of Ca2+ mobilization and protein kinase C.
Metz, SA, 1988
)
0.27
" Unlike fmet-leu-phe and C5a, PMA elicited a biphasic dose-response curve."( Evidence for distinct intracellular pools of receptors for C3b and C3bi in human neutrophils.
Brown, EJ; Frank, MM; Gallin, JI; Metcalf, JA; O'Shea, JJ; Seligmann, BE, 1985
)
0.27
" This observation, together with the TPA dose-response effects on protein phosphorylation, is discussed in relation to multiple protein kinase involvement."( Changes in phosphoproteins during commitment of HL60 cells to monocyte differentiation: evidence for multiple protein kinase involvement.
Brown, G; Lord, JM; Wong, AK, 1988
)
0.27
" Dose-response curves of phorbol-12,13-dibutyrate-induced muscle tension and -stimulated kinase activity and receptor binding indicate that these responses are mediated by the same system."( Schistosoma mansoni: evidence for protein kinase-C-like modulation of muscle activity.
Bennett, JL; Blair, KL; Pax, RA, 1988
)
0.27
" The dose-response curve to calcium in 30 mM KCl-induced contraction was shifted to the left by PMA pretreatment and the EC50 value (the concentration producing a half maximal response) of calcium was significantly lower in aorta pretreated with PMA than in the control."( Role of calcium in the potentiating effect of phorbol ester on KCl-induced vasocontraction.
Hatake, K; Hishida, S; Kakishita, E; Nagai, K; Wakabayashi, I, 1988
)
0.27
" Pea lectin failed to display a dose-response relationship, and IL-2 production increased proportionally with lectin concentration."( Lectin interactions with the Jurkat leukemic T-cell line: quantitative binding studies and interleukin-2 production.
Bastin, B; Dupuis, G, 1988
)
0.27
" However, the dose-response curves of cells expressing mutant receptors were slightly shifted to lower concentrations of EGF, rendering the cells mitogenically responsive to lower doses of EGF than cells expressing normal EGF-receptor at similar expression levels."( Biological activities of EGF-receptor mutants with individually altered autophosphorylation sites.
Bellot, F; Dull, TJ; Honegger, A; Schlessinger, J; Schmidt, A; Szapary, D; Ullrich, A; Van Obberghen, E, 1988
)
0.27
" Furthermore, we have shown that insulin-generated diacylglycerol satisfies several criteria for a mediator of insulin action, including the demonstration that insulin-stimulated endogenous diacylglycerol generation is antecedent to glucose transport and has an identical insulin dose-response curve and moreover that the magnitude and time course of subsequent stimulation of glucose transport is reproduced by the addition of the simple exogenous diacylglyerol, dioctanoylglycerol, in the complete absence of the hormone."( Insulin-induced glycerolipid mediators and the stimulation of glucose transport in BC3H-1 myocytes.
Cooper, DR; Farese, RV; Pollet, RJ; Standaert, ML, 1988
)
0.27
" The dose-response curves for both protein kinase C translocation and cell growth inhibition show that diC8 exerts its effects on both parameters in the same range of concentrations, despite some discrepancies at the lowest doses."( 1,2-Dioctanoyl-glycerol induces a discrete but transient translocation of protein kinase C as well as the inhibition of MCF-7 cell proliferation.
Darbon, JM; Issandou, M, 1988
)
0.27
" The changes in rate of LH release investigated were the initial response to GnRH, desensitization, change of dose-response during desensitization, and recovery of sensitivity between pulses of stimulation."( Effects of modifiers of cytoskeletal structures on the dynamics of release of LH from sheep anterior pituitary cells stimulated with gonadotrophin-releasing hormone, K+ or phorbol ester.
McIntosh, JE; McIntosh, RP; Starling, L, 1987
)
0.27
" However, there was no strong dose-response relation."( [Modulation of the oxidative metabolism of granulocytes by nonsteroidal anti-inflammatory agents].
Kapp, A; Schöpf, E, 1987
)
0.27
" The dose-response curves for the binding of [3H]lyngbyatoxin A and [3H]debromoaplysiatoxin to a mouse epidermal particulate fraction are virtually the same as the one previously described for [3H]12-O-tetradecanoylphorbol-13-acetate ([3H]TPA)."( Binding studies of [3H]lyngbyatoxin A and [3H]debromoaplysiatoxin to the phorbol ester receptor in a mouse epidermal particulate fraction.
Entzeroth, M; Fujiki, H; Hakii, H; Moore, RE; Morimoto, H; Patterson, GM; Suganuma, M; Sugimura, T, 1986
)
0.27
" So the use of this orthogonal design in cell culture has many advantages: several factors can be tested simultaneously; it is easy to find the optimal protocol conditions and the dose-response relationship is stable, which enables the reproducibility to be improved."( Use of an orthogonal design method to study two-stage chemical carcinogenesis in BALB/3T3 cells.
Chouroulinkov, I; Lasne, C; Lu, YP, 1986
)
0.27
" A time course and the dose-response curves of ODC induction paralleled that of ODC mRNA induction by TPA in MEC."( Involvement of protein kinase C activation in ornithine decarboxylase gene expression in primary culture of newborn mouse epidermal cells and in skin tumor promotion by 12-O-tetradecanoylphorbol-13-acetate.
Erickson, D; Pong, RC; Verma, AK, 1986
)
0.27
" The dose-response curve for TPA-induced inhibition reveals that quite a high concentration of TPA is necessary to block angiotensin action compared with that needed to stimulate aldosterone secretion."( Phorbol ester inhibits angiotensin-induced activation of phospholipase C in adrenal glomerulosa cells. Its implication in the sustained action of angiotensin.
Kojima, I; Ogata, E; Shibata, H, 1986
)
0.27
" The ED50 for TRH stimulation of hormone release was increased 2- to 4-fold in down-regulated cells, but the dose-response curves for other secretagogues were not shifted."( Differential effects of thyrotropin-releasing hormone, vasoactive intestinal peptide, phorbol ester, and depolarization in GH4C1 rat pituitary cells.
Aizawa, T; Hinkle, PM, 1985
)
0.27
" In addition, a simplified, once daily dosage of DFMO appears adequate."( Inhibition of ornithine decarboxylase activity by small doses of alpha-difluoromethylornithine.
Loprinzi, CL; Verma, AK, 1985
)
0.27
" Leukotrienes, the chemotactic fragment of the fifth component of complement (C5a des arg), N-formyl-L-methionylyl-L-leucyl-L-phenylalanine (FMLP), platelet-activating factor (PAF), and phorbol myristate acetate (PMA) increased the nonadherence of human leukocytes to glass with bell-shaped dose-response curves."( Various authentic chemoattractants mediating leukocyte adherence inhibition.
Thomson, DM, 1984
)
0.27
" Inhibition of aggregation by the beta-adrenoceptor antagonists was manifested as a parallel shift to the right in the dose-response curve."( Beta-adrenoceptor antagonists and human platelets: relationship of effects to lipid solubility.
Kerry, R; Scrutton, MC; Wallis, RB, 1984
)
0.27
" The anti-IgE dose-response pattern of this activation event further suggests that it is an integral part of the anti-IgE-induced release process itself."( Release of histamine from human leukocytes stimulated with the tumor-promoting phorbol diesters. II. Interaction with other stimuli.
Daiuta, R; Gillespie, E; Lichtenstein, LM; Schleimer, RP, 1982
)
0.26
" The IFN resembles human IFN-gamma by the following criteria: lability at pH 2, stability against 2-mercaptoethanol, cross-species activity, shape of dose-response curves, and molecular weight determined by size-exclusion chromatography (50,000-55,000)."( Lymphokines produced by herpesvirus-transformed marmoset monkey lymphoid cell lines. I. Characterization of a constitutively produced interferon.
Adolf, GR, 1984
)
0.27
" Kinetic dose-response studies showed that the number of cells induced to release virus was dependent on TPA concentration and the time of assay following TPA exposure."( Induction of type-C retrovirus by the tumor promotor TPA.
Hellman, A; Hellman, KB, 1981
)
0.26
" This conclusion was based on the kinetics and dose-response relationships for the effects of azide and cyanide on H2O2 release and on the activities of catalase and myeloperoxidase."( Hydrogen peroxide metabolism in human monocytes during differentiation in vitro.
Cohn, ZA; Nakagawara, A; Nathan, CF, 1981
)
0.26
" A positive dose-response relationship in transformation by benzo[a]pyrene occurred."( Equivalency of endothelial cell growth supplement to irradiated feeder cells in carcinogen-induced morphologic transformation of Syrian hamster embryo cells.
DiPaolo, JA; Evans, CH, 1982
)
0.26
" Treatment of 20:4 with soybean lipoxygenase did not abolish its capacity to induce O2- production; native and lipoxygenase-treated 20:4 exhibited similar dose-response ratios."( Unsaturated fatty acids as second messengers of superoxide generation by macrophages.
Bromberg, Y; Pick, E, 1983
)
0.27
" Despite such a down regulation of phorbol ester receptors, these cells respond to PMA with a dose-response similar to that of their parent cells, which have the normal number of phorbol ester receptors."( Continuous suppression of globin gene expression and differentiation of Friend erythroleukemia cells by phorbol 12-myristate 13-acetate (PMA) despite the loss of PMA binding sites by down regulation.
Fusco, A; Martel, N; Ostertag, W; Yamasaki, H, 1984
)
0.27
" However, IFN-gamma dose-response studies using both HL-60 cells and a nondifferentiation variant of HL-60 cells (HL-60 blast) clearly show that induction of transcription and expression of HLA-D gene products by IFN-gamma can be uncoupled from expression of other monocyte-macrophage characteristics."( Gamma-interferon induces expression of the HLA-D antigens on normal and leukemic human myeloid cells.
Billing, R; Bohman, R; Koeffler, HP; Ranyard, J; Yelton, L, 1984
)
0.27
" By varying the concentration of the test chemicals, it is possible to study dose-response relationships, and by changing the pellet matrix, the effects of release rate (dose rate) can be analyzed."( Heterotopic tracheal transplants: techniques and applications.
Klein-Szanto, AJ; Marchok, AC; Pal, BC; Terzaghi, M, 1984
)
0.27
" The signal for priming could be clearly distinguished from the signal causing oxidase activation by the dose-response curves for each, as well as by the use of several pharmacologic agents."( The NADPH oxidase of human polymorphonuclear leukocytes. Evidence for regulation by multiple signals.
Clayton, CC; McPhail, LC; Snyderman, R, 1984
)
0.27
" Dose-response relationships for the radiomimetic activity of phorbol derivatives in HeLa cells (Kinzel et al."( Interaction of phorbol derivatives with replicating cells.
Fürstenberger, G; Goerttler, K; Kinzel, V; Loehrke, H; Marks, F; Richards, J, 1984
)
0.27
" Dose-response results with 12-O-tetradecanoylphorbol-13-acetate (TPA) plus X-irradiation parallel those obtained on mouse skin."( Inhibition of radiation-initiated and -promoted transformation of Syrian hamster embryo cells by lymphotoxin.
DeMarinis, AJ; DiPaolo, JA; Doniger, J; Evans, CH, 1984
)
0.27
"The dose-response relationships from the data described in Paper I were analysed."( Initiation and promotion at different ages and doses in 2200 mice. III. Linear extrapolation from high doses may underestimate low-dose tumour risks.
Peto, R; Shubik, P; Stenbäck, F, 1981
)
0.26
" The dose-response curves of these two compounds were, in general, similar to that of 12-O-tetradecanoyl-phorbol-13-acetate, a powerful mouse skin tumor promoter."( Inhibition of intercellular communication in Chinese hamster V79 cells by teleocidin.
Chang, C; Fujiki, H; Jone, CM; Sugimura, T; Trosko, JE, 1982
)
0.26
" SF from both gene-carriers and normal individuals displayed an unusual biphasic dose-response (concaved upward), but the latter were considerably more sensitive to the toxic effects of this probe at all concentrations tested."( The use of a tumor promoter for the detection of individuals with the Gardner syndrome.
Gardner, EJ; Kopelovich, L, 1983
)
0.27
" Furthermore, a dose-response reduction in tumor size was observed."( Diazepam inhibition of phorbol ester tumor promotion.
Fischer, SM; Hardin, LG; Slaga, TJ, 1983
)
0.27
" The dose-response curve for EGF is bell-shaped, in contrast to the more classically shaped dose-response curve obtained with NGF."( Tumor promoter modulation of epidermal growth factor- and nerve growth factor-induced adhesion and growth factor binding of PC-12 pheochromocytoma cells.
Chandler, CE; Herschman, HR, 1980
)
0.26
"In the studies described here, we demonstrated a unique dose-response (concaved upward) to TPA in sparse human cell cultures and a dose-dependent stimulation of cell proliferation in confluent cultures, suggesting a functional difference in putative TPA receptors between these two conditions."( Genetic forms of neoplasia in man: a model for the study of tumor promotion in vitro.
Kopelovich, L, 1982
)
0.26
" The dose-response relationship was determined, and the validity of the tetrazolium test was confirmed."( Dose response in the tetrazolium test for skin carcinogenicity.
Iversen, OH, 1980
)
0.26
" Seven of 11 anergic cancer patients have been immunorestored by a relatively low dosage of azimexon."( Immunorestoration of anergic cancer patients by azimexon.
Bonardelle, D; Goutner, A; Nasrat, F; Rameau, G, 1980
)
0.26
" Skin fibroblasts (SF) from both colorectal-prone and normal individuals displayed an unusual biphasic dose-response relationship, but the latter are considerably more sensitive to the toxic effects of TPA."( The use of a tumor promoter as a single parameter approach for the detection of individuals genetically predisposed to colorectal cancer.
Kopelovich, L, 1981
)
0.26
" Based on the inhibitory effect of the steroidal anti-inflammatory drugs, non-steroidal agents, such as indomethacin, were also expected to show some degree of inhibition; however, repeated tumor experiments demonstrate that indomethacin enhances TPA promotion in a dose-response manner."( Indomethacin enhancement of TPA tumor promotion in mice.
Fischer, SM; Gleason, GL; Mills, GD; Slaga, TJ, 1980
)
0.26
" Dose-response curves revealed that the antigen-presenting capacity of activated, MHC class II+, B7+ T cells was comparable to the one of B-LCL."( Antigen-presenting human T cells and antigen-presenting B cells induce a similar cytokine profile in specific T cell clones.
Frutig, K; Gallati, H; Limat, A; Mauri, D; Pichler, WJ; Pracht, I; Wyss-Coray, T, 1993
)
0.29
" The dose-response curves of induction of HGF secretion by cholera toxin and forskolin were nearly parallel with those of the intracellular cAMP levels."( Expression of hepatocyte growth factor is up-regulated through activation of a cAMP-mediated pathway.
Gohda, E; Iwao, M; Kataoka, H; Matsunaga, T; Takebe, T; Wu, YL; Yamamoto, I, 1994
)
0.29
" A dose-response inhibition was demonstrated with maximum inhibition observed at 3 hr of exposure."( Gap junction-mediated intercellular communication in primary cultures of rainbow trout hepatocytes.
Baldwin, LA; Calabrese, EJ, 1994
)
0.29
" The ADR dose-response curve is significantly shifted to the right when cells were preincubated with the unspecific phosphodiesterase inhibitor IBMX."( Study of the activation mechanism of adriamycin on rat mast cells.
Botana, LM; Estévez, MD; Vieytes, MR, 1994
)
0.29
" The PKC activator TPA amplifies the response of mast cells to human GRF, shifting the dose-response curve to the left."( Study of the activation mechanism of human GRF(1-29)NH2 on rat mast cell histamine release.
Alfonso, A; Botana, LM; Estévez, MD; Louzao, MC; Vieytes, MR, 1995
)
0.29
" Close correspondence between the dose-response curves of 45Ca2+ uptake and TRE-binding activity by NMDA or KA suggested that Ca2+ influx not only triggered sequential activation of Ca(2+)-signaling processes leading to the increase in TRE-binding activity, but also controlled its increased level."( Involvement of protein kinase C in Ca(2+)-signaling pathways to activation of AP-1 DNA-binding activity evoked via NMDA- and voltage-gated Ca2+ channels.
Iwata, E; Oh, E; Ohtani, K; Sakurai, H; Tsuchiya, T; Tsuda, M, 1995
)
0.29
" The dose-response curve displayed a biphasic bell-shaped superoxide generation profile with two specific concentration optima for each individual blood donor, but with variations in optimal concentrations between the donors."( Superoxide anion generation by human peripheral blood mononuclear cells in response to prothymosin alpha.
Aliverti, A; Galaris, D; Tsolas, O, 1995
)
0.29
" In extracts from cells pretreated with glutamate, the activity-Ca2+ concentration dose-response relationship of the 13."( Glutamate stably enhances the activity of two cytosolic forms of phospholipase A2 in brain cortical cultures.
Bonventre, JV; Kim, DK; Koroshetz, WJ; Nemenoff, RA; Rordorf, G, 1995
)
0.29
" Exposure of transfected cells to human chorionic gonadotropin (hCG) resulted in a dose-dependent loss of maximal hCG-stimulable adenylyl cyclase activity without a significant shift to the right of the dose-response curve to hCG."( Homologous desensitization of the murine luteinizing hormone receptor expressed in L cells.
Birnbaumer, L; Birnbaumer, M; Gudermann, T, 1995
)
0.29
" The dose-response curves defining the TPA-dependent suppression of EROD induction and PKC down-regulation were very similar, as were the initial kinetics of PKC loss and the times of TPA pretreatment required for suppression of EROD induction."( Suppression of cytochrome P450 Cyp1a-1 induction in murine hepatoma 1c1c7 cells by 12-O-tetradecanoylphorbol-13-acetate and inhibitors of protein kinase C.
Bischer, P; Cantu, AR; Pavone, A; Reiners, JJ; Schöller, A, 1993
)
0.29
" TPA also shifted the dose-response curve of 1,25-(OH)2D3 to the left, so that 1,25-(OH)2D3 was effective at a concentration as low as 1 nM."( Effects of 1,25-dihydroxyvitamin D3 and phorbol ester on 25-hydroxyvitamin D3 24-hydroxylase cytochrome P450 messenger ribonucleic acid levels in primary cultures of rat renal cells.
Armbrecht, HJ; Boltz, MA; Chen, ML, 1993
)
0.29
" Dose-response analysis revealed that maximal reduction of IL-1 binding was reached at FMLP concentrations that were also optimal for chemotaxis (50% effective dose = 5 x 10(-9) M)."( Chemoattractants induce rapid release of the interleukin 1 type II decoy receptor in human polymorphonuclear cells.
Colotta, F; Fadlon, EJ; Mantovani, A; Matteucci, C; Orlando, S; Sozzani, S, 1995
)
0.29
" This study illustrates that PGE2 dose-response curves may reflect different mechanisms of action that may be intimately associated with skin irritant and tumour promoting activity."( Comparison of tumour promoter-induced prostaglandin E2 release in human and rat keratinocytes.
Benford, DJ; Lawrence, JN, 1995
)
0.29
" Comparison of the dose-response curves for carbamylcholine-induced pepsinogen secretion and alpha PKC membrane-association indicates that PKC translocation is not required for carbamylcholine-induced secretion."( Protein kinase C expression and translocation in dispersed chief cells from guinea-pig stomach.
Raffaniello, RD; Raufman, JP, 1994
)
0.29
" This stimulation was mediated by ER, because 1) dose-response curves established with tamoxifen and hydroxytamoxifen were in agreement with their affinity for ER; 2) when present with antiestrogens, estradiol abolished this phenomenon; and 3) this effect was not observed in MDT (ER-negative) cells."( Prolonged treatment of breast cancer cells with antiestrogens increases the activating protein-1-mediated response: involvement of the estrogen receptor.
Astruc, ME; Bali, P; Chabret, C; Gagne, D; Pons, M, 1995
)
0.29
" Dose-response curves were remarkably similar for all three compounds."( Methyl mercury, mercuric chloride, and silver lactate decrease superoxide anion formation and chemotaxis in human polymorphonuclear leucocytes.
Christensen, MM; Hansen, B; Nielsen, SL; Obel, N; Rungby, J, 1993
)
0.29
" By investigating the dose-response relationships of these phenomena, we have found that: (a) resting neutrophils do not produce a significant amount of superoxide (O2-) and show only minimal adhesion to serum-coated plastic surfaces; (b) fully activatory doses (> 5 x 10(-8) M) of fMLP induce the release of O2- and a significant increase of the cell adhesion; (c) pretreatment of the cells for 1 h with LPS augments cell adhesion to serum-coated culture wells in the absence of further stimulation and primes the neutrophils to enhanced fMLP-dependent O2- release; (d) addition of low, substimulatory doses of fMLP (from 10(-10) M to 5 x 10(-9) M) inhibits and reverses the adhesion of LPS-treated cells, (e) high fMLP doses ( > 10(-7) M) are additive to LPS in promoting adhesion."( Dual effects of formylpeptides on the adhesion of endotoxin-primed human neutrophils.
Andrioli, G; Bellavite, P; Bonazzi, L; Chirumbolo, S; Ferro, I; Lippi, G, 1993
)
0.29
" The dose-response curve of adenylate cyclase to the GTP analogue, GppNHp, was modified by 5HT, which promotes a significantly higher maximal response without altering the potency of GppNHp."( Heterologous sensitization of adenylate cyclase activity by serotonin in the rat cerebral cortex.
Brunello, N; Perez, J; Racagni, G; Rovescalli, AC; Steardo, L; Vitali, S, 1993
)
0.29
" In the beta cell of aged rats, the following abnormalities were found: (a) right shift of the dose-response curve (depressed sensitivity) of glucose-induced insulin release, (b) no increase of the maximum response to glucose in the face of increased insulin content of the islets (reduced responsiveness), (c) no response to forskolin and normal response to the phorbol ester and glyburide, and (d) increased sensitivity to nifedipine."( Insulin secretion by the pancreatic beta cell of aged rats.
Aizawa, T; Hashizume, K; Ishihara, F; Komatsu, M; Nishii, N; Sato, Y; Suzuki, N; Yamada, T, 1994
)
0.29
" In dose-response experiments, NGFI-A and c-fos gene activation parallels the induction of death in LNCaP cells."( Phorbol ester-induced apoptosis is accompanied by NGFI-A and c-fos activation in androgen-sensitive prostate cancer cells.
Day, ML; Humphrey, PA; Swanson, PE; Wu, S; Zhao, X, 1994
)
0.29
" Bryostatin 1 was 40-fold more potent than PMA for down-regulating PKC-alpha and showed a biphasic dose-response curve for down-regulating PKC-delta."( Bryostatin 1 protects protein kinase C-delta from down-regulation in mouse keratinocytes in parallel with its inhibition of phorbol ester-induced differentiation.
Blumberg, PM; Denning, MF; Dlugosz, AA; Pettit, GR; Smith, CB; Szallasi, Z; Yuspa, SH, 1994
)
0.29
"The dose-response curves for the inhibition of equilibrative uridine transport by dilazep, dipyridamole and nitrobenzylthioinosine (NBMPR) in undifferentiated HL-60 cells were biphasic."( Decrease in equilibrative uridine transport during monocytic differentiation of HL-60 leukaemia: involvement of protein kinase C.
Lee, CW, 1994
)
0.29
" In contrast, the dose-response curves of 5-HT-induced IPs accumulation were not shifted until the concentrations of NAN-190 and metoclopramide (5-HT1A and 5-HT3 receptor antagonists, respectively) were increased up to 10 microM."( 5-Hydroxytryptamine receptor-mediated phosphoinositide hydrolysis in canine cultured tracheal smooth muscle cells.
Hsieh, JT; Ong, R; Yang, CM; Yo, YL, 1994
)
0.29
" The only dose-response curves that differed in slope between thermal groups were those produced by the TSH response to TRH (p < ."( Somatotroph, lactotroph and thyrotroph function in three-week-old gilts reared in a hot or cool environment.
Becker, BA; Matteri, RL, 1994
)
0.29
" In experiment 3, explants were incubated in the presence of oxytocin or arginine vasopressin at 10(-9) to 10(-6) M to establish dose-response curves for the activation of PLC and release of PGF2 alpha."( Cellular mechanisms mediating the stimulation of ovine endometrial secretion of prostaglandin F2 alpha in response to oxytocin: role of phospholipase C and diacylglycerol.
Brockman, JA; Hayes, SH; Lee, JS; Lowberger, LL; Silvia, WJ; Trammell, DS, 1994
)
0.29
" Interpolating from the dose-response curve taken before desensitization, this is equivalent to an average 23% reduction in the number of muscarinic receptors."( Measurement of changes in functional muscarinic acetylcholine receptor density in single neuroblastoma cells using calcium release kinetics.
Thompson, SH; Wang, SS, 1994
)
0.29
" A strong correlation between phosphate incorporation into guanylate cyclase and increased cGMP level was also observed by time-course and dose-response studies of the PMA effect, as well as when cells were treated with various phorbol esters and diacylglycerols or with various protein kinase C inhibitors."( Activation of soluble guanylate cyclase through phosphorylation by protein kinase C in intact PC12 cells.
Louis, JC; Revel, MO; Zwiller, J, 1993
)
0.29
" The dose-response for calcium release induced by sphingosine-1-phosphate correlated closely with the concentration required for stimulation of DNA synthesis."( Sphingosine-1-phosphate, a putative second messenger, mobilizes calcium from internal stores via an inositol trisphosphate-independent pathway.
Brooker, G; Mattie, M; Spiegel, S, 1994
)
0.29
" The dose-response and temporal analysis of CGRP effect show that the maximal activity is present at the dose of 30 pmol/ear and when administered 30 min after the irritating agent."( Effects of CGRP in different models of mouse ear inflammation.
Amico-Roxas, M; Caruso, A; Catena Cutuli, VM; Clementi, G; de Bernardis, E; Maugeri, S; Prato, A; Scapagnini, U, 1994
)
0.29
" Bryo and PMA activated PBL- or T cell-derived PKC in a similar dose-response and induced a similar time kinetic of cytosol-to-membrane translocation of enzymatically active and immunoreactive PKC."( The effect of bryostatin on protein kinase C-regulated functions in human T lymphocytes and epidermal keratinocytes.
Galron, D; Gelkop, S; Grossman, N; Isakov, N; Tamir, A, 1993
)
0.29
" The dose-response of insulin effect shows a behavior typical of other insulin responses: a maximum in the physiological range (1 nM) and smaller effects at higher and lower hormone concentrations."( Modulation of the Na-H antiport by insulin: interplay between protein kinase C, tyrosine kinase, and protein phosphatases.
Baldini, P; Bellucci, V; Incerpi, S; Luly, P; Zannetti, A, 1994
)
0.29
" Stimulation of DNA synthesis and inhibition of cAMP accumulation by LPA were inhibited by pertussis toxin, but with different dose-response characteristics."( A novel synergistic stimulation of Swiss 3T3 cells by extracellular ATP and mitogens with opposite effects on cAMP levels.
Heller, EJ; Heppel, LA; Huang, NN; Wang, DJ, 1994
)
0.29
" The dose-response curves showed that tyrosine phosphorylation and O2- release were stimulated in parallel by PMA, whereas tyrosine phosphorylation and an increase in [Ca2+]i, but not O2- release, were stimulated in parallel by FMLP or ionomycin."( Activation of the respiratory burst and tyrosine phosphorylation of proteins in human neutrophils: no direct relationship and involvement of protein kinase C-dependent and -independent signaling pathways.
Azuma, EK; Kitagawa, S; Mizoguchi, H; Saito, M; Takaku, F; Umezawa, K; Yuo, A, 1993
)
0.29
"Mitoxantrone has been shown in vitro to exhibit a steep dose-response relationship with respect to the clonogenic survival of acute myeloid leukemia cells."( High-dose mitoxantrone induces programmed cell death or apoptosis in human myeloid leukemia cells.
Bhalla, K; Bullock, G; Grant, S; Huang, Y; Ibrado, AM; Mahoney, ME; Ponnathpur, V; Tang, C; Tourkina, E, 1993
)
0.29
" High dosage LDL and insulin may keep SMC away from normal growth control and induce their proliferation by means of inhibiting junctional communication."( [Studies on gap junction formation and junctional communication between cultured endothelial cells and smooth muscle cells].
Lou, DA; Zhang, R, 1993
)
0.29
" TPA markedly enhanced both haptotactic response to type-IV collagen and motility on tissue-culture glass substrate of L-10 cells in a dose-response manner quite similar to that of TPA-enhanced invasion of Matrigel."( TPA-enhanced invasion of Matrigel associated with augmentation of cell motility but not metalloproteinase activity in a highly metastatic variant (L-10) of human rectal adenocarcinoma cell line RCM-1.
Hayakawa, T; Inoue, T; Kishi, J; Koita, H; Komada, N; Koono, M; Nabeshima, K, 1993
)
0.29
" Staurosporin potentiated Ca(2+)-induced Peth formation by shifting the [Ca2+]cyt dose-response curve to the left."( The role of cytosolic Ca2+, protein kinase C, and protein kinase A in hormonal stimulation of phospholipase D in rat hepatocytes.
Benistant, C; Gustavsson, L; Hoek, JB; Moehren, G; Rubin, R; Torres-Marquez, ME, 1994
)
0.29
" Bryostatin 1 was markedly more potent than PMA for translocating PKC delta but showed a biphasic dose-response curve for down-regulating this isozyme."( Differential regulation of protein kinase C isozymes by bryostatin 1 and phorbol 12-myristate 13-acetate in NIH 3T3 fibroblasts.
Blumberg, PM; Pettit, GR; Smith, CB; Szallasi, Z, 1994
)
0.29
"14 microM Ro 31-8220) and shifted the dose-response curve for the effect of carbachol concentration of aminopyrine accumulation downwards and to the right."( Inhibition by Ro 31-8220 of acid secretory activity induced by carbachol indicates a stimulatory role for protein kinase C in the action of muscarinic agonists on isolated rat parietal cells.
Hanson, PJ; McKenna, JP, 1993
)
0.29
" The dexamethasone dose-response curves were similar, except that a greater proportion of spleen T cells were dexamethasone-resistant."( Regulation of apoptosis in vitro in mature murine spleen T cells.
Ashman, RF; Illera, VA; Peckham, D; Perandones, CE; Stunz, LL, 1993
)
0.29
" While there was a clear effect of dBcAMP-induced differentiation on the maximal NE-induced PI-response, no effect on the dose-response relationship was detectable, resulting in similar EC50-values for astrocytes cultured either in the absence or presence of dBcAMP."( Dibutyryl cyclic AMP-induced morphological differentiation of rat brain astrocytes increases alpha 1-adrenoceptor induced phosphoinositide breakdown by a mechanism involving protein synthesis.
Fahrig, T; Sommermeyer, H, 1993
)
0.29
" The resulting dose-response curves allowed for the determination of the effective concentration for half-maximal pigment dispersion (EC50) or half-maximal inhibition of bombesin-stimulated pigment dispersion (IC50) for the peptides."( Pigment dispersion in frog melanophores can be induced by a phorbol ester or stimulation of a recombinant receptor that activates phospholipase C.
Graminski, GF; Jayawickreme, CK; Lerner, MR; Potenza, MN, 1993
)
0.29
" The effects of PDE were dose dependent over the range of 10-70% (v/v) and simply augmented and reduced the dose-response curve to fMLP and PMA, respectively."( Effect of peritoneal dialysis effluent on superoxide anion production by polymorphonuclear neutrophils.
Daniels, I; Fletcher, J; Haynes, AP; Lindsay, M; Morgan, AG; Porter, C, 1993
)
0.29
" DFMO has shown a dose-response effect in tumor inhibition in mice."( Randomized phase I chemoprevention dose-seeking study of alpha-difluoromethylornithine.
Carbone, PP; Carey, P; Gilmore, D; Love, RR; Pomplun, M; Tutsch, KD; Verma, AK; Wilding, G, 1993
)
0.29
" In acini prepared from the camostate-treated rats, responsiveness to both CCK-8 and carbamylcholine was greatly decreased with no shift in the dose-response curves compared to control acini prepared from saline-treated rats."( Chronic oral administration of synthetic trypsin inhibitor camostate reduces amylase release from isolated rat pancreatic acini.
Fujii, M; Nakamura, T; Okabayashi, Y; Otsuki, M; Tani, S, 1995
)
0.29
" In addition, treatment of FLC with staurosporine prevented the induction of IFN-stimulated genes and the establishment of the antiviral state only when this drug was used at high dosage (500 nM)."( Staurosporine inhibits interferon alpha-induced gene expression in Friend erythroleukemia cells through a PKC independent pathway.
Affabris, E; Fiorucci, G; Mangino, G; Marcolin, C; Percario, ZA; Romeo, G,
)
0.13
" Male Fischer 344 rats were dosed intratracheally with silica (2."( Characteristics of the acute-phase pulmonary response to silica in rats.
Antonini, JM; DiMatteo, M; Reasor, MJ; Van Dyke, K, 1996
)
0.29
" Thus, both binding and activation dose-response curves for SAPD were double sigmoidal, which was also observed for dose-dependent activation by the commonly used phorbol ester, 4beta-12-O-tetradecanoylphorbol-13-acetate (TPA)."( Protein kinase Calpha contains two activator binding sites that bind phorbol esters and diacylglycerols with opposite affinities.
Ho, C; Kelly, MB; Larkin, JD; Slater, SJ; Stubbs, CD; Taddeo, FJ; Yeager, MD, 1996
)
0.29
" The time course and dose-response relationships between mu receptor phosphorylation and agonist-induced desensitization display interesting parallels."( Differential mu opiate receptor phosphorylation and desensitization induced by agonists and phorbol esters.
Mackin, S; Uhl, GR; Wang, JB; Weight, FF; Yu, Y; Zhang, L, 1996
)
0.29
"The question was addressed whether the dose-response relationship derived from a carcinogenicity study can be used for mechanistic interpretation and to what extent the shape of the curve is dependent on the duration of the bioassay and the time of analysis."( Dose-time response in mouse skin tumor induction by 7, 12-dimethylbenz[a]anthracene and 12-O-tetradecanoyl-phorbol-13-acetate.
Beland, PE; Candrian, R; Fekete, T; Fischer, WH; Lutz, WK, 1996
)
0.29
" Northern blots revealed concomitant increases in PGHS-2 mRNA levels that peaked at 2 h and were dependent on the dosage of IL-1 beta."( Interleukin-1 beta induces prostaglandin G/H synthase-2 (cyclooxygenase-2) in primary murine astrocyte cultures.
Chang, JW; Coleman, PD; Kaplan, MD; Miller, JC; O'Banion, MK, 1996
)
0.29
" Dose-response experiments indicated an initial effect with 5 ng/ml PRL and a maximum effect with 500 ng/ml PRL."( Characteristics of the prolactin stimulation of c-fos mRNA levels in mouse mammary gland explants.
Rillema, JA; Rowady, DL, 1996
)
0.29
" The relative potencies of SP-related peptides to stimulate pepsinogen secretion and [Ca2+]i demonstrated a close agreement with their abilities to inhibit the binding of 125I-BH-SP, and comparison of the dose-response curves suggests occupation of the low affinity sites mediate changes in biologic activity."( Gastric chief cells possess NK1 receptors which mediate pepsinogen secretion and are regulated by agents that increase cAMP and phospholipase C.
Jensen, RT; Kitsukawa, Y; Pradhan, TK; Turner, RJ, 1996
)
0.29
" Our approach was to mutate either the first, the second, or both zinc fingers of PKCdelta, to express the mutated enzyme in NIH 3T3 cells, and to monitor the effect of the mutations on the dose-response curve for translocation induced by phorbol 12-myristate 13-acetate."( Non-equivalent roles for the first and second zinc fingers of protein kinase Cdelta. Effect of their mutation on phorbol ester-induced translocation in NIH 3T3 cells.
Acs, P; Biro, T; Blumberg, PM; Bogi, K; Gohari, S; Szallasi, Z, 1996
)
0.29
" While fMLP exerted similar effects in both populations, dose-response curves for SP1 NKA and the NK2 receptor agonist were shifted leftwards (1, 4 and 3 orders of magnitude, respectively) in sensitized AMs."( Modulation by protein kinase C of the enhanced responsiveness to tachykinins in ovalbumin-sensitized guinea pig alveolar macrophages.
Brunelleschi, S; Fantozzi, R; Guidotto, S; Tonso, E; Viano, I, 1996
)
0.29
"3 microM) produced an approximately parallel shift to the right in the dose-response curve to NA."( Inhibitory effect of noradrenaline uptake inhibitors on contractions of rat aortic smooth muscle.
Huang, Y, 1996
)
0.29
" The dose-response curve shows increased mRNA levels starting at 10 ng/ml of TPA and reaching a maximum by 50 ng/ml TPA (10-fold stimulation over control)."( Identification by differential display of a mRNA specifically induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in T84 human colon carcinoma cells.
Cafferata, EG; Gonzalez-Guerrico, AM; Pivetta, OH; Santa-Coloma, TA, 1996
)
0.29
" Preexposure of the cells to GLP-1 induced a decrease in GLP-1-mediated cAMP production, as assessed by a 3- to 5-fold rightward shift of the dose-response curve and an approximately 20 percent decrease in the maximal production of cAMP."( Desensitization and phosphorylation of the glucagon-like peptide-1 (GLP-1) receptor by GLP-1 and 4-phorbol 12-myristate 13-acetate.
Dolci, W; Thorens, B; Widmann, C, 1996
)
0.29
" Phorbol 12-myristate 13-acetate (PMA)-stimulated and net H2O2 productions for a minor subpopulation of peritoneal cells showed positive dose-response correlations by linear regression analysis."( Differential modulation of natural and adaptive immunity in Fischer rats exposed for 6 weeks to 60 Hz linear sinusoidal continuous-wave magnetic fields.
Gagnon, J; Houde, M; Mandeville, R; Mercier, G; Tremblay, L, 1996
)
0.29
" Among unfractionated peripheral blood mononuclear cells (PBMC), the major producers of detectable IL-4 in primary in vitro cultures were found to be basophils based on: (i) an allergen dose-response corresponding closely to that required for basophil histamine release and lower than that required for T cell activation; (ii) a rapid time course for IL-4 production (detectable at 3 h), inconsistent with the typical activation requirements of fresh T cells; (iii) the production of comparable levels of IL-4 in cultures stimulated with allergen or anti-IgE; and (iv) the complete loss of detectable IL-4 production following specific depletion of basophils from PBMC."( IL-4 production by allergen-stimulated primary cultures: identification of basophils as the major IL-4-producing cell type.
Clay, MJ; Garman, RD; Happ, MP; Hirani, S; Kasaian, MT; Luqman, M, 1996
)
0.29
" Examination of the Ang II dose-response relation revealed detectable JNK activation at 10(-9) mol/L and maximal activation at 10(-6) mol/L."( Angiotensin II stimulates c-Jun NH2-terminal kinase in cultured cardiac myocytes of neonatal rats.
Komuro, I; Kudoh, S; Mizuno, T; Shiojima, I; Takekoshi, N; Yamazaki, T; Yazaki, Y; Zou, Y, 1997
)
0.3
" However, since the optimal dose, the dosing interval, and the mechanisms of action are not well-defined, we studied the effects on CGD neutrophil (PMN) functions ex vivo of interferon-gamma (IFN-gamma)."( Dose-dependent enhancements by interferon-gamma on functional responses of neutrophils from chronic granulomatous disease patients.
Ahlin, A; Elinder, G; Palmblad, J, 1997
)
0.3
"Tilapia were dosed by intraperitoneal injection for 5 consecutive days with either 20 or 40 mg/kg of the environmental contaminant hexachlorocyclohexane (lindane)."( Exposure of tilapian fish to the pesticide lindane results in hypocellularity of the primary hematopoietic organ (pronephros) and the spleen without altering activity of phagocytic cells in these organs.
Hart, LJ; Holladay, SD; Robertson, J; Smith, BJ; Smith, SA, 1997
)
0.3
" For these patients orally administered pentoxifylline failed to decrease reactive oxygen species generation by spermatozoa, and had no effect on sperm motility, sperm motion parameters and sperm fertilizing ability at low dosage (300 mg."( Formation of reactive oxygen species by spermatozoa from asthenospermic patients: response to treatment with pentoxifylline.
Arakawa, S; Fujisawa, M; Kamidono, S; Kanzaki, M; Okada, H; Tatsumi, N, 1997
)
0.3
" Orally administered pentoxifylline had no effect at low dosage but it increased sperm motility and some sperm motion parameters without altering sperm fertilizing ability at high dosage."( Formation of reactive oxygen species by spermatozoa from asthenospermic patients: response to treatment with pentoxifylline.
Arakawa, S; Fujisawa, M; Kamidono, S; Kanzaki, M; Okada, H; Tatsumi, N, 1997
)
0.3
" Differential sensitivity to IgM receptor ligation is reproduced by multivalent nominal antigen, in cell populations that show identical dose-response inhibition curves to direct activation of protein kinase C by phorbol esters."( Differential sensitivity of B lymphocyte populations to IgM receptor ligation is determined by local factors.
Andersson, J; Coutinho, A; Demengeot, J; Grandien, A; Modigliani, Y; Vasconcellos, R, 1997
)
0.3
" Dose-response curves for A23187 and PMA were derived for the three functions."( Functional characterization of equine neutrophils in response to calcium ionophore A23187 and phorbol myristate acetate ex vivo.
Chilcoat, C; Crisman, M; Eyre, P; Moore, T; Wilcke, J, 1997
)
0.3
" In addition, these magnetic fields did not enhance tumor promoter-induced transformation showing no increase in the maximum number of transformed colonies and no shift in the dose-response curve."( Power frequency magnetic fields do not contribute to transformation of JB6 cells.
Chen, G; Colburn, NH; Saffer, JD; Thurston, SJ, 1997
)
0.3
" Co-incubating 0-10 nmol/l T3 with 100 nmol/l insulin resulted in a downward shift in the dose-response curve without a change in the half-maximal response to T3."( Modulation of T3-induced sex hormone-binding globulin secretion by human hepatoblastoma cells.
Barlow, JW; Lim, CF; Loidl, NM; Payne, KL; Stockigt, JR; Topliss, DJ, 1997
)
0.3
"Bryostatin 1 (Bryo) has been shown to induce biphasic dose-response curves for down-regulating protein kinase Cdelta (PKCdelta) as well as for protecting PKCdelta from down-regulation induced by phorbol 12-myristate 13-acetate (PMA)."( The catalytic domain of protein kinase Cdelta confers protection from down-regulation induced by bryostatin 1.
Acs, P; Blumberg, PM; Bögi, K; Lorenzo, PS; Pettit, GR, 1997
)
0.3
" After NMDA treatment, the DPDPE dose-response curve shifted to the right (EC50 value increased approximately 7-fold, from 6 to 40 nM), and the maximal response induced by DPDPE was reduced by approximately 60%."( N-Methyl-D-aspartate attenuates opioid receptor-mediated G protein activation and this process involves protein kinase C.
Fan, GH; Jing, Q; Lou, LG; Ma, L; Pei, G; Wu, YL; Zhang, Z; Zhao, J, 1998
)
0.3
" Short-term (3 min) pretreatment with the PKC activator 12-O-tetradecanoylphorbol 13-acetate (TPA) evoked a rightward shift of the dose-response curve for the Ca2+ mobilizing effect of CCK-8-S in both cell lines."( Protein kinase C-mediated inhibition of transmembrane signalling through CCK(A) and CCK(B) receptors.
De Pont, JJ; Fouraux, MA; Smeets, RL; van Emst-de Vries, SE; Willems, PH, 1998
)
0.3
" Additional studies with TPA after the determination of optimum dosing regimens are needed to determine whether long-lasting or permanent remissions of myelocytic leukemia can be achieved."( Effect of intravenous infusions of 12-O-tetradecanoylphorbol-13-acetate (TPA) in patients with myelocytic leukemia: preliminary studies on therapeutic efficacy and toxicity.
Cao, GS; Chang, RL; Conney, AH; Han, ZT; Liu, XJ; Newmark, HL; Sun, JZ; Tian, GF; Yang, RY; Zhu, XX, 1998
)
0.3
" Dose-response studies with PMA also indicated that the increased JNK activity was tightly correlated with elevated u-PAR protein levels."( Stimulation of urokinase-type plasminogen activator receptor expression by PMA requires JNK1-dependent and -independent signaling modules.
Allgayer, H; Boyd, D; Gum, R; Juarez, J; Mazar, A; Wang, Y, 1998
)
0.3
" The dose-response curves for CCK-8-induced cyclic AMP accumulation and inositol 1,4,5-trisphosphate (Ins(1,4,5)P3) formation were shifted to the left in CHO-CCK(A)MT cells."( Mutational analysis of the potential phosphorylation sites for protein kinase C on the CCK(A) receptor.
De Pont, JJ; Fouraux, MA; Pouwels, W; Ronken, E; Smeets, RL; van Emst-de Vries, SE; Willems, PH, 1998
)
0.3
" Papules were first detected in DMBA-initiated mice 21 days after the start of dosing with TPA."( Squamous cell hyperplastic foci: precursors of cutaneous papillomas induced in SENCAR mice by a two-stage carcinogenesis regimen.
Binder, RL; Conti, CJ; Gallagher, PM; Johnson, GR; Stockman, SL; Sundberg, JP, 1998
)
0.3
" However, a higher gene dosage of the transgenic Bcl-2 was required for protection against Dex, compared to the PMA and/or ionomycin-induced apoptosis."( Biochemical and kinetic characterization of the glucocorticoid-induced apoptosis of immature CD4+CD8+ thymocytes.
Ivanov, VN; Nikolić-Zugić, J, 1998
)
0.3
" Measurement of intracellular cAMP levels revealed that in the case of PTH and AVP, the dose-response curve for the increase in cAMP virtually matched that for transcellular Ca2+ transport."( Hormone-stimulated Ca2+ reabsorption in rabbit kidney cortical collecting system is cAMP-independent and involves a phorbol ester-insensitive PKC isotype.
Bindels, RJ; De Pont, JJ; Hoenderop, JG; Willems, PH, 1999
)
0.3
" If IB4 administration was delayed for 3 h post injection of PMA and bronchoalveolar lavage performed 3 h later, the extents of PMN accumulation and edema formation were similar to those observed 3 h following PMA challenge in control animals not dosed with IB4."( The effects of IB4, a monoclonal antibody to the CD18 leukocyte integrin on phorbol myristate acetate (PMA)-induced polymorphonuclear leukocyte (PMN) accumulation and endothelial injury in rabbit lungs.
Forrest, MJ; MacIntyre, DE; Meurer, RD, 1999
)
0.3
" Comparison of the dose-response curves between TPA-induced hydrogen (H+) secretion, as measured by aminopyrine (AP) uptake, and the membrane-associated PKC-alpha suggests that translocation of PKC-alpha is not involved in the H+ secretory process in PC."( Expression and characterization of protein kinase C in isolated rabbit parietal cells.
Kim, SW; Levine, RA; Loo, A; Nandi, J, 1999
)
0.3
" Experimentation utilized three different doses of TPA within its dose-response range (0."( Lack of effect of a 60 Hz magnetic field on biomarkers of tumor promotion in the skin of SENCAR mice.
Anderson, LE; DiGiovanni, J; Johnston, DA; Kavet, R; Miller, DL; Morris, JE; Rupp, T; Sasser, LB; Walborg, EF, 1999
)
0.3
" Thrombin-stimulated platelets contained not only the three major proteins: actin (43 kDa), myosin (200 kDa) and an actin-binding protein (250 kDa), but three additional proteins of Mr56 kDa, 80 kDa and 85 kDa in the cytoskeleton, which were induced in by thrombin dose-response relationship."( Cytoskeletal changes in platelets induced by thrombin and phorbol myristate acetate (PMA).
Chen, R; Liang, N, 1998
)
0.3
" TNF-alpha(-/-) mice were resistant to development of benign and malignant skin tumors, whether induced by initiation with DMBA and promotion with TPA or by repeated dosing with DMBA."( Mice deficient in tumor necrosis factor-alpha are resistant to skin carcinogenesis.
Arnott, C; Balkwill, F; Burke, F; East, N; Holdsworth, H; Kollias, G; Moore, RJ; Owens, DM; Pasparakis, M; Rollins, B; Stamp, G; Turner, L, 1999
)
0.3
" In summary, we could not show beneficial effects of L-carnitine administration in hemodialysis patients for the dosage and duration of treatment stated, either on phagocytic function and viability or on the clinical and biochemical parameters observed."( Effects of L-carnitine on leukocyte function and viability in hemodialysis patients: A double-blind randomized trial.
Fischer, FP; Kuhlmann, U; Mettang, T; Pauli-Magnus, C; Thomas, S; Weber, J, 1999
)
0.3
" Western blotting confirmed that VT (50 to 1000 ng/ml) also significantly diminished GRP/BiP protein levels in a dose-response manner in PMA/ION-stimulated cells."( Down-regulation of the endoplasmic reticulum chaperone GRP78/BiP by vomitoxin (Deoxynivalenol).
Li, S; Pestka, JJ; Yang, GH, 2000
)
0.31
" Time-course and dose-response studies showed a maximal approx."( Biogenesis of endoplasmic reticulum proteins involved in Ca2+ signalling during megakaryocytic differentiation: an in vitro study.
Bredoux, R; Corvazier, E; Enouf, J; Lacabaratz-Porret, C; Launay, S; Papp, B, 2000
)
0.31
"1 mM)-stimulated AP accumulation, which was dose-dependently inhibited by higher concentrations of TPA with corresponding shifts in the dose-response curve for carbachol-stimulated AP accumulation."( Effects of phorbol ester treatment on dibutyryl cyclic adenosine-5' monophosphate- and carbachol-stimulated aminopyrine accumulation in isolated rat parietal cells.
Kopp, R; Pfeiffer, A, 2000
)
0.31
" In the presence of tetrodotoxin, NMDA produced a bell-shaped dose-response curve with stimulation of phospho-ERK2 at 10, 25, and 50 microm NMDA and reduced stimulation at 100 microm NMDA."( N-methyl D-aspartate receptor-mediated bidirectional control of extracellular signal-regulated kinase activity in cortical neuronal cultures.
Chandler, LJ; Dorairaj, NR; Norwood, D; Sutton, G, 2001
)
0.31
" MT, like PMA, evoked a leftward shift of the dose-response curve for the STZ-induced [Ca(2)+](i) rise, indicating PKC-dependent sensitization of neutrophils for stimulation by STZ."( Nutritional lipid emulsions modulate cellular signaling and activation of human neutrophils.
Naber, T; van Emst-De Vries, S; Wanten, G; Willems, P, 2001
)
0.31
" In addition, prolonged treatment of cells with PMA suppressed the expression of the myogenic differentiation marker desmin showing similar dose-response characteristics."( Phorbol ester treatment inhibits proliferation and differentiation of cultured human skeletal muscle satellite cells by differentially acting on protein kinase C isoforms.
Adány, R; Bárdos, H; Bíró, T; Boczán, J; Czifra, G; Kovács, L; Lázár, J; Mechler, F; Papp, H, 2001
)
0.31
" IgE levels were inhibited in a B cell dose-response curve, whereas IgM and IgG1 were induced by Bryo treatment."( Bryostatin-1 specifically inhibits in vitro IgE synthesis.
Conrad, DH; Grant, S; Ma, C; Rabah, D, 2001
)
0.31
"5 micromol/L PMA (t(1/2)); (2) Dose-response curve in response to PMA (0."( [The increased reactivity of isolated pulmonary artery rings from rats with hypoxia-induced pulmonary hypertension to activator of protein kinase C].
Liu, Y; Ni, W; Xu, Y; Zhang, Z, 1999
)
0.3
"1 mM neomycin neither shifted the dose-response curve of the peak I(ACh) to the right (dissociation constant (K(d)) = 16."( Decrease in acetylcholine-induced current by neomycin in PC12 cells.
Cheng, XH; Liu, LA; Shi, LJ; Wang, CA, 2002
)
0.31
" A requirement for PKC betaII for phagocytosis was demonstrated collectively by phorbol 12-myristate 13-acetate-induced depletion of PKC betaII, by dose-response to PKC inhibitor Ro-32-0432, and by use of PKC betaII myristoylated peptide as a blocker."( Activation of protein kinase C beta II by the stereo-specific phosphatidylserine receptor is required for phagocytosis of apoptotic thymocytes by resident murine tissue macrophages.
Curtis, JL; Hu, B; Polak, T; Punturieri, A; Sonstein, J; Todt, JC, 2002
)
0.31
" The CCK dose-response curve for TyrP for sites in each kinase was similar."( Phosphospecific site tyrosine phosphorylation of p125FAK and proline-rich kinase 2 is differentially regulated by cholecystokinin receptor type A activation in pancreatic acini.
Bragado, MJ; García-Marin, LJ; Jensen, RT; Pace, A; Tapia, JA, 2003
)
0.32
" The cells show a clear dose-response relationship concerning the formation of ROS with regard to the mass of particles applied."( Formation of reactive oxygen species in rat epithelial cells upon stimulation with fly ash.
Diabaté, S; Krug, HF; Voelkel, K, 2003
)
0.32
" Our data suggested that PMA stimulated the production of superoxide anion in a dose-response manner, as compared with A23187, which did not induce a significant release of superoxide anion in PMNs-RA."( Phospholipase A2 modulates respiratory burst developed by neutrophils in patients with rheumatoid arthritis.
Bostan, M; Brasoveanu, LI; Constantin, MC; Galatiuc, C; Hirt, M; Iordachescu, D,
)
0.13
" Evidence of systemic toxicity was observed in animals dosed chronically with pyrimethamine or amiloride, but no skin papillomas were observed in mice treated with amiloride, dipyridamole, or pyrimethamine for 26 weeks."( Evaluation of the Tg.AC assay: specificity testing with three noncarcinogenic pharmaceuticals that induce selected stress gene promoters in vitro and the inhibitory effects of solvent components.
Lin, KK; Rosenzweig, BA; Sistare, FD; Thompson, KL; Weaver, JL; Zhang, J, 2003
)
0.32
" Dose-response inhibitor potency was established for sigmoidin A (IC (50) = 31 microM)."( Anti-inflammatory activities of two flavanones, sigmoidin A and sigmoidin B, from Erythrina sigmoidea.
Fomum, ZT; Giner, RM; Kamanyi, A; Máñez, S; Mbafor, JT; Mbanya, JC; Njamen, D; Recio, MC; Ríos, JL, 2004
)
0.32
" This synergy may explain, at least in part, the steep dose-response relationship observed for CCh-induced TRPC6 currents expressed in HEK cells."( Activation of human TRPC6 channels by receptor stimulation.
Bahra, P; Estacion, M; Gosling, M; Li, S; Poll, C; Schilling, WP; Sinkins, WG; Westwick, J, 2004
)
0.32
" I3A induced a higher level of secretion of the inflammatory cytokine interleukin 6 compared with PMA in the WEHI-231 cells and displayed a marked biphasic dose-response curve for the induction."( Characterization of the interaction of ingenol 3-angelate with protein kinase C.
Blumberg, PM; Garfield, SH; Kedei, N; Lundberg, DJ; Toth, A; Welburn, P, 2004
)
0.32
" Because these two waves of activation differ in time course, dose-response curve, requirement for GRPr CTD, and sensitivity to inhibitors, they result from different signaling pathways."( Alterations in receptor expression or agonist concentration change the pathways gastrin-releasing peptide receptor uses to regulate extracellular signal-regulated kinase.
Chen, PW; Kroog, GS, 2004
)
0.32
" Differential effectiveness between the isoforms was demonstrated in dose-response studies, as was differential binding to ILT2 and ILT4 in receptor-blocking studies."( Recombinant HLA-G5 and -G6 drive U937 myelomonocytic cell production of TGF-beta1.
Colonna, M; Hunt, JS; McIntire, RH; Morales, PJ; Petroff, MG, 2004
)
0.32
" All of these molecular and cellular alterations also occurred to a lesser extent in Smad3(+/-) mice as compared with Smad3(+/+) mice, suggesting a Smad3 gene dosage effect."( Smad3 knockout mice exhibit a resistance to skin chemical carcinogenesis.
Deng, C; Li, AG; Lu, SL; Wang, XJ; Zhang, MX, 2004
)
0.32
" Transfer of 3, 5, 10, or 23 million pure in vitro-activated T-cells accelerated diabetes onset in >90% of the recipients, with the degree of acceleration being dosage dependent."( In vivo control of diabetogenic T-cells by regulatory CD4+CD25+ T-cells expressing Foxp3.
Holm, TL; Hornum, L; Lundsgaard, D; Markholst, H, 2005
)
0.33
" The cumulative dose-response curve of SMA to NE and Ca2+ after shock was shifted to the right."( The role of calcium desensitization in vascular hyporeactivity and its regulation after hemorrhagic shock in the rat.
Liu, L; Xu, J, 2005
)
0.33
" The animals were dosed per gavage with the test substance on study days 0, 14, 28, and 42."( Effects of crude oil and diesel exposures on biochemical activities of polymorphonuclear leukocytes in cattle.
Coppock, RW; Dziwenka, M; Embury, C; Hiltz, MN; Khan, AA; Schuler, MM, 2005
)
0.33
" The 1,3,5-triazines tested inhibited the adhesion evoked by pro-inflammatory stimuli, such as platelet activating factor (PAF), FMLP, phorbol myristate acetate (PMA), tumour necrosis factor-alpha (TNF-alpha) and interleukin-1beta(IL-1beta) in a dose-response manner over the concentration range 10(-9) to 10(-4)M, compounds 5 and 6 being the most active."( Evaluation of in-vitro anti-inflammatory activity of some 2-alkyl-4,6-dimethoxy-1,3,5-triazines.
Collino, M; Dianzani, C; Fantozzi, R; Gallicchio, M; Menicagli, R; Samaritani, S; Signore, G, 2006
)
0.33
" Furthermore, particular cytokine levels were significantly decreased 2 h after drug dosing, compared with cytokine levels before dosing in mitogen-stimulated whole blood."( Cytokine analysis to predict immunosuppression.
Barten, MJ; Bocsi, J; Boldt, A; Dhein, S; Garbade, J; Gummert, JF; Mohr, FW; Rahmel, A, 2006
)
0.33
" Phorbol 12-myristate 13-acetate (PMA) attenuated the receptor-mediated lipolysis by causing a shift of the dose-response curve to the higher concentrations of norepinephrine and isoproterenol."( Protein kinase C attenuates beta-adrenergic receptor-mediated lipolysis, probably through inhibition of the beta1-adrenergic receptor system.
Nakamura, J, 2006
)
0.33
" The level of protein decreased around 50% after treatment for 3-5 days using the dosage of PMA effective against the mRNA expression."( Protein kinase Cbeta isoform down-regulates the expression of MDR3 P-glycoprotein in human Chang liver cells.
Hayashi, H; Kondo, T; Suzuki, S; Takagi, K; Ueyama, J; Wakusawa, S, 2006
)
0.33
" Furthermore, upregulation of three candidate genes (NFIL3, SKIL, and JMJD3) was shown to be dosage and time dependent with TPA treatment and was found to be directly regulated by TPA through PKC-dependent signaling."( An efficient strategy to identify early TPA-responsive genes during differentiation of HL-60 cells.
Hu, LY; Lin, WC; Lo, SH; Tepper, CG, 2006
)
0.33
" Dosage effects of immunosuppressive drugs (tacrolimus, cyclosporin A, sirolimus, mycophenolic acid, and methylprednisolone) were evaluated in vitro and the assay was applied successfully to dialysis, renal transplant, and liver transplant patients."( Validation of immunological biomarkers for the pharmacodynamic monitoring of immunosuppressive drugs in humans.
Böhler, T; Budde, K; Glander, P; Gurragchaa, P; Kamar, N; Klupp, J; Neumayer, HH; Nolting, J; Reisener, K, 2007
)
0.34
" dose-response and progress curves, determined by numerical integration of the LE models constituting the superposition."( Chemiluminescent picture of diphenyleneiodonium-inhibited NADPH oxidase: a bimodal process and its logistic-exponential model-based description.
Arnhold, J; Kochel, B; Vocks, A,
)
0.13
" This is the first systematic dose-response evaluation of soluble stimulants of neutrophil respiratory burst in rats."( Flow-cytometric measurement of respiratory burst in rat polymorphonuclear granulocytes: Comparison of four cell preparation procedures, and concentration-response evaluation of soluble stimulants.
Bitzinger, DI; Dittmar, MS; Lindner, R; Schlachetzki, F; Trabold, B, 2008
)
0.35
" Upregulation of TNFR1 expression by priming with TAPI-2 and IFNgamma resulted in enhanced ICAM-1 expression in response to TNFalpha stimulation (significant change in the slope of the dose-response curve)."( Regulation of the receptor for TNFalpha, TNFR1, in human conjunctival epithelial cells.
Barney, NP; Cook, EB; Graziano, FM; Stahl, JL, 2008
)
0.35
"For normal sperm with normal sperm-ZP binding, both PMA and dbcAMP significantly enhanced sperm-ZP binding in a dose-response manner."( Enhancement of sperm-zona pellucida (ZP) binding capacity by activation of protein kinase A and C pathways in certain infertile men with defective sperm-ZP binding.
Baker, HW; Liu, DY; Liu, ML, 2009
)
0.35
" For OB assays, dose-response curves were performed for each activator."( Oxidative burst assessment and neutrophil-platelet complexes in unlysed whole blood.
Avendaño, A; Marin, L; Marin, P; Petriz, J; Sales-Pardo, I, 2008
)
0.35
" Maximal TPA activation of protein kinase C (PKCalpha) as measured by activity assays and activation of target genes and induction of cornified envelopes correlated with TGFbeta1 gene dosage in keratinocytes and addition of exogenous TGFbeta1 restored the cornification defect in TGFbeta1+/- keratinocytes."( Transforming growth factor beta1 enhances tumor promotion in mouse skin carcinogenesis.
Glick, AB; Hogan, KA; Markell, LM; Pérez-Lorenzo, R; Yuspa, SH, 2010
)
0.36
"Three different methods--hair plucking or treatment with retinoic acid (RA) or O-tetradecanoylphorbol-13-acetate (TPA)--were used to induce mice hair follicles into the anagen stage before they were dosed with a β-galactosidase-encoding plasmid, and the specific antibody responses induced were evaluated."( The extent of the uptake of plasmid into the skin determines the immune responses induced by a DNA vaccine applied topically onto the skin.
Chung, WG; Cui, Z; Li, X; Löhr, CV; Rodriguez, BL; Sloat, BR; Weiss, R; Yu, Z, 2011
)
0.37
" Thus, we propose that RasGRP1 upregulates signaling from Ras and contributes to epidermal tumorigenesis by increasing the total dosage of active Ras."( Targeted deletion of RasGRP1 impairs skin tumorigenesis.
Cline, JM; Endo, Y; Fonseca, LL; Ji, J; Lorenzo, PS; Rajani, C; Ramos, JW; Sharma, A; Stone, JC; Yanagida, JK, 2014
)
0.4
" Dose-response studies acknowledging the process of multistage tumorigenesis are important; however, data pertaining nonlinearity are not yet available."( Does increase in DNA repair allow "tolerance-to-insult" in chemical carcinogenesis? Skin tumor experiments with MGMT-overexpressing mice.
Becker, K; Kaina, B; Thomas, AD, 2014
)
0.4
"The effective dose (ED) is the pharmaceutical dosage required to produce a therapeutic response in a fixed proportion of the patients."( A random set approach to confidence regions with applications to the effective dose with combinations of agents.
Jankowski, H; Ji, X; Stanberry, L, 2014
)
0.4
" It had also efficient effect on healing process and duration of wound healing with a dose-response by oral administration and a maximal effect observed from the lowest to the highest dose by topical application."( Oral and Topical Administration of ROQUETTE Schizochytrium sp. Alleviate Skin Inflammation and Improve Wound Healing in Mice.
Baert, B; Bisson, JF; Guerin-Deremaux, L; Hidalgo-Lucas, S; Rozan, P; Saniez-Degrave, MH; Violle, N, 2015
)
0.42
" Based on the parameterization of a TPA dose-response curve, the transcriptional response of MDCK cells to Jatropha oil exposure was expressed in term of TPA toxic equivalent (TEQ), a convenient metric to report the inflammatory potential of complex mixtures."( Development of a sensitive in vitro assay to quantify the biological activity of pro-inflammatory phorbol esters in Jatropha oil.
Hawari, J; Padhi, BK; Pelletier, G; Poon, R; Sunahara, GI, 2015
)
0.42
"This study evidenced that TQF, particularly at its lower dosage (10 mg/kg), ameliorated DMBA/TPA-induced mouse skin tumorigenesis."( Low dose triterpene-quinone fraction from Ardisia crispa root precludes chemical-induced mouse skin tumor promotion.
Abdul Hamid, R; Khaza'ai, H; Mohtarrudin, N; Saiful Yazan, L; Yeong, LT, 2015
)
0.42
" This study used flow cytometry and quantitative reverse transcription-polymerase chain reaction (qRT-PCR) to evaluate the effects of high-dose oral cyclosporine across a 12-h dosing interval."( Effects of oral cyclosporine on canine T-cell expression of IL-2 and IFN-gamma across a 12-h dosing interval.
Archer, TM; Fellman, CL; Lunsford, KV; Mackin, AJ; Stokes, JV; Wills, RW, 2016
)
0.43
"In general, chronotherapy is desirable for a more effective and/or safe dosage regimen."( Chronotherapy of maxacalcitol on skin inflammation induced by topical 12-O-tetradecanoylphorbol-13-acetate in mice.
Ando, H; Fujimura, A; Kumazaki, M; Ushijima, K; Yoshioka, D, 2018
)
0.48
" Differentiation of cells by PMA induced midkine, TNF-α, IL-10 and IFN-γ secretions in monocytic cells even at the lowest dosage (10 ng/ml)."( [Investigation of cytokine and midkine responses of human THP-1 leukemia cells induced by phorbol-12-Myristate-13-Acetate (PMA) at different concentrations and times].
Biriken, D; Yazıhan, N; Yılmaz, Ş, 2018
)
0.48
"Single-cell protein therapeutics is expected to promote our in-depth understanding of how a specific protein with a therapeutic dosage treats the cell without population averaging."( Electrochemical Single-Cell Protein Therapeutics Using a Double-Barrel Nanopipette.
Chen, HY; Jiang, D; Shi, XM; Wang, B; Xu, JJ; Xu, YT; Yu, SY; Zhao, WW; Zhou, BY, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (7)

RoleDescription
protein kinase C agonistAn agonist that selectively binds to and activates a protein kinase C receptor
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
reactive oxygen species generatorAny entity used to generate reactive oxygen species.
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
mitogenA chemical substance that encourages a cell to commence cell division, triggering mitosis.
carcinogenic agentA role played by a chemical compound which is known to induce a process of carcinogenesis by corrupting normal cellular pathways, leading to the acquistion of tumoral capabilities.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
phorbol esterEsters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.
acetate esterAny carboxylic ester where the carboxylic acid component is acetic acid.
tetradecanoate esterA fatty acid ester obtained by condensation of the carboxy group of tetradecanoic acid (also known as myristic acid) with a hydroxy group of an alcohol or phenol.
diesterA diester is a compound containing two ester groups.
tertiary alpha-hydroxy ketoneAn alpha-hydroxy ketone in which the carbonyl group and the hydroxy group are linked by a carbon bearing two organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (3)

PathwayProteinsCompounds
Regucalcin in proximal tubule epithelial kidney cells2415
Integrated breast cancer pathway9818
Non-genomic actions of 1,25 dihydroxyvitamin D364

Protein Targets (55)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.89130.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency63.09570.004023.8416100.0000AID485290
Microtubule-associated protein tauHomo sapiens (human)Potency19.95260.180013.557439.8107AID1460
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency10.00000.016525.307841.3999AID602332
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency10.00000.00798.23321,122.0200AID2551
DNA polymerase kappa isoform 1Homo sapiens (human)Potency39.81070.031622.3146100.0000AID588579
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID1705
Chain A, Ferritin light chainEquus caballus (horse)Potency19.95265.623417.292931.6228AID2323
Chain A, CruzipainTrypanosoma cruziPotency10.00000.002014.677939.8107AID1476
endonuclease IVEscherichia coliPotency35.48130.707912.432431.6228AID1708
dopamine D1 receptorHomo sapiens (human)Potency0.23110.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency17.45350.100020.879379.4328AID488773; AID588453; AID588456
ATAD5 protein, partialHomo sapiens (human)Potency0.00440.004110.890331.5287AID493106; AID493107
Fumarate hydrataseHomo sapiens (human)Potency35.48130.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency35.48130.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency1.99530.35487.935539.8107AID624146
regulator of G-protein signaling 4Homo sapiens (human)Potency15.00300.531815.435837.6858AID504845
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency0.00680.001530.607315,848.9004AID1224819; AID1224820; AID1224821; AID1224823
polyproteinZika virusPotency35.48130.00308.794948.0869AID1347053
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.14900.035520.977089.1251AID504332
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency36.89770.016525.307841.3999AID602332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency19.95260.540617.639296.1227AID2364; AID2528
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.04790.01262.451825.0177AID485313
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency42.561523.934123.934123.9341AID1967
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency0.13460.134610.395030.1313AID1347049
chromobox protein homolog 1Homo sapiens (human)Potency1.19170.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.11220.01789.637444.6684AID588834
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency0.00660.00669.809418.4927AID1347050
ras-related protein Rab-9AHomo sapiens (human)Potency63.09570.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency23.99110.00378.618923.2809AID2660; AID2666; AID2667; AID2668
eyes absent homolog 2 isoform aHomo sapiens (human)Potency100.00001.199814.641950.1187AID488837
DNA polymerase eta isoform 1Homo sapiens (human)Potency44.66840.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency50.11870.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency0.09270.15855.287912.5893AID493164
plasminogen precursorMus musculus (house mouse)Potency0.09270.15855.287912.5893AID493164
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency0.09270.15855.287912.5893AID493164
gemininHomo sapiens (human)Potency4.77030.004611.374133.4983AID463097; AID493164
DNA polymerase kappa isoform 1Homo sapiens (human)Potency26.67950.031622.3146100.0000AID588579
M-phase phosphoprotein 8Homo sapiens (human)Potency0.70790.177824.735279.4328AID488949
lamin isoform A-delta10Homo sapiens (human)Potency17.74960.891312.067628.1838AID1459; AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency6.30960.015812.3113615.5000AID1461
D(1A) dopamine receptorSus scrofa (pig)Potency23.28090.00378.108123.2809AID2667
Ataxin-2Homo sapiens (human)Potency2.23870.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.75690.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Protein kinase C gamma typeHomo sapiens (human)Ki0.00490.00120.42536.0000AID221771
Protein kinase C beta typeHomo sapiens (human)Ki0.00180.00040.69246.0000AID220908
Protein kinase C alpha typeHomo sapiens (human)Ki0.00440.00021.09456.9600AID218662; AID599010
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki0.00180.00000.667310.0000AID220908
Protein kinase C epsilon typeHomo sapiens (human)Ki0.00040.00040.97976.0000AID218937
Protein kinase C delta typeHomo sapiens (human)Ki0.00080.00030.94896.9600AID220518
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase D3Homo sapiens (human)EC50 (µMol)0.00950.00950.33070.9100AID1459482
Protein kinase C gamma typeHomo sapiens (human)EC50 (µMol)0.00950.00950.33070.9100AID1459482
Protein kinase C beta typeHomo sapiens (human)EC50 (µMol)0.00950.00950.33070.9100AID1459482
Luciferin 4-monooxygenasePhotinus pyralis (common eastern firefly)EC50 (µMol)0.01000.01000.01000.0100AID1535468
Protein kinase C alpha typeHomo sapiens (human)EC50 (µMol)850.00470.00950.33070.9100AID1459482; AID614623
Protein kinase C eta typeHomo sapiens (human)EC50 (µMol)0.00950.00950.33070.9100AID1459482
Protein kinase C iota typeHomo sapiens (human)EC50 (µMol)0.00950.00950.33070.9100AID1459482
Protein kinase C epsilon typeHomo sapiens (human)EC50 (µMol)2.78470.00952.94848.1900AID1459482; AID458316
Protein kinase C theta typeHomo sapiens (human)EC50 (µMol)1.59980.00952.77877.2500AID1459482; AID458317
Protein kinase C zeta typeHomo sapiens (human)EC50 (µMol)0.00950.00300.24880.9100AID1459482
Protein kinase C delta typeHomo sapiens (human)EC50 (µMol)1.82320.00410.92295.1700AID1459482; AID1505448; AID458315
Serine/threonine-protein kinase D1Homo sapiens (human)EC50 (µMol)0.00950.00950.33070.9100AID1459482
Ras guanyl-releasing protein 3Homo sapiens (human)EC50 (µMol)0.08200.08200.08200.0820AID1505443
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (250)

Processvia Protein(s)Taxonomy
protein phosphorylationSerine/threonine-protein kinase D3Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D3Homo sapiens (human)
sphingolipid biosynthetic processSerine/threonine-protein kinase D3Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase D3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D3Homo sapiens (human)
protein phosphorylationProtein kinase C gamma typeHomo sapiens (human)
chemical synaptic transmissionProtein kinase C gamma typeHomo sapiens (human)
learning or memoryProtein kinase C gamma typeHomo sapiens (human)
chemosensory behaviorProtein kinase C gamma typeHomo sapiens (human)
response to toxic substanceProtein kinase C gamma typeHomo sapiens (human)
phosphorylationProtein kinase C gamma typeHomo sapiens (human)
negative regulation of protein ubiquitinationProtein kinase C gamma typeHomo sapiens (human)
regulation of response to foodProtein kinase C gamma typeHomo sapiens (human)
positive regulation of mismatch repairProtein kinase C gamma typeHomo sapiens (human)
negative regulation of protein catabolic processProtein kinase C gamma typeHomo sapiens (human)
regulation of circadian rhythmProtein kinase C gamma typeHomo sapiens (human)
response to morphineProtein kinase C gamma typeHomo sapiens (human)
negative regulation of neuron apoptotic processProtein kinase C gamma typeHomo sapiens (human)
response to painProtein kinase C gamma typeHomo sapiens (human)
rhythmic processProtein kinase C gamma typeHomo sapiens (human)
regulation of phagocytosisProtein kinase C gamma typeHomo sapiens (human)
long-term synaptic potentiationProtein kinase C gamma typeHomo sapiens (human)
innervationProtein kinase C gamma typeHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionProtein kinase C gamma typeHomo sapiens (human)
negative regulation of proteasomal protein catabolic processProtein kinase C gamma typeHomo sapiens (human)
response to psychosocial stressProtein kinase C gamma typeHomo sapiens (human)
regulation of synaptic vesicle exocytosisProtein kinase C gamma typeHomo sapiens (human)
intracellular signal transductionProtein kinase C gamma typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C gamma typeHomo sapiens (human)
adaptive immune responseProtein kinase C beta typeHomo sapiens (human)
chromatin remodelingProtein kinase C beta typeHomo sapiens (human)
regulation of transcription by RNA polymerase IIProtein kinase C beta typeHomo sapiens (human)
protein phosphorylationProtein kinase C beta typeHomo sapiens (human)
calcium ion transportProtein kinase C beta typeHomo sapiens (human)
intracellular calcium ion homeostasisProtein kinase C beta typeHomo sapiens (human)
apoptotic processProtein kinase C beta typeHomo sapiens (human)
mitotic nuclear membrane disassemblyProtein kinase C beta typeHomo sapiens (human)
signal transductionProtein kinase C beta typeHomo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
response to xenobiotic stimulusProtein kinase C beta typeHomo sapiens (human)
response to glucoseProtein kinase C beta typeHomo sapiens (human)
regulation of glucose transmembrane transportProtein kinase C beta typeHomo sapiens (human)
negative regulation of glucose transmembrane transportProtein kinase C beta typeHomo sapiens (human)
regulation of dopamine secretionProtein kinase C beta typeHomo sapiens (human)
dibenzo-p-dioxin metabolic processProtein kinase C beta typeHomo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
positive regulation of insulin secretionProtein kinase C beta typeHomo sapiens (human)
response to vitamin DProtein kinase C beta typeHomo sapiens (human)
regulation of growthProtein kinase C beta typeHomo sapiens (human)
B cell activationProtein kinase C beta typeHomo sapiens (human)
positive regulation of odontogenesis of dentin-containing toothProtein kinase C beta typeHomo sapiens (human)
lipoprotein transportProtein kinase C beta typeHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionProtein kinase C beta typeHomo sapiens (human)
post-translational protein modificationProtein kinase C beta typeHomo sapiens (human)
response to ethanolProtein kinase C beta typeHomo sapiens (human)
positive regulation of angiogenesisProtein kinase C beta typeHomo sapiens (human)
positive regulation of DNA-templated transcriptionProtein kinase C beta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
B cell receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
positive regulation of B cell receptor signaling pathwayProtein kinase C beta typeHomo sapiens (human)
cellular response to carbohydrate stimulusProtein kinase C beta typeHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionProtein kinase C beta typeHomo sapiens (human)
regulation of synaptic vesicle exocytosisProtein kinase C beta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C beta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C beta typeHomo sapiens (human)
angiogenesisProtein kinase C alpha typeHomo sapiens (human)
positive regulation of endothelial cell proliferationProtein kinase C alpha typeHomo sapiens (human)
desmosome assemblyProtein kinase C alpha typeHomo sapiens (human)
chromatin remodelingProtein kinase C alpha typeHomo sapiens (human)
protein phosphorylationProtein kinase C alpha typeHomo sapiens (human)
mitotic nuclear membrane disassemblyProtein kinase C alpha typeHomo sapiens (human)
cell adhesionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of endothelial cell migrationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyProtein kinase C alpha typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C alpha typeHomo sapiens (human)
peptidyl-threonine phosphorylationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of cell migrationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of lipopolysaccharide-mediated signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C alpha typeHomo sapiens (human)
regulation of mRNA stabilityProtein kinase C alpha typeHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationProtein kinase C alpha typeHomo sapiens (human)
post-translational protein modificationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of macrophage differentiationProtein kinase C alpha typeHomo sapiens (human)
positive regulation of angiogenesisProtein kinase C alpha typeHomo sapiens (human)
positive regulation of bone resorptionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of cell adhesionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of mitotic cell cycleProtein kinase C alpha typeHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProtein kinase C alpha typeHomo sapiens (human)
response to interleukin-1Protein kinase C alpha typeHomo sapiens (human)
regulation of platelet aggregationProtein kinase C alpha typeHomo sapiens (human)
apoptotic signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
positive regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
positive regulation of angiotensin-activated signaling pathwayProtein kinase C alpha typeHomo sapiens (human)
positive regulation of dense core granule biogenesisProtein kinase C alpha typeHomo sapiens (human)
intracellular signal transductionProtein kinase C alpha typeHomo sapiens (human)
positive regulation of insulin secretionProtein kinase C alpha typeHomo sapiens (human)
protein phosphorylationProtein kinase C eta typeHomo sapiens (human)
signal transductionProtein kinase C eta typeHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationProtein kinase C eta typeHomo sapiens (human)
cell differentiationProtein kinase C eta typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C eta typeHomo sapiens (human)
positive regulation of keratinocyte differentiationProtein kinase C eta typeHomo sapiens (human)
positive regulation of B cell receptor signaling pathwayProtein kinase C eta typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C eta typeHomo sapiens (human)
positive regulation of glial cell proliferationProtein kinase C eta typeHomo sapiens (human)
protein kinase C signalingProtein kinase C eta typeHomo sapiens (human)
positive regulation of protein localization to plasma membraneProtein kinase C eta typeHomo sapiens (human)
regulation of bicellular tight junction assemblyProtein kinase C eta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C eta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C eta typeHomo sapiens (human)
protein phosphorylationProtein kinase C iota typeHomo sapiens (human)
protein targeting to membraneProtein kinase C iota typeHomo sapiens (human)
cytoskeleton organizationProtein kinase C iota typeHomo sapiens (human)
actin filament organizationProtein kinase C iota typeHomo sapiens (human)
positive regulation of neuron projection developmentProtein kinase C iota typeHomo sapiens (human)
vesicle-mediated transportProtein kinase C iota typeHomo sapiens (human)
cell migrationProtein kinase C iota typeHomo sapiens (human)
cellular response to insulin stimulusProtein kinase C iota typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C iota typeHomo sapiens (human)
establishment of apical/basal cell polarityProtein kinase C iota typeHomo sapiens (human)
eye photoreceptor cell developmentProtein kinase C iota typeHomo sapiens (human)
negative regulation of apoptotic processProtein kinase C iota typeHomo sapiens (human)
negative regulation of neuron apoptotic processProtein kinase C iota typeHomo sapiens (human)
establishment or maintenance of epithelial cell apical/basal polarityProtein kinase C iota typeHomo sapiens (human)
cell-cell junction organizationProtein kinase C iota typeHomo sapiens (human)
positive regulation of Notch signaling pathwayProtein kinase C iota typeHomo sapiens (human)
positive regulation of glucose importProtein kinase C iota typeHomo sapiens (human)
secretionProtein kinase C iota typeHomo sapiens (human)
Golgi vesicle buddingProtein kinase C iota typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C iota typeHomo sapiens (human)
positive regulation of glial cell proliferationProtein kinase C iota typeHomo sapiens (human)
membrane organizationProtein kinase C iota typeHomo sapiens (human)
cellular response to chemical stressProtein kinase C iota typeHomo sapiens (human)
response to interleukin-1Protein kinase C iota typeHomo sapiens (human)
regulation of postsynaptic membrane neurotransmitter receptor levelsProtein kinase C iota typeHomo sapiens (human)
positive regulation of protein localization to plasma membraneProtein kinase C iota typeHomo sapiens (human)
positive regulation of endothelial cell apoptotic processProtein kinase C iota typeHomo sapiens (human)
intracellular signal transductionProtein kinase C iota typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C iota typeHomo sapiens (human)
MAPK cascadeProtein kinase C epsilon typeHomo sapiens (human)
macrophage activation involved in immune responseProtein kinase C epsilon typeHomo sapiens (human)
protein phosphorylationProtein kinase C epsilon typeHomo sapiens (human)
apoptotic processProtein kinase C epsilon typeHomo sapiens (human)
signal transductionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of epithelial cell migrationProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of fibroblast migrationProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of cell-substrate adhesionProtein kinase C epsilon typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C epsilon typeHomo sapiens (human)
insulin secretionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of actin filament polymerizationProtein kinase C epsilon typeHomo sapiens (human)
negative regulation of protein ubiquitinationProtein kinase C epsilon typeHomo sapiens (human)
cell-substrate adhesionProtein kinase C epsilon typeHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of insulin secretionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of cytokinesisProtein kinase C epsilon typeHomo sapiens (human)
locomotory exploration behaviorProtein kinase C epsilon typeHomo sapiens (human)
TRAM-dependent toll-like receptor 4 signaling pathwayProtein kinase C epsilon typeHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionProtein kinase C epsilon typeHomo sapiens (human)
response to morphineProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of MAPK cascadeProtein kinase C epsilon typeHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of lipid catabolic processProtein kinase C epsilon typeHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosolProtein kinase C epsilon typeHomo sapiens (human)
cell divisionProtein kinase C epsilon typeHomo sapiens (human)
establishment of localization in cellProtein kinase C epsilon typeHomo sapiens (human)
synaptic transmission, GABAergicProtein kinase C epsilon typeHomo sapiens (human)
regulation of insulin secretion involved in cellular response to glucose stimulusProtein kinase C epsilon typeHomo sapiens (human)
mucus secretionProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of mucus secretionProtein kinase C epsilon typeHomo sapiens (human)
cellular response to ethanolProtein kinase C epsilon typeHomo sapiens (human)
cellular response to prostaglandin E stimulusProtein kinase C epsilon typeHomo sapiens (human)
cellular response to hypoxiaProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of wound healingProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of protein localization to plasma membraneProtein kinase C epsilon typeHomo sapiens (human)
negative regulation of sodium ion transmembrane transporter activityProtein kinase C epsilon typeHomo sapiens (human)
positive regulation of cellular glucuronidationProtein kinase C epsilon typeHomo sapiens (human)
intracellular signal transductionProtein kinase C epsilon typeHomo sapiens (human)
regulation of cell growthProtein kinase C theta typeHomo sapiens (human)
regulation of DNA-templated transcriptionProtein kinase C theta typeHomo sapiens (human)
protein phosphorylationProtein kinase C theta typeHomo sapiens (human)
membrane protein ectodomain proteolysisProtein kinase C theta typeHomo sapiens (human)
inflammatory responseProtein kinase C theta typeHomo sapiens (human)
axon guidanceProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomere maintenance via telomeraseProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-17 productionProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-2 productionProtein kinase C theta typeHomo sapiens (human)
positive regulation of interleukin-4 productionProtein kinase C theta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C theta typeHomo sapiens (human)
CD4-positive, alpha-beta T cell proliferationProtein kinase C theta typeHomo sapiens (human)
Fc-epsilon receptor signaling pathwayProtein kinase C theta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C theta typeHomo sapiens (human)
positive regulation of T cell activationProtein kinase C theta typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomerase activityProtein kinase C theta typeHomo sapiens (human)
cell chemotaxisProtein kinase C theta typeHomo sapiens (human)
negative regulation of T cell apoptotic processProtein kinase C theta typeHomo sapiens (human)
regulation of platelet aggregationProtein kinase C theta typeHomo sapiens (human)
positive regulation of telomere cappingProtein kinase C theta typeHomo sapiens (human)
positive regulation of T-helper 17 type immune responseProtein kinase C theta typeHomo sapiens (human)
positive regulation of CD4-positive, alpha-beta T cell proliferationProtein kinase C theta typeHomo sapiens (human)
positive regulation of T-helper 2 cell activationProtein kinase C theta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C theta typeHomo sapiens (human)
microtubule cytoskeleton organizationProtein kinase C zeta typeHomo sapiens (human)
positive regulation of cell-matrix adhesionProtein kinase C zeta typeHomo sapiens (human)
protein phosphorylationProtein kinase C zeta typeHomo sapiens (human)
inflammatory responseProtein kinase C zeta typeHomo sapiens (human)
signal transductionProtein kinase C zeta typeHomo sapiens (human)
cell surface receptor signaling pathwayProtein kinase C zeta typeHomo sapiens (human)
long-term memoryProtein kinase C zeta typeHomo sapiens (human)
positive regulation of cell population proliferationProtein kinase C zeta typeHomo sapiens (human)
cell migrationProtein kinase C zeta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C zeta typeHomo sapiens (human)
establishment of cell polarityProtein kinase C zeta typeHomo sapiens (human)
negative regulation of protein-containing complex assemblyProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-10 productionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-13 productionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-4 productionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of interleukin-5 productionProtein kinase C zeta typeHomo sapiens (human)
cellular response to insulin stimulusProtein kinase C zeta typeHomo sapiens (human)
negative regulation of apoptotic processProtein kinase C zeta typeHomo sapiens (human)
establishment or maintenance of epithelial cell apical/basal polarityProtein kinase C zeta typeHomo sapiens (human)
positive regulation of T-helper 2 cell differentiationProtein kinase C zeta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C zeta typeHomo sapiens (human)
positive regulation of insulin receptor signaling pathwayProtein kinase C zeta typeHomo sapiens (human)
vesicle transport along microtubuleProtein kinase C zeta typeHomo sapiens (human)
negative regulation of peptidyl-tyrosine phosphorylationProtein kinase C zeta typeHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityProtein kinase C zeta typeHomo sapiens (human)
positive regulation of protein transportProtein kinase C zeta typeHomo sapiens (human)
membrane depolarizationProtein kinase C zeta typeHomo sapiens (human)
membrane hyperpolarizationProtein kinase C zeta typeHomo sapiens (human)
long-term synaptic potentiationProtein kinase C zeta typeHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProtein kinase C zeta typeHomo sapiens (human)
protein kinase C signalingProtein kinase C zeta typeHomo sapiens (human)
protein localization to plasma membraneProtein kinase C zeta typeHomo sapiens (human)
regulation of neurotransmitter receptor localization to postsynaptic specialization membraneProtein kinase C zeta typeHomo sapiens (human)
neuron projection extensionProtein kinase C zeta typeHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialProtein kinase C zeta typeHomo sapiens (human)
positive regulation of T-helper 2 cell cytokine productionProtein kinase C zeta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C zeta typeHomo sapiens (human)
protein phosphorylationProtein kinase C delta typeHomo sapiens (human)
apoptotic processProtein kinase C delta typeHomo sapiens (human)
DNA damage responseProtein kinase C delta typeHomo sapiens (human)
signal transductionProtein kinase C delta typeHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressProtein kinase C delta typeHomo sapiens (human)
regulation of signaling receptor activityProtein kinase C delta typeHomo sapiens (human)
immunoglobulin mediated immune responseProtein kinase C delta typeHomo sapiens (human)
peptidyl-serine phosphorylationProtein kinase C delta typeHomo sapiens (human)
peptidyl-threonine phosphorylationProtein kinase C delta typeHomo sapiens (human)
termination of signal transductionProtein kinase C delta typeHomo sapiens (human)
negative regulation of actin filament polymerizationProtein kinase C delta typeHomo sapiens (human)
positive regulation of endodeoxyribonuclease activityProtein kinase C delta typeHomo sapiens (human)
negative regulation of protein bindingProtein kinase C delta typeHomo sapiens (human)
activation of protein kinase activityProtein kinase C delta typeHomo sapiens (human)
positive regulation of superoxide anion generationProtein kinase C delta typeHomo sapiens (human)
regulation of actin cytoskeleton organizationProtein kinase C delta typeHomo sapiens (human)
negative regulation of glial cell apoptotic processProtein kinase C delta typeHomo sapiens (human)
cellular response to UVProtein kinase C delta typeHomo sapiens (human)
positive regulation of protein dephosphorylationProtein kinase C delta typeHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisProtein kinase C delta typeHomo sapiens (human)
B cell proliferationProtein kinase C delta typeHomo sapiens (human)
neutrophil activationProtein kinase C delta typeHomo sapiens (human)
positive regulation of protein import into nucleusProtein kinase C delta typeHomo sapiens (human)
defense response to bacteriumProtein kinase C delta typeHomo sapiens (human)
negative regulation of MAP kinase activityProtein kinase C delta typeHomo sapiens (human)
regulation of mRNA stabilityProtein kinase C delta typeHomo sapiens (human)
post-translational protein modificationProtein kinase C delta typeHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayProtein kinase C delta typeHomo sapiens (human)
negative regulation of inflammatory responseProtein kinase C delta typeHomo sapiens (human)
negative regulation of peptidyl-tyrosine phosphorylationProtein kinase C delta typeHomo sapiens (human)
protein stabilizationProtein kinase C delta typeHomo sapiens (human)
negative regulation of filopodium assemblyProtein kinase C delta typeHomo sapiens (human)
cell chemotaxisProtein kinase C delta typeHomo sapiens (human)
cellular response to hydrogen peroxideProtein kinase C delta typeHomo sapiens (human)
cellular response to hydroperoxideProtein kinase C delta typeHomo sapiens (human)
negative regulation of platelet aggregationProtein kinase C delta typeHomo sapiens (human)
cellular senescenceProtein kinase C delta typeHomo sapiens (human)
positive regulation of phospholipid scramblase activityProtein kinase C delta typeHomo sapiens (human)
cellular response to angiotensinProtein kinase C delta typeHomo sapiens (human)
regulation of ceramide biosynthetic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of ceramide biosynthetic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of glucosylceramide catabolic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of sphingomyelin catabolic processProtein kinase C delta typeHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProtein kinase C delta typeHomo sapiens (human)
intracellular signal transductionProtein kinase C delta typeHomo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
angiogenesisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell proliferationSerine/threonine-protein kinase D1Homo sapiens (human)
apoptotic processSerine/threonine-protein kinase D1Homo sapiens (human)
inflammatory responseSerine/threonine-protein kinase D1Homo sapiens (human)
Golgi organizationSerine/threonine-protein kinase D1Homo sapiens (human)
signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
integrin-mediated signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
nervous system developmentSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of autophagySerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell migrationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of gene expressionSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of keratinocyte proliferationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of neuron projection developmentSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of skeletal muscle contraction by modulation of calcium ion sensitivity of myofibrilSerine/threonine-protein kinase D1Homo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
sphingolipid biosynthetic processSerine/threonine-protein kinase D1Homo sapiens (human)
cell differentiationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to amino acid starvationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to oxidative stressSerine/threonine-protein kinase D1Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of protein import into nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationSerine/threonine-protein kinase D1Homo sapiens (human)
innate immune responseSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of osteoblast differentiationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of angiogenesisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of cell sizeSerine/threonine-protein kinase D1Homo sapiens (human)
negative regulation of endocytosisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISerine/threonine-protein kinase D1Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of protein export from nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
Golgi vesicle transportSerine/threonine-protein kinase D1Homo sapiens (human)
defense response to Gram-negative bacteriumSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activitySerine/threonine-protein kinase D1Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of sarcomere organizationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to hydroperoxideSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to norepinephrine stimulusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of peptide hormone secretionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assemblySerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to angiotensinSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to endothelinSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell chemotaxisSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of integrin-mediated signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
MAPK cascadeRas guanyl-releasing protein 3Homo sapiens (human)
small GTPase-mediated signal transductionRas guanyl-releasing protein 3Homo sapiens (human)
Ras protein signal transductionRas guanyl-releasing protein 3Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (45)

Processvia Protein(s)Taxonomy
diacylglycerol-dependent serine/threonine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein bindingSerine/threonine-protein kinase D3Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase D3Homo sapiens (human)
kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase D3Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein kinase activityProtein kinase C gamma typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C gamma typeHomo sapiens (human)
calcium,diacylglycerol-dependent serine/threonine kinase activityProtein kinase C gamma typeHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityProtein kinase C gamma typeHomo sapiens (human)
protein bindingProtein kinase C gamma typeHomo sapiens (human)
ATP bindingProtein kinase C gamma typeHomo sapiens (human)
zinc ion bindingProtein kinase C gamma typeHomo sapiens (human)
protein serine kinase activityProtein kinase C gamma typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C gamma typeHomo sapiens (human)
chromatin bindingProtein kinase C beta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C beta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C beta typeHomo sapiens (human)
protein kinase C bindingProtein kinase C beta typeHomo sapiens (human)
calcium channel regulator activityProtein kinase C beta typeHomo sapiens (human)
protein bindingProtein kinase C beta typeHomo sapiens (human)
ATP bindingProtein kinase C beta typeHomo sapiens (human)
zinc ion bindingProtein kinase C beta typeHomo sapiens (human)
nuclear receptor coactivator activityProtein kinase C beta typeHomo sapiens (human)
histone H3T6 kinase activityProtein kinase C beta typeHomo sapiens (human)
histone bindingProtein kinase C beta typeHomo sapiens (human)
nuclear androgen receptor bindingProtein kinase C beta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C beta typeHomo sapiens (human)
protein kinase activityProtein kinase C alpha typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C alpha typeHomo sapiens (human)
calcium,diacylglycerol-dependent serine/threonine kinase activityProtein kinase C alpha typeHomo sapiens (human)
integrin bindingProtein kinase C alpha typeHomo sapiens (human)
protein bindingProtein kinase C alpha typeHomo sapiens (human)
ATP bindingProtein kinase C alpha typeHomo sapiens (human)
zinc ion bindingProtein kinase C alpha typeHomo sapiens (human)
enzyme bindingProtein kinase C alpha typeHomo sapiens (human)
histone H3T6 kinase activityProtein kinase C alpha typeHomo sapiens (human)
protein serine kinase activityProtein kinase C alpha typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C alpha typeHomo sapiens (human)
diacylglycerol bindingProtein kinase C alpha typeHomo sapiens (human)
protein kinase activityProtein kinase C eta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C eta typeHomo sapiens (human)
diacylglycerol-dependent, calcium-independent serine/threonine kinase activityProtein kinase C eta typeHomo sapiens (human)
protein bindingProtein kinase C eta typeHomo sapiens (human)
ATP bindingProtein kinase C eta typeHomo sapiens (human)
enzyme bindingProtein kinase C eta typeHomo sapiens (human)
small GTPase bindingProtein kinase C eta typeHomo sapiens (human)
metal ion bindingProtein kinase C eta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C eta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C eta typeHomo sapiens (human)
protein kinase activityProtein kinase C iota typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C iota typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C iota typeHomo sapiens (human)
protein bindingProtein kinase C iota typeHomo sapiens (human)
ATP bindingProtein kinase C iota typeHomo sapiens (human)
phospholipid bindingProtein kinase C iota typeHomo sapiens (human)
metal ion bindingProtein kinase C iota typeHomo sapiens (human)
protein serine kinase activityProtein kinase C iota typeHomo sapiens (human)
actin monomer bindingProtein kinase C epsilon typeHomo sapiens (human)
protein kinase activityProtein kinase C epsilon typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
diacylglycerol-dependent, calcium-independent serine/threonine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
protein bindingProtein kinase C epsilon typeHomo sapiens (human)
ATP bindingProtein kinase C epsilon typeHomo sapiens (human)
enzyme activator activityProtein kinase C epsilon typeHomo sapiens (human)
enzyme bindingProtein kinase C epsilon typeHomo sapiens (human)
signaling receptor activator activityProtein kinase C epsilon typeHomo sapiens (human)
ethanol bindingProtein kinase C epsilon typeHomo sapiens (human)
metal ion bindingProtein kinase C epsilon typeHomo sapiens (human)
14-3-3 protein bindingProtein kinase C epsilon typeHomo sapiens (human)
protein serine kinase activityProtein kinase C epsilon typeHomo sapiens (human)
protein kinase activityProtein kinase C theta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C theta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C theta typeHomo sapiens (human)
protein bindingProtein kinase C theta typeHomo sapiens (human)
ATP bindingProtein kinase C theta typeHomo sapiens (human)
metal ion bindingProtein kinase C theta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C theta typeHomo sapiens (human)
protein kinase activityProtein kinase C zeta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C zeta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C zeta typeHomo sapiens (human)
protein bindingProtein kinase C zeta typeHomo sapiens (human)
ATP bindingProtein kinase C zeta typeHomo sapiens (human)
potassium channel regulator activityProtein kinase C zeta typeHomo sapiens (human)
protein kinase bindingProtein kinase C zeta typeHomo sapiens (human)
phospholipase bindingProtein kinase C zeta typeHomo sapiens (human)
insulin receptor substrate bindingProtein kinase C zeta typeHomo sapiens (human)
protein-containing complex bindingProtein kinase C zeta typeHomo sapiens (human)
metal ion bindingProtein kinase C zeta typeHomo sapiens (human)
14-3-3 protein bindingProtein kinase C zeta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C zeta typeHomo sapiens (human)
protein kinase activityProtein kinase C delta typeHomo sapiens (human)
protein serine/threonine kinase activityProtein kinase C delta typeHomo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C delta typeHomo sapiens (human)
diacylglycerol-dependent, calcium-independent serine/threonine kinase activityProtein kinase C delta typeHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityProtein kinase C delta typeHomo sapiens (human)
protein bindingProtein kinase C delta typeHomo sapiens (human)
ATP bindingProtein kinase C delta typeHomo sapiens (human)
enzyme activator activityProtein kinase C delta typeHomo sapiens (human)
enzyme bindingProtein kinase C delta typeHomo sapiens (human)
protein kinase bindingProtein kinase C delta typeHomo sapiens (human)
insulin receptor substrate bindingProtein kinase C delta typeHomo sapiens (human)
metal ion bindingProtein kinase C delta typeHomo sapiens (human)
protein serine kinase activityProtein kinase C delta typeHomo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
protein kinase C bindingSerine/threonine-protein kinase D1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase D1Homo sapiens (human)
kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
heat shock protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase D1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
phosphatidylinositol 3-kinase activator activitySerine/threonine-protein kinase D1Homo sapiens (human)
guanyl-nucleotide exchange factor activityRas guanyl-releasing protein 3Homo sapiens (human)
GTPase activator activityRas guanyl-releasing protein 3Homo sapiens (human)
calcium ion bindingRas guanyl-releasing protein 3Homo sapiens (human)
protein bindingRas guanyl-releasing protein 3Homo sapiens (human)
kinase bindingRas guanyl-releasing protein 3Homo sapiens (human)
diacylglycerol bindingRas guanyl-releasing protein 3Homo sapiens (human)
small GTPase bindingRas guanyl-releasing protein 3Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (63)

Processvia Protein(s)Taxonomy
nucleoplasmSerine/threonine-protein kinase D3Homo sapiens (human)
cytosolSerine/threonine-protein kinase D3Homo sapiens (human)
plasma membraneSerine/threonine-protein kinase D3Homo sapiens (human)
cytosolSerine/threonine-protein kinase D3Homo sapiens (human)
nucleusProtein kinase C gamma typeHomo sapiens (human)
cytosolProtein kinase C gamma typeHomo sapiens (human)
plasma membraneProtein kinase C gamma typeHomo sapiens (human)
cell-cell junctionProtein kinase C gamma typeHomo sapiens (human)
postsynaptic densityProtein kinase C gamma typeHomo sapiens (human)
dendriteProtein kinase C gamma typeHomo sapiens (human)
calyx of HeldProtein kinase C gamma typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C gamma typeHomo sapiens (human)
synaptic membraneProtein kinase C gamma typeHomo sapiens (human)
presynaptic cytosolProtein kinase C gamma typeHomo sapiens (human)
postsynaptic cytosolProtein kinase C gamma typeHomo sapiens (human)
nucleusProtein kinase C beta typeHomo sapiens (human)
nucleoplasmProtein kinase C beta typeHomo sapiens (human)
cytoplasmProtein kinase C beta typeHomo sapiens (human)
centrosomeProtein kinase C beta typeHomo sapiens (human)
cytosolProtein kinase C beta typeHomo sapiens (human)
plasma membraneProtein kinase C beta typeHomo sapiens (human)
brush border membraneProtein kinase C beta typeHomo sapiens (human)
calyx of HeldProtein kinase C beta typeHomo sapiens (human)
extracellular exosomeProtein kinase C beta typeHomo sapiens (human)
presynaptic cytosolProtein kinase C beta typeHomo sapiens (human)
spectrinProtein kinase C beta typeHomo sapiens (human)
ciliary basal bodyProtein kinase C alpha typeHomo sapiens (human)
nucleoplasmProtein kinase C alpha typeHomo sapiens (human)
cytoplasmProtein kinase C alpha typeHomo sapiens (human)
mitochondrionProtein kinase C alpha typeHomo sapiens (human)
endoplasmic reticulumProtein kinase C alpha typeHomo sapiens (human)
cytosolProtein kinase C alpha typeHomo sapiens (human)
plasma membraneProtein kinase C alpha typeHomo sapiens (human)
mitochondrial membraneProtein kinase C alpha typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C alpha typeHomo sapiens (human)
extracellular exosomeProtein kinase C alpha typeHomo sapiens (human)
alphav-beta3 integrin-PKCalpha complexProtein kinase C alpha typeHomo sapiens (human)
cytoplasmProtein kinase C eta typeHomo sapiens (human)
cytosolProtein kinase C eta typeHomo sapiens (human)
plasma membraneProtein kinase C eta typeHomo sapiens (human)
cell-cell junctionProtein kinase C eta typeHomo sapiens (human)
extracellular exosomeProtein kinase C eta typeHomo sapiens (human)
Golgi membraneProtein kinase C iota typeHomo sapiens (human)
nucleusProtein kinase C iota typeHomo sapiens (human)
nucleoplasmProtein kinase C iota typeHomo sapiens (human)
endosomeProtein kinase C iota typeHomo sapiens (human)
cytosolProtein kinase C iota typeHomo sapiens (human)
plasma membraneProtein kinase C iota typeHomo sapiens (human)
brush borderProtein kinase C iota typeHomo sapiens (human)
bicellular tight junctionProtein kinase C iota typeHomo sapiens (human)
microtubule cytoskeletonProtein kinase C iota typeHomo sapiens (human)
apical plasma membraneProtein kinase C iota typeHomo sapiens (human)
cell leading edgeProtein kinase C iota typeHomo sapiens (human)
Schmidt-Lanterman incisureProtein kinase C iota typeHomo sapiens (human)
intercellular bridgeProtein kinase C iota typeHomo sapiens (human)
extracellular exosomeProtein kinase C iota typeHomo sapiens (human)
tight junctionProtein kinase C iota typeHomo sapiens (human)
Schaffer collateral - CA1 synapseProtein kinase C iota typeHomo sapiens (human)
glutamatergic synapseProtein kinase C iota typeHomo sapiens (human)
PAR polarity complexProtein kinase C iota typeHomo sapiens (human)
Golgi apparatusProtein kinase C epsilon typeHomo sapiens (human)
nucleusProtein kinase C epsilon typeHomo sapiens (human)
cytoplasmProtein kinase C epsilon typeHomo sapiens (human)
mitochondrionProtein kinase C epsilon typeHomo sapiens (human)
endoplasmic reticulumProtein kinase C epsilon typeHomo sapiens (human)
cytosolProtein kinase C epsilon typeHomo sapiens (human)
plasma membraneProtein kinase C epsilon typeHomo sapiens (human)
intracellular membrane-bounded organelleProtein kinase C epsilon typeHomo sapiens (human)
intermediate filament cytoskeletonProtein kinase C epsilon typeHomo sapiens (human)
synapseProtein kinase C epsilon typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C epsilon typeHomo sapiens (human)
cell peripheryProtein kinase C epsilon typeHomo sapiens (human)
immunological synapseProtein kinase C theta typeHomo sapiens (human)
cytosolProtein kinase C theta typeHomo sapiens (human)
plasma membraneProtein kinase C theta typeHomo sapiens (human)
aggresomeProtein kinase C theta typeHomo sapiens (human)
centriolar satelliteProtein kinase C theta typeHomo sapiens (human)
stress fiberProtein kinase C zeta typeHomo sapiens (human)
nuclear envelopeProtein kinase C zeta typeHomo sapiens (human)
cytoplasmProtein kinase C zeta typeHomo sapiens (human)
endosomeProtein kinase C zeta typeHomo sapiens (human)
microtubule organizing centerProtein kinase C zeta typeHomo sapiens (human)
cytosolProtein kinase C zeta typeHomo sapiens (human)
plasma membraneProtein kinase C zeta typeHomo sapiens (human)
cell-cell junctionProtein kinase C zeta typeHomo sapiens (human)
bicellular tight junctionProtein kinase C zeta typeHomo sapiens (human)
postsynaptic densityProtein kinase C zeta typeHomo sapiens (human)
membraneProtein kinase C zeta typeHomo sapiens (human)
apical plasma membraneProtein kinase C zeta typeHomo sapiens (human)
nuclear matrixProtein kinase C zeta typeHomo sapiens (human)
cell junctionProtein kinase C zeta typeHomo sapiens (human)
cell leading edgeProtein kinase C zeta typeHomo sapiens (human)
vesicleProtein kinase C zeta typeHomo sapiens (human)
myelin sheath abaxonal regionProtein kinase C zeta typeHomo sapiens (human)
axon hillockProtein kinase C zeta typeHomo sapiens (human)
apical cortexProtein kinase C zeta typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C zeta typeHomo sapiens (human)
extracellular exosomeProtein kinase C zeta typeHomo sapiens (human)
tight junctionProtein kinase C zeta typeHomo sapiens (human)
Schaffer collateral - CA1 synapseProtein kinase C zeta typeHomo sapiens (human)
glutamatergic synapseProtein kinase C zeta typeHomo sapiens (human)
PAR polarity complexProtein kinase C zeta typeHomo sapiens (human)
extracellular regionProtein kinase C delta typeHomo sapiens (human)
nucleusProtein kinase C delta typeHomo sapiens (human)
nucleoplasmProtein kinase C delta typeHomo sapiens (human)
cytoplasmProtein kinase C delta typeHomo sapiens (human)
mitochondrionProtein kinase C delta typeHomo sapiens (human)
endoplasmic reticulumProtein kinase C delta typeHomo sapiens (human)
cytosolProtein kinase C delta typeHomo sapiens (human)
plasma membraneProtein kinase C delta typeHomo sapiens (human)
cell-cell junctionProtein kinase C delta typeHomo sapiens (human)
nuclear matrixProtein kinase C delta typeHomo sapiens (human)
azurophil granule lumenProtein kinase C delta typeHomo sapiens (human)
endolysosomeProtein kinase C delta typeHomo sapiens (human)
perinuclear region of cytoplasmProtein kinase C delta typeHomo sapiens (human)
extracellular exosomeProtein kinase C delta typeHomo sapiens (human)
autophagosome membraneSerine/threonine-protein kinase D1Homo sapiens (human)
nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
trans-Golgi networkSerine/threonine-protein kinase D1Homo sapiens (human)
cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
plasma membraneSerine/threonine-protein kinase D1Homo sapiens (human)
cell-cell junctionSerine/threonine-protein kinase D1Homo sapiens (human)
cell cortexSerine/threonine-protein kinase D1Homo sapiens (human)
Z discSerine/threonine-protein kinase D1Homo sapiens (human)
perinuclear region of cytoplasmSerine/threonine-protein kinase D1Homo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase D1Homo sapiens (human)
cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
plasma membraneRas guanyl-releasing protein 3Homo sapiens (human)
perinuclear region of cytoplasmRas guanyl-releasing protein 3Homo sapiens (human)
guanyl-nucleotide exchange factor complexRas guanyl-releasing protein 3Homo sapiens (human)
plasma membraneRas guanyl-releasing protein 3Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (208)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1459493Activation of PKC in human platelet assessed as phosphorylation of p38 at 0.1 uM measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID282122Induction of translocation of RasGRP1 to plasma membrane in HEK293 cells2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID746932Induction of EBV-early antigen expressed in human Raji cells at 10'-6 M after 48 hrs by immunofluorescence assay relative to control2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Structure-activity studies on the side chain of a simplified analog of aplysiatoxin (aplog-1) with anti-proliferative activity.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID336961Displacement of [3H]TPA from TPA receptor in ICR mouse dorsal epidermis
AID1459490Activation of PKC in human platelet assessed as phosphorylation of VASP at 0.1 uM measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1459487Activation of PKC in human platelet assessed as phosphorylation of AKT at ser-308 at 0.1 uM measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID378390Displacement of [3H]PDBu from partially purified rabbit brain PKC1999Journal of natural products, Feb, Volume: 62, Issue:2
28-deacetylbelamcandal, a tumor-promoting triterpenoid from Iris tectorum.
AID327061Cytotoxicity against BALB/c mouse 3T3 cells2008Journal of natural products, Jan, Volume: 71, Issue:1
Isolation of cytotoxic metabolites from targeted peruvian amazonian medicinal plants.
AID1291798Induction of cell differentiation in human U937 cells assessed as upregulation of CD68 at 0.1 uM after 72 hrs by flow cytometry (Rvb = 5.9%)2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Induction of apoptosis and differentiation by atractylenolide-1 isolated from Atractylodes macrocephala in human leukemia cells.
AID164825Activation of partially purified HeLa cell protein kinase C, 32P incorporation into calf thymus histone(III-S).1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis of structural analogues of lyngbyatoxin A and their evaluation as activators of protein kinase C.
AID745813Cytotoxicity against human SNU387 cells after 48 hrs by MTT assay2013Journal of natural products, May-24, Volume: 76, Issue:5
Cytotoxic phorbol esters of Croton tiglium.
AID282121Increase in ERK phosphorylation in Rat2 cells expressing human Ras-GTP1 at 100 nM2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID501124Activation of PKC signaling in human HUES8 definitive endoderm cells assessed as increase in Pdx1-expressing cells at 14 nM after 4 days by immunocytochemistry (Rvb = 2.8+/-0.6%)2009Nature chemical biology, Apr, Volume: 5, Issue:4
A small molecule that directs differentiation of human ESCs into the pancreatic lineage.
AID1532547Induction of mitochondrial dysfunction in human MCF7 cells assessed as mitochondria fusion at 400 nM after 6 hrs in presence of UV irradiation by Mitotracker Orange CMTM-ROS staining-based confocal microscopic analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and photocytotoxic activity of [1,2,3]triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines.
AID220518Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C delta2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
AID517259Inhibition of TPA-induced EBA-early antigen production in human Raji cells at 1 uM2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID1228048Induction of human HL60 cell differentiation into macrophages at 16 nM after 72 hrs by May-Giemsa staining based microscopy2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Mebamamides A and B, Cyclic Lipopeptides Isolated from the Green Alga Derbesia marina.
AID1332914Induction of lysosomal dysfunction in human MCF7 cells at 400 nM irradiated with 1.5 J/cm2 UV-light measured after 6 hrs by Lysotracker green DND staining based confocal microscopic method2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and antiproliferative mechanism of action of pyrrolo[3',2':6,7] cyclohepta[1,2-d]pyrimidin-2-amines as singlet oxygen photosensitizers.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID378689Carcinogenesis in CD1 mouse skin assessed as tumor incidence at 4 nmol twice a week for 20 weeks1999Journal of natural products, Feb, Volume: 62, Issue:2
28-deacetylbelamcandal, a tumor-promoting triterpenoid from Iris tectorum.
AID599041Activation of human recombinant PKCalpha assessed as rate of phosphate incorporation into PepTag C1 peptide at 0.001 uM after 40 mins by agarose gel electrophoresis analysis relative to control2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID1459507Activation of PKC in human platelet assessed as phosphorylation of PKC substrates at 0.1 uM measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID501122Activation of PKC signaling in human HUES8 cells assessed as increase in Pdx1-expressing cells at 14 nM after 4 days by immunocytochemistry pregrown in medium with Wnt3a, activin A, FGF10, KAAD-cyclopamine and retinoic acid relative to ILV treated cells2009Nature chemical biology, Apr, Volume: 5, Issue:4
A small molecule that directs differentiation of human ESCs into the pancreatic lineage.
AID1505443Activation of GFP-tagged RasGRP3 (unknown origin) expressed in HEK293 cells after 30 mins by immunoblot method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
α-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.
AID1439397Induction of mitochondrial dysfunction in human MCF7 cells assessed as organelle fusion at 400 nM upon UV light irradiation measured after 6 hrs by mitotracker orange CMTM-ROS/LCS1 dye based confocal microscopic method2017European journal of medicinal chemistry, Mar-10, Volume: 128Pyrrolo[3',2':6,7]cyclohepta[1,2-b]pyridines with potent photo-antiproliferative activity.
AID662571Antiproliferative activity against human U937 cells at 0.1 to 1000 nM after 60 hrs2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.
AID687827Tumor promoting activity in human Raji cells assessed as induction of EBV-early antigen activation at 1 uM after 48 hrs by FITC staining based indirect immunofluorescence assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.
AID221443Activity against TPA-induced epidermal hyperplasia in mice, and epidermal thickness value was reported2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
New strategy for antedrug application: development of metalloproteinase inhibitors as antipsoriatic drugs.
AID378387Induction of human HL-60 cell adhesion after 48 hrs1999Journal of natural products, Feb, Volume: 62, Issue:2
28-deacetylbelamcandal, a tumor-promoting triterpenoid from Iris tectorum.
AID718287Selectivity index, ratio of CC50 for african green monkey Vero cells to EC50 for Chikungunya virus 8992012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID378389Activation of rabbit brain PKC assessed as [32P] incorporation in histone 3-S from [gamma32P]ATP1999Journal of natural products, Feb, Volume: 62, Issue:2
28-deacetylbelamcandal, a tumor-promoting triterpenoid from Iris tectorum.
AID221771Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C gamma2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
AID1228117Induction of cell attachment of human U937 cells at 0.1 nM to 1000 nM after 60 hrs by particle counter based cell counting assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships.
AID164962Inhibition of [3H]PDBu binding to murine brain PKC (protein kinase C)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Cyclohexane diester analogues of phorbol ester as potential activators of protein kinase C.
AID1459529Induction of PKC-theta translocation from cytosol to plasma membrane in human platelet at 0.1 uM measured after 1 min by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1231851Selectivity index, CC50 for african green monkey Vero cells to EC50 for HIV2 ROD2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID458317Binding affinity to GST-tagged PKCtheta expressed in Escherichia coli BL21(DE3) by fluorescence quenching2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.
AID1231846Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID614623Binding affinity to recombinant C1 domain of PKCalpha expressed in Escherichia coli BL21 (DE3) after 45 mins by fluorescence quenching assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Chemical modifications of resveratrol for improved protein kinase C alpha activity.
AID1502298Cytotoxicity against African green monkey Vero cells assessed as morphological changes by microscopic method2017Journal of natural products, 10-27, Volume: 80, Issue:10
Environmentally Friendly Procedure Based on Supercritical Fluid Chromatography and Tandem Mass Spectrometry Molecular Networking for the Discovery of Potent Antiviral Compounds from Euphorbia semiperfoliata.
AID1459532Activation of PKC in human platelet assessed as increase in platelet secretion by measuring ATP release at 0.1 uM in presence of PKCalpha/beta inhibitor Go6976 measured after 5 mins by luciferin-luciferase assay2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID718286Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID1502299Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Chikungunya virus Indian ocean strain 899 infected in African green monkey Vero cells2017Journal of natural products, 10-27, Volume: 80, Issue:10
Environmentally Friendly Procedure Based on Supercritical Fluid Chromatography and Tandem Mass Spectrometry Molecular Networking for the Discovery of Potent Antiviral Compounds from Euphorbia semiperfoliata.
AID751657Displacement of [3H]PDBu from phorbol ester receptor in ICR mouse brain after 60 mins2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID220908Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C beta2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
AID378388Induction of TNFalpha release from human HL-60 cells after 24 hrs by ELISA1999Journal of natural products, Feb, Volume: 62, Issue:2
28-deacetylbelamcandal, a tumor-promoting triterpenoid from Iris tectorum.
AID687836Tumor promoting activity in ICR mouse assessed as effect on DMBA-mediated skin carcinogenesis at 1.7 nmol administered 1 week after DMBA challenge twice weekly measured after 6 weeks by two-stage carcinogenesis test2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.
AID1152274Activation of RasGRP3 (unknown origin) overexpressed in HEK293 cells assessed as ERK1/2 phosphorylation at 0.1 to 30 uM after 30 mins by Western blot analysis2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
AID218937Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C epsilon2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
AID517260Induction of EBA-early antigen production in human Raji cells at 1 uM2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID1291799Induction of cell differentiation in human U937 cells assessed as upregulation of CD14 at 0.1 uM after 72 hrs by flow cytometry (Rvb = 4.3%)2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Induction of apoptosis and differentiation by atractylenolide-1 isolated from Atractylodes macrocephala in human leukemia cells.
AID282126Induction of T cell activation marker CD69 expression in concanavalin-A activated CD8+ mouse spleen lymphocytes2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID662638Modulation of PKCepsilon in human K562 cells assessed as induction of protein activity after 24 hrs by Western blotting analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.
AID1459513Induction of PKC-delta translocation from cytosol to plasma membrane in human platelet at 0.1 uM measured after 1 min by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID599015Activation of human recombinant PKCalpha assessed as rate of phosphate incorporation into PepTag C1 peptide at 0.1 uM after 40 mins by agarose gel electrophoresis analysis relative to control2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID662639Modulation of RASGRP3 in human K562 cells assessed as induction of protein activity after 24 hrs by Western blotting analysis2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.
AID517255Cytotoxicity against human Raji cells assessed as viability at 1 uM in presence of TPA2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID380908Toxicity against Swiss-Webster mouse assessed as irritation in ear per 5 ul after 4 hrs
AID1291794Induction of phagocytosis in human U937 cells at 0.1 uM measured using fluorescent latex beads after 2 hrs by flow cytometry2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Induction of apoptosis and differentiation by atractylenolide-1 isolated from Atractylodes macrocephala in human leukemia cells.
AID1655260Displacement of [3H]PDBu from recombinant human PKCalpha expressed in baculovirus infected Sf9 insect cells incubated for 10 mins by liquid scintillation counting method2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Missing Selectivity of Targeted 4β-Phorbol Prodrugs Expected to be Potential Chemotherapeutics.
AID1459482Activation of PKC in human platelet assessed as induction of platelet aggregation measured within 15 mins by tribidimetric method2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1439401Induction of lysosomal activation in human MCF7 cells at 400 nM upon UV light irradiation measured up to 6 hrs by lysotracker green DND26 dye based confocal microscopic method2017European journal of medicinal chemistry, Mar-10, Volume: 128Pyrrolo[3',2':6,7]cyclohepta[1,2-b]pyridines with potent photo-antiproliferative activity.
AID80963Tested for superoxide (O2-) generation inducing activity in differentiated HL-60 cells at 10e-7 M2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.
AID662570Induction of human U937 cells attachment at 0.1 to 1000 nM treated for 24 hrs measured after 60 hrs2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.
AID1152280Binding affinity to recombinant human GFP-tagged PKC-alpha expressed in CHOK1 cells assessed as induction of protein translocation from plasma membrane to internal membrane at 1000 nM after 5 to 15 mins by confocal microscopic analysis2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
AID1459511Induction of PKC-beta1 translocation from cytosol to plasma membrane in human platelet at 0.1 uM measured after 1 min by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1655282Activation of PKC in human DU145 cells assessed as increase in ERK1/ERK2 phosphorylation at 10 nM incubated for 30 mins by Western blot analysis2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Missing Selectivity of Targeted 4β-Phorbol Prodrugs Expected to be Potential Chemotherapeutics.
AID608032Induction of sensitization of human HeLa cells to staurosporine-induced apoptosis assessed as induction DNA fragmentation at 160 nM after 24 hrs by propidium iodide-staining based FACS assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1152284Binding affinity to recombinant human GFP-tagged PKC-delta expressed in human LNCAP cells assessed as induction of protein translocation from plasma membrane to internal membrane at 1000 nM after 2 to 10 mins by confocal microscopic analysis2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
AID1332910Induction of mitochondrial fusion in human MCF7 cells at 400 nM irradiated with 1.5 J/cm2 UV-light measured after 6 hrs by Mitotracker orange CMTM-ROS/Nuclear green staining based confocal microscopic method2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and antiproliferative mechanism of action of pyrrolo[3',2':6,7] cyclohepta[1,2-d]pyrimidin-2-amines as singlet oxygen photosensitizers.
AID282120Induction of increase in Ras-GTP level in Rat2 cells expressing human Ras-GTP1 at 100 nM2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID1502297Antiviral activity against Chikungunya virus Indian ocean strain 899 infected in African green monkey Vero cells assessed as reduction in virus-induced cytopathic effect by MTS assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Environmentally Friendly Procedure Based on Supercritical Fluid Chromatography and Tandem Mass Spectrometry Molecular Networking for the Discovery of Potent Antiviral Compounds from Euphorbia semiperfoliata.
AID718289Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID599040Activation of human recombinant PKCalpha assessed as rate of phosphate incorporation into PepTag C1 peptide at 0.01 uM after 40 mins by agarose gel electrophoresis analysis relative to control2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID746931Cytotoxicity against human Raji cells assessed as cell viability at 10'-7 M2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Structure-activity studies on the side chain of a simplified analog of aplysiatoxin (aplog-1) with anti-proliferative activity.
AID1459499Activation of PKC in human platelet assessed as induction of platelet aggregation in presence of PKC inhibitor GF109203X measured within 15 mins by tribidimetric method2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID282119Accumulation of Ras-GTP level in Rat2 cells expressing empty pBabePuro vector2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID1459509Induction of PKC-alpha translocation from cytosol to plasma membrane in human platelet at 0.1 uM measured after 1 min by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1459520Activation of PKC in human platelet assessed as reduction in phosphorylation of p38 at 0.1 in presence of PKCalpha/beta inhibitor Go6976 measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID718288Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID1231847Selectivity index, CC50 for african green monkey Vero cells to EC50 for chikungunya virus Indian ocean strain 8992015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID1808956Activation of GFP-fused PKCalpha in HeLa cells assessed as translocation of PKCepsilon from cytosol to membrane measured after 30 mins by DAPI staining based fluorescence microscopy2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Design, Synthesis, and Characterization of Novel
AID1459517Activation of PKC in human platelet assessed as reduction in phosphorylation of MARCK at 0.1 uM in presence of PKCalpha/beta inhibitor Go6976 measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID530150Effect on polymorphonuclear neutrophil killing of Aspergillus fumigatus assessed as survival rate of fungi (Rvb = 53% +/- 11%)2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Impact of mycophenolic acid on the functionality of human polymorphonuclear neutrophils and dendritic cells during interaction with Aspergillus fumigatus.
AID334631Skin irritant activity in SIM mouse ear assessed as irritation unit per ear after 24 hrs
AID517256Cytotoxicity against human Raji cells assessed as viability at 1 uM2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID599012Activation of human recombinant PKCalpha assessed as rate of phosphate incorporation into PepTag C1 peptide at 100 uM after 40 mins by agarose gel electrophoresis analysis relative to control2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID608031Induction of sensitization of human HeLa cells to camptothecin-induced apoptosis assessed as induction DNA fragmentation at 160 nM after 24 hrs by propidium iodide-staining based FACS assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.
AID1535468Activation of firefly luciferase activity expressed in HEK293T cells after 6 hrs by luminescence assay2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
Discovery of an isocoumarin analogue that modulates neuronal functions via neurotrophin receptor TrkB.
AID1228050Induction of human HL60 cell phagocytotic activity at 16 nM after 48 hrs by trypan based fluorescent microscopy2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Mebamamides A and B, Cyclic Lipopeptides Isolated from the Green Alga Derbesia marina.
AID1332902Photocytotoxicity against human MCF7 cells assessed as increase in production of radical oxygen species at 400 nM pretreated for 30 mins followed by 1.5 J/cm2 UV-light irradiation for 5 mins measured after 6 hrs by H2DCFDA dye based fluorescence assay rel2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and antiproliferative mechanism of action of pyrrolo[3',2':6,7] cyclohepta[1,2-d]pyrimidin-2-amines as singlet oxygen photosensitizers.
AID1459505Activation of PKC in human platelet assessed as phosphorylation of ERK at 0.1 uM measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID746929Cytotoxicity against human Raji cells assessed as cell viability at 10'-6 M2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Structure-activity studies on the side chain of a simplified analog of aplysiatoxin (aplog-1) with anti-proliferative activity.
AID654581Immunomodulatory activity in human NK92 cells assessed as induction of IFNgamma after 12 hrs by ELISA2012Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6
Tigliane diterpene esters with IFN γ-inducing activity from the leaves of Aleurites fordii.
AID458315Binding affinity to GST-tagged PKCdelta expressed in Escherichia coli BL21(DE3) by fluorescence quenching2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.
AID746933Induction of EBV-early antigen expressed in human Raji cells at 10'-7 M after 48 hrs by immunofluorescence assay relative to control2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Structure-activity studies on the side chain of a simplified analog of aplysiatoxin (aplog-1) with anti-proliferative activity.
AID380909Toxicity against Swiss-Webster mouse assessed as irritation in ear per 5 ul after 24 hrs
AID1459518Activation of PKC in human platelet assessed as reduction in phosphorylation of AKT at ser-308 at 0.1 uM in presence of PKCalpha/beta inhibitor Go6976 measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1332901Photocytotoxicity against human MCF7 cells assessed as increase in production of radical oxygen species at 400 nM pretreated for 30 mins followed by 1.5 J/cm2 UV-light irradiation for 5 mins measured after 2 hrs by H2DCFDA dye based fluorescence assay rel2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and antiproliferative mechanism of action of pyrrolo[3',2':6,7] cyclohepta[1,2-d]pyrimidin-2-amines as singlet oxygen photosensitizers.
AID599014Activation of human recombinant PKCalpha assessed as rate of phosphate incorporation into PepTag C1 peptide at 1 uM after 40 mins by agarose gel electrophoresis analysis relative to control2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID1532552Induction of lysosomal activation in human MCF7 cells at 400 nM after 6 hrs under UV-irradiation by Lysotracker Green DND 26 staining-based confocal microscopic analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and photocytotoxic activity of [1,2,3]triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines.
AID1291800Induction of cell differentiation in human K562 cells assessed as upregulation of CD14 at 0.1 uM after 72 hrs by flow cytometry (Rvb = 6.4%)2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Induction of apoptosis and differentiation by atractylenolide-1 isolated from Atractylodes macrocephala in human leukemia cells.
AID1228113Growth inhibition of human U937 cells at 0.1 nM to 1000 nM after 72 hrs by particle counter based cell counting assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships.
AID1291795Induction of phagocytosis in human K562 cells at 0.1 uM preincubated for 4 to 6 days followed by addition of fluorescent latex beads measured after 2 hrs by flow cytometry2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Induction of apoptosis and differentiation by atractylenolide-1 isolated from Atractylodes macrocephala in human leukemia cells.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID357337Toxicity in mouse assessed as irritant dose causing ear redness after 24 hours by inflammation assay2001Journal of natural products, Aug, Volume: 64, Issue:8
New jatrophane diterpenoid esters from Euphorbia turczaninowii.
AID1808955Activation of GFP-fused PKCepsilon in HeLa cells assessed as translocation of PKCepsilon from cytosol to membrane measured after 30 mins by DAPI staining based fluorescence microscopy2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Design, Synthesis, and Characterization of Novel
AID334632Skin irritant activity in NMRI mouse ear assessed as irritant dose 50 per ear after 24 hrs
AID599013Activation of human recombinant PKCalpha assessed as rate of phosphate incorporation into PepTag C1 peptide at 10 uM after 40 mins by agarose gel electrophoresis analysis relative to control2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID282125Induction of T cell activation marker CD69 expression in concanavalin-A activated CD4+ mouse spleen lymphocytes2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID599042Activation of human recombinant PKCalpha assessed as rate of phosphate incorporation into PepTag C1 peptide at 0.0001 uM after 40 mins by agarose gel electrophoresis analysis relative to control2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID1281296Induction of cell differentiation in human HL60 at 10 uM after 3 days by leishmans staining based microscopic analysis2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Synthesis of minoxidil conjugates and their evaluation as HL-60 differentiation agents.
AID1152271Activation of RasGRP3 (unknown origin) overexpressed in HEK293 cells assessed as protein phosphorylation at T133 at 0.1 to 30 uM after 30 mins by Western blot analysis2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
AID357338Toxicity in mouse assessed as irritant dose causing ear redness after 4 hours by inflammation assay2001Journal of natural products, Aug, Volume: 64, Issue:8
New jatrophane diterpenoid esters from Euphorbia turczaninowii.
AID1231849Selectivity index, CC50 for african green monkey Vero cells to EC50 for HIV1 3B2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID1226755Immunostimulatory activity in B6 mouse iNKT cells assessed as induction of IFN-gamma production incubated for 16 hrs followed by brefeldin A addition measured after 2 hrs by flow cytometric analysis in presence of ionomycin (Rvb = 0.6%)2015ACS medicinal chemistry letters, Apr-09, Volume: 6, Issue:4
Synthesis and Biological Activities of 5-Thio-α-GalCers.
AID1491060Proinflammatory activity in human neutrophils assessed as elastase release by measuring degranulation of azurophilic granules using MeOSuc-Ala-Ala-ProVal-p-nitroanilide as substrate incubated for 5 mins relative to control2017Journal of natural products, 05-26, Volume: 80, Issue:5
Inflammation Modulatory Phorbol Esters from the Seeds of Aquilaria malaccensis.
AID280060Induction of attachment of U937 cells after 48 hrs2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.
AID599010Displacement of [3H]PDBu from human recombinant PKCalpha after 20 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID458316Binding affinity to GST-tagged PKCepsilon expressed in Escherichia coli BL21(DE3) by fluorescence quenching2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.
AID1152273Activation of PKC-delta in HEK293 cells overexpressing RasGRP3 assessed as protein phosphorylation at S299 at 0.1 to 30 uM after 30 mins by Western blot analysis2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
AID1459503Activation of PKC in human platelet assessed as phosphorylation of MARCK at 0.1 uM measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1532533Induction of ROS generation in human MCF7 cells at 0.4 uM preincubated for 30 mins followed by irradiation at 1.5 J/cm2 for 2 hrs by H2DCFDA probe-based fluorescence assay (Rvb = 100%)2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and photocytotoxic activity of [1,2,3]triazolo[4,5-h][1,6]naphthyridines and [1,3]oxazolo[5,4-h][1,6]naphthyridines.
AID282124Induction of T cell activation marker CD69 expression in PBL cells2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID517257Cytotoxicity against human Raji cells assessed as viability at 10'-7 M in presence of TPA2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID1459501Activation of PKC in human platelet assessed as increase in platelet secretion by measuring ATP release at 0.1 uM in presence of PKC inhibitor GF109203X measured after 5 mins by luciferin-luciferase assay2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1505448Activation of PKCdelta (unknown origin) expressed in HEK293 cells harboring GFP-tagged RasGRP3 assessed as phosphorylation at ser299 residues after 30 mins by immunoblot method2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
α-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.
AID334931Displacement of [3H]TPA from TPA receptor in ICR mouse epidermal particulate fraction by Me2CO filter method
AID282118Activation of ERK in knockout mouse RasGRP1- mutant thymocytes2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID718290Cytotoxicity against african green monkey Vero cells by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID1655280Activation of PKC in human 22Rv1 cells assessed as increase in ERK1/ERK2 phosphorylations at 10 nM incubated for 30 mins by Western blot analysis2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Missing Selectivity of Targeted 4β-Phorbol Prodrugs Expected to be Potential Chemotherapeutics.
AID1505458Selectivity ratio of EC50 for PKCdelta (unknown origin) expressed in HEK293 cells harboring GFP-tagged RasGRP3 to EC50 for GFP-tagged RasGRP3 (unknown origin) expressed in HEK293 cells2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
α-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.
AID1152272Activation of PKC-delta in HEK293 cells assessed as protein phosphorylation at S299 at 0.1 to 30 uM after 30 mins by Western blot analysis2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
AID327069Cytotoxicity against human K562 cells2008Journal of natural products, Jan, Volume: 71, Issue:1
Isolation of cytotoxic metabolites from targeted peruvian amazonian medicinal plants.
AID1439385Induction of ROS generation in human MCF7 cells at 400 nM preincubated for 30 mins followed by UV light irradiation measured after 2 hrs by H2DCFDA staining based fluorescence assay relative to control2017European journal of medicinal chemistry, Mar-10, Volume: 128Pyrrolo[3',2':6,7]cyclohepta[1,2-b]pyridines with potent photo-antiproliferative activity.
AID517261Inhibition of TPA-induced EBA-early antigen production in human Raji cells at 10'-7 M2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID751722Displacement of [3H]PDBu from phorbol ester receptor in ICR mouse brain at 10 uM after 60 mins relative to control2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.
AID1231848Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID1459515Activation of PKC in human platelet assessed as platelet aggregation in presence of PKCalpha/beta inhibitor Go6976 measured within 15 mins by tribidimetric method2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID1459496Activation of PKC in human platelet assessed as phosphorylation of PKD at 0.1 uM measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID334633Skin irritant activity in NMRI mouse ear assessed as irritancy 50 after 24 hrs
AID1152286Binding affinity to recombinant human GFP-tagged RasGRP3 expressed in human LNCAP cells assessed as induction of protein translocation from plasma membrane to internal membrane at 1000 nM after 2 to 10 mins by confocal microscopic analysis2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological, and biophysical studies of DAG-indololactones designed as selective activators of RasGRP.
AID1459516Activation of PKC in human platelet assessed as reduction in phosphorylation of PKC substrates at 0.1 uM in presence of PKCalpha/beta inhibitor Go6976 measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID296501Induction of HIV-LTR transactivation assessed by GFP expression in Jurkat cells at 10 ng/ml after 36 hrs by flow cytometry2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Isolation of new phenylacetylingol derivatives that reactivate HIV-1 latency and a novel spirotriterpenoid from Euphorbia officinarum latex.
AID687839Tumor promoting activity in DMBA treated ICR mouse assessed as number of papillomas at 1.7 nmol administered 1 week after DMBA challenge twice weekly measured after 20 weeks by two-stage carcinogenesis test2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.
AID1459519Activation of PKC in human platelet assessed as reduction in phosphorylation of VASP at 0.1 uM in presence of PKCalpha/beta inhibitor Go6976 measured after 10 mins by Western blot analysis2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID687838Tumor promoting activity in ICR mouse assessed as effect on DMBA-mediated skin carcinogenesis at 1.7 nmol administered 1 week after DMBA challenge twice weekly measured after 11 weeks by two-stage carcinogenesis test2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.
AID282117Activation of ERK in wild type mouse thymocytes at 100 nM2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID1491059Proinflammatory activity in human neutrophils assessed as superoxide anion generation at 10 uM incubated for 5 mins by spectrophotometric method relative to control2017Journal of natural products, 05-26, Volume: 80, Issue:5
Inflammation Modulatory Phorbol Esters from the Seeds of Aquilaria malaccensis.
AID280058Inhibition of cell proliferation in WEHI231 cell line after 48 hrs2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.
AID1459484Activation of PKC in human platelet assessed as increase in platelet secretion by measuring ATP release at 0.1 uM measured after 5 mins by luciferin-luciferase assay2016Journal of natural products, 10-28, Volume: 79, Issue:10
Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.
AID517258Cytotoxicity against human Raji cells assessed as viability at 10'-7 M2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID1231850Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID1502294Antiviral activity against HIV NL4.3 harboring renilla luciferase infected in human MT2 cells pretreated for 2 hrs followed by viral infection measured after 48 to 96 hrs post infection by luciferase reporter gene assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Environmentally Friendly Procedure Based on Supercritical Fluid Chromatography and Tandem Mass Spectrometry Molecular Networking for the Discovery of Potent Antiviral Compounds from Euphorbia semiperfoliata.
AID1228120Induction of TNFalpha secretion in human U937 cells at 0.01 nM to 10000 nM by real time qPCR method2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships.
AID218662Inhibition of [3H]-phorbol 12,13-dibutyrate (PDBu) binding to human recombinant protein kinase C alpha2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.
AID282123Induction of T cell activation marker CD69 expression in Jurkat T cells at 100 nM2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Synthetic bryostatin analogues activate the RasGRP1 signaling pathway.
AID517254Induction of EBA-early antigen production in human Raji cells at 10'-7 M2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.
AID464279Activation of latent recombinant HIV1 LTR-GFP gene expression infected in human Jurkat LAT-GFP cells assessed as GFP positive cells after 6 hrs by flow cytometry relative to control2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Synthesis and biological evaluation of 12-aminoacylphorboids.
AID1346465Rat KNa1.1 (Calcium- and sodium-activated potassium channels)2006The Journal of neuroscience : the official journal of the Society for Neuroscience, May-10, Volume: 26, Issue:19
Opposite regulation of Slick and Slack K+ channels by neuromodulators.
AID1346458Human KNa1.2 (Calcium- and sodium-activated potassium channels)2006The Journal of neuroscience : the official journal of the Society for Neuroscience, May-10, Volume: 26, Issue:19
Opposite regulation of Slick and Slack K+ channels by neuromodulators.
AID1346607Mouse TRPV4 (Transient Receptor Potential channels)2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives.
AID1346578Rat Kir3.4 (Inwardly rectifying potassium channels)2004Proceedings of the National Academy of Sciences of the United States of America, Jan-27, Volume: 101, Issue:4
Molecular basis for the inhibition of G protein-coupled inward rectifier K(+) channels by protein kinase C.
AID1346605Human TRPV4 (Transient Receptor Potential channels)2003British journal of pharmacology, Sep, Volume: 140, Issue:2
Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID718290Cytotoxicity against african green monkey Vero cells by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID718288Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1231848Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID718287Selectivity index, ratio of CC50 for african green monkey Vero cells to EC50 for Chikungunya virus 8992012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID1231846Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID1231849Selectivity index, CC50 for african green monkey Vero cells to EC50 for HIV1 3B2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID718289Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID1231851Selectivity index, CC50 for african green monkey Vero cells to EC50 for HIV2 ROD2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1231850Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID718286Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication.
AID1231847Selectivity index, CC50 for african green monkey Vero cells to EC50 for chikungunya virus Indian ocean strain 8992015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (30,325)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907471 (24.64)18.7374
1990's14205 (46.84)18.2507
2000's6079 (20.05)29.6817
2010's2310 (7.62)24.3611
2020's260 (0.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.69

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.69 (24.57)
Research Supply Index10.35 (2.92)
Research Growth Index4.44 (4.65)
Search Engine Demand Index46.62 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.69)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials61 (0.20%)5.53%
Trials0 (0.00%)5.53%
Reviews342 (1.10%)6.00%
Reviews0 (0.00%)6.00%
Case Studies75 (0.24%)4.05%
Case Studies0 (0.00%)4.05%
Observational4 (0.01%)0.25%
Observational0 (0.00%)0.25%
Other30,568 (98.45%)84.16%
Other16 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]