Page last updated: 2024-12-10

sphingosine

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Description

sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position. [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]

sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration. [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]

sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds. [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]

2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4. [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]

Cross-References

ID SourceID
PubMed CID5280335
CHEMBL ID67166
CHEBI ID16393
CHEBI ID26743
SCHEMBL ID1471985
SCHEMBL ID19398
MeSH IDM0020302

Synonyms (133)

Synonym
MLS002172450
trans-d-erythro-2-amino-4-octadecene-1,3-diol
(2s,3r)-(e)-2-amino-1,3-dihydroxy-4-octadecene
CHEBI:16393 ,
d-(+)-erythro-1,3-dihydroxy-2-amino-4-trans-octadecene
trans-4-sphingenine
sphingosin
(e)-d-erythro-4-octadecene-1,3-diol
c18 sphingosine
sphingosine d18:1
(4e)-sphingenine
(2s,3r,4e)-2-aminooctadec-4-ene-1,3-diol
(2s,3r,4e)-2-amino-4-octadecene-1,3-diol
(2s,3r,4e)-2-amino-3-hydroxyoctadec-4-ene-1-ol
(e)-2-amino-4-octadecan-1,3-diol
LOPAC0_001049
IDI1_033996
BIOMOLKI_000034
LMSP01010001
2s-amino-4e-octadecene-1,3r-diol
BIOMOLKI2_000042
BSPBIO_001526
smr000857107
MLS001332469
MLS001332470
(2s,3r)-sphingosine
4-trans-sphingenine
c18-sphingosine
4-octadecene-1,3-diol, 2-amino-, [r-[r*,s*-(e)]]-
d-erythro-c18-sphingosine
4-octadecene-1,3-diol, 2-amino-, (2s,3r,4e)-
d-sphingosine
erythro-4-sphingenine
d-(+)-erytho-4-trans-sphingenine
(-)-d-erythro-sphingosine
4-sphingenine
erythro-c18-sphingosine
4-octadecene-1,3-diol, 2-amino-, (e)-d-erythro- (8ci)
4-octadecene-1,3-diol, 2-amino-, (2s,3r,4e)- (9ci)
4-octadecene-1,3-diol, 2-amino-, (r-(r*,s*-(e)))
ccris 6899
SPHINGOSINE ,
sphingoid
d-erythro-sphingosine
sphing-4-enine
123-78-4
C00319
sphingenine
2-amino-4-octadecene-1,3-diol
d-sphingosine, synthetic
DB03203
NCGC00024697-03
NCGC00024697-06
2-aminooctadec-4-ene-1,3-diol
CHEBI:26743
NCGC00024697-05
(2s,3r)-2-aminooctadec-4-ene-1,3-diol
NCGC00024697-07
NCGC00024697-02
NCGC00024697-04
gtpl2452
d-erythrosphingosine
4-octadecene-1,3-diol, 2-amino-, (r-(r*,s*-(e)))-
HMS1989M08
E66DE871-3B37-406A-891B-A804BDC7ABF9
CHEMBL67166 ,
BML3-C09
BMK1-D10
HMS1361M08
HMS1791M08
(e,2s,3r)-2-aminooctadec-4-ene-1,3-diol
BMSE000850
SCHEMBL1471985
HMS2232M04
CCG-100638
MLS-0412588.0001 ,
2733-29-1
4-octadecene-1,3-diol, 2-amino-, (r*,s*-(e))-(+)-
4-octadecene-1,3-diol, 2-amino-, (r*,s*-(e))-
c18-erythro-sphingenine
dl-erythro-sphingosine
erythro-dl-sphingosine
0y6svq612q ,
unii-0y6svq612q
4-octadecene-1,3-diol, 2-amino-, (2r,3s,4e)-rel-
4-octadecene-1,3-diol, 2-amino-, (e)-dl-erythro-
unii-ngz37hre42
ngz37hre42 ,
einecs 204-651-3
erythro-sphingosine, (+/-)-
4-octadecene-1,3-diol, 2-amino-, (e)-d-erythro-
(-)-sphingosine
4-octadecene-1,3-diol, 2-amino-, (r*,s*-(e))-(+/-)-
dl-erythro-sphingosine [mi]
sphingosine [mi]
S2210
EI-155
SCHEMBL19398
d-erythro-sphingosine (synthetic)
cid_5280335
(e,2s,3r)-2-azanyloctadec-4-ene-1,3-diol
(e,2s,3r)-2-amino-4-octadecene-1,3-diol
bdbm83205
sphingosine, c18 chain
HB0239
AC-28329
AKOS024458590
HMS3650M05
HMS3402M08
(2s,3r,e)-2-amino-4-octadecene-1,3-diol
S0874
erythrosphingosine; erythro-c18-sphingosine; trans-4-sphingenine
mfcd00036751
(2s,3r)-2-amino-4-octadecene-1,3-diol
J-004983
sr-01000597656
SR-01000597656-1
d-sphingosine, >=98.0% (tlc)
AS-66175
d-sphingosine, from bovine brain, ~99% (tlc)
[r-[r*,s*-(e)]]-2-amino-4-octadecene-1,3-diol
HY-101047
CS-0020759
sphingosine (d18:1), d-erythro-sphingosine, powder
brain sphingosine, d-erythro-sphingosine (brain, porcine), powder
(2s,3r,e)-2-aminooctadec-4-ene-1,3-diol
d-erythro-spinghosine
DTXSID90861763
89164-20-5
F20671
EX-A1428
Q46298
A901185

Research Excerpts

Overview

Sphingosine is a long-chain sphingoid base that has been shown to have bactericidal activity against many pathogens. It is a signaling molecule involved in the control of cell migration, differentiation, survival and other physiological processes.

ExcerptReferenceRelevance
"Sphingosine kinase (SphK) is an enzyme that plays a crucial role in the synthesis of sphingosine-1-phosphate (S1P)."( The role of SphK/S1P/S1PR signaling pathway in bone metabolism.
Fan, F; Han, Y; Liu, Y; Luo, D; Wang, X; Xu, X; Zhu, T, 2023
)
1.63
"Sphingosine-1-phosphate is a natural metabolite that is cardioprotective, but its effects on endothelial glycocalyx damage during ischemia-reperfusion are unknown. "( The effect of sphingosine-1-phosphate on the endothelial glycocalyx during ischemia-reperfusion injury in the isolated rat heart.
Araibi, H; Gwanyanya, A; Kelly-Laubscher, R; van der Merwe, E, 2020
)
2.36
"Sphingosine is a long-chain sphingoid base that has been shown to have bactericidal activity against many pathogens, including "( Sphingosine kills bacteria by binding to cardiolipin.
Becker, KA; Edwards, MJ; Gulbins, E; Verhaegh, R, 2020
)
3.44
"Sphingosine-1-phosphate is a signaling molecule involved in the control of cell migration, differentiation, survival and other physiological processes. "( Mitochondrial sphingosine-1-phosphate lyase is essential for phosphatidylethanolamine synthesis and survival of Trypanosoma brucei.
Bütikofer, P; Dawoody Nejad, L; Hemphill, A; Rauch, M; Schneiter, R; Serricchio, M; Stumpe, M, 2020
)
2.36
"Sphingosine 1-phosphate is a bioactive sphingolipid mediator involved in various cellular functions through S1PR1‒5, expressed by keratinocytes."( Sphingosine 1-Phosphate Receptor 2 Is Central to Maintaining Epidermal Barrier Homeostasis.
Di Nardo, A; Dokoshi, T; Igawa, S; Nakatsuji, T; Ohzono, A; Pham, P; Wang, Z, 2021
)
2.79
"Sphingosine is a natural sphingolipid found in membranes of all eukaryotic cells. "( Sphingosine's role in epithelial host defense: A natural antimicrobial and novel therapeutic.
Becker, KA; Boudreau, RM; Caldwell, CC; Couch, C; Edwards, MJ; Gulbins, E; Martin, GE; Seitz, A, 2017
)
3.34
"Sphingosine-1-phosphate is a bioactive lipid mediator that promotes cell survival, proliferation, migration, angiogenesis/lymphangiogenesis, and immune responsiveness, which are all factors involved in cancer progression."( The role of sphingosine-1-phosphate in the tumor microenvironment and its clinical implications.
Nagahashi, M; Nakajima, M; Rashid, OM; Takabe, K; Wakai, T, 2017
)
1.56
"Phytosphingosine is a well-known cosmetic agent, but its anti-melanogenic activity and mechanism of action remain unclear."( Anti-melanogenic activity of phytosphingosine via the modulation of the microphthalmia-associated transcription factor signaling pathway.
Hong, JY; Jang, EJ; Jung, C; Kim, D; Kim, S; Lee, SK; Park, HJ; Shin, Y, 2017
)
1.19
"Sphingosine kinase (SphK) is a lipid enzyme that maintains cellular lipid homeostasis. "( "Dicing and Splicing" Sphingosine Kinase and Relevance to Cancer.
Haddadi, N; Lin, Y; McGowan, EM; Nassif, NT; Simpson, AM, 2017
)
2.21
"Phytosphingosine (PHS) is a sphingoid that is a key component of phytoceramides NP, AP and EOP. "( Phytosphingosine enhances moisture level in human skin barrier through stimulation of the filaggrin biosynthesis and degradation leading to NMF formation.
Cho, YH; Choi, HK; Kim, JW; Lee, EO; Park, CS, 2017
)
1.48
"Sphingosine kinase (SPHK) is an important regulator for keeping this balance."( The sphingosine kinase-1/sphingosine-1-phosphate axis in cancer: Potential target for anticancer therapy.
Chen, X; Du, G; Li, W; Liu, J; Pang, X; Ren, L; Wang, J; Zheng, X, 2019
)
1.79
"Sphingosine kinase 1 is an enzyme-regulating inflammatory response."( Preclinical evidence of sphingosine kinase 1 inhibition in alleviation of intestinal epithelial injury in polymicrobial sepsis.
Ho, J; Ugwu, FN, 2019
)
1.54
"Sphingosine 1-phosphate is a multifunctional signalling molecule, which was shown to influence several hallmarks of glomerulonephritis including mesangial cell proliferation, renal inflammation and fibrosis."( Targeting the sphingosine kinase/sphingosine 1-phosphate pathway to treat chronic inflammatory kidney diseases.
Huwiler, A; Pfeilschifter, J; Schwalm, S, 2014
)
1.48
"Sphingosine kinase is a key enzyme in sphingolipid metabolism, catalysing the conversion of sphingosine or dihydrosphingosine into sphingosine-1-phosphate or dihydrosphingosine-1-phosphate respectively. "( Sphingosine kinase A is a pleiotropic and essential enzyme for Leishmania survival and virulence.
Hsu, FF; Pawlowic, M; Xu, W; Zhang, K; Zhang, O, 2013
)
3.28
"Sphingosine kinase (SphK) is an oncogenic lipid kinase that regulates the sphingolipid metabolic pathway that has been shown to play a role in numerous hyperproliferative/inflammatory diseases. "( Importance of sphingosine kinase (SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors.
Amin, S; Plano, D; Sharma, AK, 2014
)
2.21
"Sphingosine (Sph) is a simple lipid involved in the regulation of several biological processes. "( Biophysical implications of sphingosine accumulation in membrane properties at neutral and acidic pH.
Carreira, AC; de Almeida, RF; Silva, LC; Zupancic, E, 2014
)
2.14
"Sphingosine is a major storage compound in Niemann-Pick type C disease (NP-C), although the pathological role(s) of this accumulation have not been fully characterized. "( Pathological roles of the VEGF/SphK pathway in Niemann-Pick type C neurons.
Bae, JH; Bae, JS; He, X; Hong, YR; Jin, HK; Kim, H; Lee, H; Lee, JK; Marti, HH; Okada, Y; Okino, N; Otsu, M; Park, JH; Park, MH; Schuchman, EH; Seo, EJ, 2014
)
1.85
"Sphingosine is a physiological inhibitor of protein kinase C (PKC) activity."( The ATP-Binding Cassette Transporter-2 (ABCA2) Overexpression Modulates Sphingosine Levels and Transcription of the Amyloid Precursor Protein (APP) Gene.
Davis, W, 2015
)
1.37
"Sphingosine 1-phophate is a molecule with extensive receptor expression on both immune and glial cells and is also a target of fingolimod, a drug used in relapsing remitting patients that sequesters lymphocytes within lymph nodes."( Sphingosine 1-phosphate signaling in astrocytes: Implications for progressive multiple sclerosis.
Correale, J; Farez, MF, 2016
)
2.6
"Sphingosine kinase (SphK) is an important signalling enzyme that catalyses the phosphorylation of sphingosine (Sph) to form sphingosine‑1‑phosphate (S1P). "( The role of sphingolipid signalling in diabetes‑associated pathologies (Review).
Ng, ML; Sukocheva, OA; Wadham, C, 2017
)
1.9
"The sphingosine analog FTY720 is a prodrug, and FTY720 phosphate (FTY720-P) its functional form."( Production and release of sphingosine 1-phosphate and the phosphorylated form of the immunomodulator FTY720.
Igarashi, Y; Kihara, A, 2008
)
1.13
"Sphingosine kinase (SphK) is a key enzyme in the sphingolipid metabolic pathway responsible for phosphorylating sphingosine into sphingosine-1-phosphate (S1P). "( Anti-inflammatory effects of sphingosine kinase modulation in inflammatory arthritis.
Goh, HH; Howe, HS; Irwan, AW; Lai, WQ; Leung, BP; McInnes, IB; Melendez, AJ; Valle-Oñate, R; Yu, DT, 2008
)
2.08
"Sphingosine-1-phosphate is a potent sphingolipid mediator of diverse processes important for brain tumors, including cell growth, survival, migration, invasion, and angiogenesis. "( Targeting sphingosine kinase 1 inhibits Akt signaling, induces apoptosis, and suppresses growth of human glioblastoma cells and xenografts.
Adams, JK; Allegood, JC; Almenara, JA; Dent, P; Hait, NC; Kapitonov, D; Kordula, T; Milstien, S; Mitchell, C; Spiegel, S; Zipkin, RE, 2009
)
2.2
"Phytosphingosine (PS) is a promising compound in skin formulations, considering its application in the treatment of acne and different inflammations as well as in the 'anti age' cosmetics. "( Analysis of skin penetration of phytosphingosine by fluorescence detection and influence of the thermotropic behaviour of DPPC liposomes.
Hasanovic, A; Hoeller, S; Valenta, C, 2010
)
1.15
"Sphingosine 1-phosphate is a bioactive sphingolipid that regulates crucial physiological processes."( Sphingosine 1-phosphate and sphingosine kinase are involved in a novel signaling pathway leading to acrosomal exocytosis.
Belmonte, SA; Darszon, A; De Blas, GA; Mayorga, LS; Obeid, LM; Suhaiman, L, 2010
)
2.52
"Sphingosine kinase-1 is a crucial regulator of this two-pan balance, because its produces the pro-survival and pro-angiogenic sphingosine 1-phosphate and decreases the amount of both ceramide and sphingosine, the pro-apoptotic sphingolipids."( Activation of sphingosine kinase-1 in cancer: implications for therapeutic targeting.
Ader, I; Bouquerel, P; Brizuela, L; Cuvillier, O; Malavaud, B; Mazerolles, C; Rischmann, P, 2010
)
1.44
"Sphingosine kinase (SphK) is a key enzyme in modulating the levels of sphingosine 1-phosphate (S1P) as well as an important enzyme in numerous biological responses. "( Determination of sphingosine kinase activity in biological samples by liquid chromatography-tandem mass spectrometry.
Bi, H; Huang, H; Lan, T; Le, K; Liu, Y; Xie, Z; Xu, S, 2010
)
2.14
"Sphingosine-1-phosphate is an example of such sphingolipid derivatives which has antiapoptotic effects."( Therapeutic applications of bioactive sphingolipids in hematological malignancies.
Baran, Y; Ekiz, HA, 2010
)
1.08
"Sphingosine is a bioactive molecule which is known to participate in the regulation of a number of cellular processes such as apoptosis, cell differentiation, growth, etc. "( Effect of sphingosine on domain morphology in giant vesicles.
Georgieva, R; Koumanov, K; Momchilova, A; Staneva, G; Tessier, C, 2010
)
2.21
"Sphingosine-1-phosphate functions as a growth and survival factor, acting as a ligand for a family of G protein-coupled receptors, whereas ceramide activates intrinsic and extrinsic apoptotic pathways through receptor-independent mechanisms."( Cancer treatment strategies targeting sphingolipid metabolism.
Oskouian, B; Saba, JD, 2010
)
1.08
"Sphingosine (SPH) is an important bioactive lipid involved in mediating a variety of cell functions including apoptosis. "( Protein phosphatase 1-dependent dephosphorylation of Akt is the prime signaling event in sphingosine-induced apoptosis in Jurkat cells.
Chathoth, S; Galadari, S; Hago, A; Kizhakkayil, J; Patel, M; Shahin, A; Thayyullathil, F, 2011
)
2.03
"S1P (sphingosine 1-phosphate) is a signalling molecule involved in a host of cellular and physiological functions, most notably cell survival and migration. "( Sphingosine kinase type 1 inhibition reveals rapid turnover of circulating sphingosine 1-phosphate.
Gellett, AM; Kennedy, PC; Kharel, Y; Lynch, KR; Macdonald, TL; Mathews, TP; Moyer, ML; Tomsig, JL, 2011
)
2.33
"Sphingosine 1-phosphate is a bioactive sphingolipid that regulates crucial physiological processes."( Optimized protocols to analyze sphingosine-1-phosphate signal transduction pathways during acrosomal exocytosis in human sperm.
Belmonte, SA; Suhaiman, L, 2012
)
1.39
"Sphingosine kinase is an enzyme that catalyses the phosphorylation of sphingosine to form sphingosine 1-phosphate. "( Identification of novel functional and spatial associations between sphingosine kinase 1, sphingosine 1-phosphate receptors and other signaling proteins that affect prognostic outcome in estrogen receptor-positive breast cancer.
Edwards, J; Elsberger, B; Mallon, E; Ohotski, J; Orange, C; Pyne, NJ; Pyne, S; Watson, C, 2013
)
2.07
"S1P (sphingosine 1-phosphate) is a pleiotropic lipid mediator involved in numerous cellular and physiological functions. "( Sphingosine kinase type 2 inhibition elevates circulating sphingosine 1-phosphate.
Gao, M; Gellett, AM; Kharel, Y; Lynch, KR; Raje, M; Santos, WL; Tomsig, JL, 2012
)
2.34
"Sphingosine (SPH) is a ligand for SF-1."( Acid ceramidase (ASAH1) represses steroidogenic factor 1-dependent gene transcription in H295R human adrenocortical cells by binding to the receptor.
Bandyopadhyay, S; Li, D; Lucki, NC; Merrill, AH; Sewer, MB; Wang, E, 2012
)
1.1
"Sphingosine 1-phosphate is a novel lipid mediator which exerts various actions on endothelial cells and vascular smooth muscle cells. "( Sphingosine 1-phosphate signaling in atherosclerosis and vascular biology.
Okajima, F; Tamama, K, 2002
)
3.2
"Sphingosine (Sph) is a metabolite product of ceramide that has some different biochemical properties."( Sphingosine may have cytotoxic effects via apoptosis on the growth of keloid fibroblasts.
Chang, SE; Choi, JH; Kim, KJ; Lim, YJ; Moon, KC; Ro, KH; Sung, KJ, 2004
)
2.49
"Sphingosine kinase (SPHK) is a key enzyme catalysing the formation of sphingosine 1-phosphate (SPP), a lipid messenger that is implicated in the regulation of a wide variety of important cellular events acting through intracellular, as well as extracellular, mechanisms. "( Delta-catenin/NPRAP (neural plakophilin-related armadillo repeat protein) interacts with and activates sphingosine kinase 1.
Fujita, T; Hayashi, S; Jahangeer, S; Miwa, N; Nakamura, S; Okada, T, 2004
)
1.98
"Sphingosine kinase (SPK) is a key enzyme catalyzing the formation of sphingosine-1-phosphate (S1P), a lipid messenger that is implicated in the regulation of a wide variety of important cellular events through both intracellular and extracellular mechanisms."( Sphingosine kinase activation regulates hepatocyte growth factor induced migration of endothelial cells.
Duan, HF; Jia, XX; Liu, HJ; Lu, Y; Lu, ZZ; Wang, H; Wang, LS; Wu, CT; Zhang, QW, 2004
)
2.49
"Sphingosine 1-phosphate is a bioactive sphingolipid that regulates cell growth and suppresses programmed cell death. "( The mechanism of membrane targeting of human sphingosine kinase 1.
Cho, W; Hwang, JH; Johnson, KR; Kim, JH; Obeid, LM; Park, ZY; Stahelin, RV, 2005
)
2.03
"Sphingosine kinase (SphK) is a conserved lipid kinase that catalyzes formation of important regulators of inter- and intracellular signaling, sphingosine-1 phosphate (S1P), and dihydrosphingosine 1-phosphate (dhS1P). "( Dihydrosphingosine 1-phosphate stimulates MMP1 gene expression via activation of ERK1/2-Ets1 pathway in human fibroblasts.
Bielawska, A; Bielawski, J; Bu, S; Hannun, YA; Obeid, L; Pei, H; Trojanowska, M; Yamanaka, M, 2006
)
2.23
"Sphingosine kinase is a key enzyme in modulating the levels of these lipids and is emerging as an important and regulated enzyme."( Sphingosine kinase: biochemical and cellular regulation and role in disease.
Hannun, YA; Obeid, LM; Taha, TA, 2006
)
2.5
"Sphingosine kinase (SK) is an oncogenic sphingolipid-metabolizing enzyme that catalyzes the formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) at the expense of proapoptotic ceramide. "( Antitumor activity of sphingosine kinase inhibitors.
French, KJ; Keller, SN; Smith, CD; Upson, JJ; Yun, JK; Zhuang, Y, 2006
)
2.09
"Sphingosine kinase (SphK) is a key enzyme in the synthesis of sphingosine 1-phosphate (S1P), a bioactive sphingolipid. "( A sphingosine kinase 1 mutation sensitizes the myocardium to ischemia/reperfusion injury.
Hoover, HE; Huang, Y; Jin, ZQ; Karliner, JS; Vessey, DA; Zhang, J, 2007
)
2.5
"Sphingosine kinase (SphK) is a conserved lipid kinase that catalyzes the formation of sphingosine 1-phosphate (S1P), an important lipid mediator, which regulates fundamental biological processes. "( Sphingosine kinase activity is required for myogenic differentiation of C2C12 myoblasts.
Bruni, P; Cencetti, F; Donati, C; Farnararo, M; Meacci, E; Nuti, F, 2008
)
3.23
"Sphingosine kinase (SK) is a signaling enzyme that phosphorylates sphingosine to produce sphingosine 1-phosphate. "( An assay system for measuring the acute production of sphingosine 1-phosphate in intact monolayers.
Siow, DL; Wattenberg, BW, 2007
)
2.03
"Sphingosine is a product of sphingolipid metabolism that has been linked to a protein kinase C-independent mitogenic response. "( Differential regulation of sphingomyelinase and ceramidase activities by growth factors and cytokines. Implications for cellular proliferation and differentiation.
Coroneos, E; Kester, M; Martinez, M; McKenna, S, 1995
)
1.73
"Sphingosine is a positive regulator of cell growth in Swiss 3T3 fibroblasts (Zhang, H., Buckley, N. "( Stereospecificity of sphingosine-induced intracellular calcium mobilization and cellular proliferation.
Carlson, RO; Mattie, ME; Olivera, A; Schmidt, RR; Spiegel, S; Zhang, H, 1994
)
2.05
"Sphingosine is a long-chain base which provides the back-bone of all sphingolipid molecules. "( The quantification of free sphingosine in the stratum corneum of patients with hereditary ichthyosis.
Harper, JI; Morse-Fisher, N; Paige, DG, 1993
)
2.03
"Sphingosine is a known inhibitor of protein kinase C and the involvement of this enzyme is postulated in the modulatory effects of sphingosine on intracellular calcium dynamics."( Sphingosine stimulates calcium mobilization and modulates calcium signals evoked by thapsigargin in glioma C6 cells.
Barańska, J; Chaban, V; Czarny, M; Sabała, P; Wiktorek, M, 1996
)
2.46
"Sphingosine is a potent inhibitor of a mammalian DNA primase in vitro (Simbulan et al., Biochemistry 33, 9007-9012, 1994). "( Inhibition of DNA primase by sphingosine and its analogues parallels with their growth suppression of cultured human leukemic cells.
Furuta, K; Izuta, S; Murate, T; Nakagawa, M; Simbulan, CM; Suzuki, M; Takemura, M; Tamiya-Koizumi, K; Yoshida, S, 1997
)
2.03
"Sphingosine is a noncompetitive inhibitor at the high-affinity ryanodine binding site, and it interacts with a site between Arg4475 and the carboxy terminus of the Ca(2+)-release channel."( Modulation of skeletal muscle Ca2(+)-release channel activity by sphingosine.
Aghdasi, B; Hamilton, SL; Needleman, DH; Schroepfer, GJ; Seryshev, AB, 1997
)
1.26
"Sphingosine was found to be an exogenous inhibitor of protein kinase C and of many cell functions which depend on this enzyme including cell proliferation, differentiation, and programmed death."( Functions of sphingosine in cell proliferation and death.
Alessenko, AV, 1998
)
1.39
"Sphingosine-1-phosphate is a sphingolipid metabolite involved in the regulation of cell proliferation in mammalian cells. "( The DPL1 gene is involved in mediating the response to nutrient deprivation in Saccharomyces cerevisiae.
Gottlieb, D; Heideman, W; Saba, JD, 1999
)
1.75
"Sphingosine 1-phosphate is a naturally occurring biologically active lysophospholipid. "( Sphingosine 1-phosphate induces sinus tachycardia and coronary vasoconstriction in the canine heart.
Hashimoto, K; Ozaki, Y; Sugiyama, A; Yatomi, Y, 2000
)
3.19
"Sphingosine thus appears to be a true PDK1 activator."( Sphingosine is a novel activator of 3-phosphoinositide-dependent kinase 1.
Bokoch, GM; Dawson, PE; Dutil, EM; Hemmings, BA; King, CC; Newton, AC; Zenke, FT, 2000
)
2.47
"Sphingosine is an endogenous inhibitor of protein kinase C and has an inhibitory effect on many cell functions depending on the activity of this enzyme."( The role of sphingomyelin cycle metabolites in transduction of signals of cell proliferation, differentiation and death.
Alessenko, AV, 2000
)
1.03
"Sphingosine 1-phosphate is an intermediate of sphingosine catabolism as well as a potent signaling compound. "( A high-performance liquid chromatographic method to measure sphingosine 1-phosphate and related compounds from sphingosine kinase assays and other biological samples.
Caligan, TB; Merrill, AH; Ou, J; Peters, K; Saba, J; Wang, E, 2000
)
1.99
"Sphingosine kinase (SphK) is a highly conserved lipid kinase that phosphorylates sphingosine to form sphingosine-1-phosphate (S1P). "( An oncogenic role of sphingosine kinase.
D'Andrea, RJ; Gamble, JR; Moretti, PA; Pitson, SM; Vadas, MA; Wang, L; Wattenberg, BW; Xia, P, 2000
)
2.07
"Sphingosine-1-phosphate is a potent proliferative, survival, and morphogenetic factor, acting as an extracellular ligand for the EDG family of G-protein-coupled receptors and possibly intracellularly through as yet, unidentified targets. "( Sphingosine-1-phosphate phosphatases.
Mandala, SM, 2001
)
3.2
"Sphingosine is a biologically active derivative of sphingomyelin. "( Sphingosine synergistically stimulates tumor necrosis factor alpha-induced prostaglandin E2 production in human fibroblasts.
Ballou, LR; Barker, SC; Candela, M, 1991
)
3.17
"Sphingosine is a naturally occurring long-chain amino diol with potent inhibitory activity against protein kinase C in vitro and in cell systems. "( Use of D-erythro-sphingosine as a pharmacological inhibitor of protein kinase C in human platelets.
Carroll, FI; Hannun, YA; Khan, WA; Lewin, AH; Mascarella, SW; Wyrick, CD, 1991
)
2.06
"Sphingosine was found to be a reversible inhibitor of CT with respect to the activating lipids such as phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, and fatty acid:phosphatidylcholine vesicles."( Sphingosine inhibits the activity of rat liver CTP:phosphocholine cytidylyltransferase.
Cornell, RB; Sohal, PS, 1990
)
2.44
"Sphingosine is a potent inhibitor of several calmodulin-dependent enzymes. "( Sphingosine inhibits calmodulin-dependent enzymes.
Jefferson, AB; Schulman, H, 1988
)
3.16
"Sphingosine is a potent inhibitor of [3H]phorbol dibutyrate binding and protein kinase C activity in vitro and in human platelets (Hannun, Y., Loomis, C., Merrill, A., and Bell, R. "( Sphingosine inhibition of agonist-dependent secretion and activation of human platelets implies that protein kinase C is a necessary and common event of the signal transduction pathways.
Bell, RM; Greenberg, CS; Hannun, YA, 1987
)
3.16
"Sphingosine is a competitive inhibitor of phorbol ester binding to protein kinase C (Ca2+/phospholipid-dependent enzyme) and potently inhibits phosphotransferase activity in vitro."( Regulation of the epidermal growth factor receptor phosphorylation state by sphingosine in A431 human epidermoid carcinoma cells.
Bell, RM; Davis, RJ; Faucher, M; Gironès, N; Hannun, YA, 1988
)
1.23

Effects

Sphingosine kinase (Sphk) has been shown to be activated by growth factor and survival factors, and one of its products plays an important role in the regulation of various cellular responses. The mechanism of this effect remains obscure. Sphingosinedine (SPH) has a smaller effect than psychosine (PSY)

ExcerptReferenceRelevance
"Sphingosine (SPH) has a smaller effect and treatment with psychosine (PSY) is ineffective, which suggests that phosphorylation of the 1-carbon of SPH is required for the SPC to act as a Ca2+ release agonist in synaptosomes."( Sphingolipid derivatives modulate intracellular Ca2+ in rat synaptosomes.
Calcerrada, MC; Catalán, RE; Martínez, AM; Miguel, BG, 2001
)
1.03
"Sphingosine 1-phosphate has been emerged as a crucial metabolite of sphingolipids to regulate the cell survival, vascular integrity and inflammatory cascades in ischemia reperfusion injury."( Sphingosine 1-phosphate signaling in ischemia and reperfusion injury.
Naureen, Z; Raza, Z; Saleem, U, 2020
)
2.72
"Sphingosine has been shown to prevent and eliminate bacterial infections of the respiratory tract, but it is unknown whether sphingosine can be also employed to prevent viral infections. "( Sphingosine prevents binding of SARS-CoV-2 spike to its cellular receptor ACE2.
Ahmad, SA; Becker, KA; Carpinteiro, A; Carpinteiro, E; Edwards, MJ; Fassbender, K; Gripp, B; Gulbins, A; Gulbins, E; Hoffmann, M; Keitsch, S; Patel, SH; Pöhlmann, S; Soddemann, M; Walter, S; Wilker, B; Wilson, GC, 2020
)
3.44
"Sphingosine kinase 1 has emerged as an important determinant of sphingosine-1-phosphate lung levels, which, when aberrantly high, contribute to lung fibrosis, maladaptive vascular remodeling, and allergic asthma."( Ceramide Signaling and Metabolism in Pathophysiological States of the Lung.
Berdyshev, EV; Petrache, I, 2016
)
1.16
"Sphingosine has been shown to modulate neurotransmitter release. "( Permissive role of sphingosine on calcium-dependent endocytosis in chromaffin cells.
Gandía, L; García, AG; Rosa, JM, 2010
)
2.13
"Sphingosine kinase (SphK) has emerged as an attractive target for cancer therapeutics due to its role in cell survival. "( Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors.
Bissel, P; Kharel, Y; Knott, K; Lynch, KR; Raje, MR; Santos, WL, 2012
)
2.08
"Sphingosine kinase has been shown to play dynamic roles in the responses of cells to stress, leading to modulation of cell fate through a variety of signaling pathways impinging on the processes of cell proliferation, apoptosis, autophagy and senescence."( The control of the balance between ceramide and sphingosine-1-phosphate by sphingosine kinase: oxidative stress and the seesaw of cell survival and death.
Van Brocklyn, JR; Williams, JB, 2012
)
1.36
"Sphingosine has recently been implicated in lysosomal permeabilization and is increased in the liver by TNF-alpha."( Tumor necrosis factor-alpha-associated lysosomal permeabilization is cathepsin B dependent.
Bronk, SF; Gores, GJ; Guicciardi, ME; Werneburg, NW, 2002
)
1.04
"Sphingosine 1-phosphate has emerged as a multifaceted regulator of endothelial cell function and its high affinity S1P1 receptor is one among the many shear stress regulated genes."( Fluid shear stress differentially regulates gpr3, gpr6, and gpr12 expression in human umbilical vein endothelial cells.
Ardati, A; Busch, AE; Huber, J; Kostenis, E; Uhlenbrock, K, 2003
)
1.04
"Sphingosine (Sph) has been implicated as a modulator of membrane signal transduction systems and as a regulatory element of cardiac and skeletal muscle physiology, but little information is presently available on its precise mechanism of action. "( Sphingosine kinase activity is required for sphingosine-mediated phospholipase D activation in C2C12 myoblasts.
Becciolini, L; Bruni, P; Cencetti, F; Donati, C; Meacci, E; Nuti, F, 2004
)
3.21
"Sphingosine kinase (Sphk) has been shown to be activated by growth factor and survival factors, and one of its products, sphingosine-1-phosphate, plays an important role in the regulation of various cellular responses. "( Sphingosine kinase inhibitor suppresses a Th1 polarization via the inhibition of immunostimulatory activity in murine bone marrow-derived dendritic cells.
Ahn, SC; Banno, Y; Baumruker, T; Billlich, A; Han, J; Jeong, YI; Jung, ID; Kim, YJ; Lee, CM; Lee, JS; Lee, MG; Park, WS; Park, YM, 2007
)
3.23
"Sphingosine has been shown to inhibit cell growth in many cell lines although the mechanism of this effect remains obscure. "( Stereoselectivity of induction of the retinoblastoma gene product (pRb) dephosphorylation by D-erythro-sphingosine supports a role for pRb in growth suppression by sphingosine.
Bielawska, A; Chao, R; Crane, HM; Hannun, YA; Lagu, B; Liotta, D; Merrill, AH; Pushkareva, M, 1995
)
1.95
"Sphingosine has been shown to activate protein kinases in Jurkat T cell cytosol [Pushkareva, Khan, Alessenko, Sahyoun and Hannun (1992) J. "( Regulation of sphingosine-activated protein kinases: selectivity of activation by sphingoid bases and inhibition by non-esterified fatty acids.
Bielawska, A; Hannun, YA; Liotta, D; Menaldiv, D, 1993
)
2.09
"Sphingosine (SPH) has a smaller effect and treatment with psychosine (PSY) is ineffective, which suggests that phosphorylation of the 1-carbon of SPH is required for the SPC to act as a Ca2+ release agonist in synaptosomes."( Sphingolipid derivatives modulate intracellular Ca2+ in rat synaptosomes.
Calcerrada, MC; Catalán, RE; Martínez, AM; Miguel, BG, 2001
)
1.03
"Sphingosine (SPN) has been claimed to be a negative modulator of transmembrane signaling through protein kinase C (PK-C) or some yet unidentified mechanism [for review see Y. "( Cell membrane signaling as target in cancer therapy: inhibitory effect of N,N-dimethyl and N,N,N-trimethyl sphingosine derivatives on in vitro and in vivo growth of human tumor cells in nude mice.
Endo, K; Hakomori, S; Igarashi, Y; Nisar, M; Zhou, QH, 1991
)
1.94
"Sphingosine has been shown to be a potent and specific inhibitor of protein kinase C in vitro and in cell systems including human platelets. "( Protein kinase C and platelet inhibition by D-erythro-sphingosine: comparison with N,N-dimethylsphingosine and commercial preparation.
Dobrowsky, R; el Touny, S; Hannun, YA; Khan, WA, 1990
)
1.97
"Sphingosine, which has been proposed to be a physiological inhibitor of protein kinase C, also markedly potentiates the mitogenic effect of the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA)."( Sphingosine stimulates cellular proliferation via a protein kinase C-independent pathway.
Buckley, NE; Gibson, K; Spiegel, S; Zhang, H, 1990
)
2.44
"Free sphingosine has been found in rat liver (Merrill, A."( Free sphingosine formation from endogenous substrates by a liver plasma membrane system with a divalent cation dependence and a neutral pH optimum.
Burgess, C; Hunter, R; Liotta, DC; Merrill, AH; Slife, CW; Wang, E; Wang, S, 1989
)
1.25
"Sphingosine has been reported to be a potent inhibitor of PK-C in vitro and in intact leukocytes."( Sphingosine inhibits phorbol ester-induced inflammation, ornithine decarboxylase activity, and activation of protein kinase C in mouse skin.
Elder, JT; Fisher, GJ; Gupta, AK; Nickoloff, BJ; Voorhees, JJ, 1988
)
2.44

Actions

The sphingosine-induced increase in rigidity and breakdown of the plasma membrane permeability barrier could be responsible for some of the physiological effects. Sphingosina did not cause Ca2+ entry from extracellular medium, as also shown by following Mn2+ quenching of Fura-2 fluorescence.

ExcerptReferenceRelevance
"Sphingosine is known to inhibit protein kinase C (PKC), and PKC inhibition with nanomolar concentrations of staurosporine, calphostin C, and GF109203X down-regulated surface expression of S1P(1) but not S1P(4) in transfected rat hepatoma HTC(4) cells."( Down-regulation of S1P1 receptor surface expression by protein kinase C inhibition.
Gräler, MH; Sensken, SC, 2010
)
1.08
"Sphingosine-1-phosphate promotes Dupuytren's fibroblast contractility through S1P(2), which stimulates activation of NMMII. "( Dupuytren's fibroblast contractility by sphingosine-1-phosphate is mediated through non-muscle myosin II.
Bond, J; Komatsu, I; Levin, LS; Levinson, H; Selim, A; Tomasek, JJ, 2010
)
2.07
"Sphingosine kinases (SK) catalyze the phosphorylation of proapoptotic sphingosine to the prosurvival factor sphingosine 1-phosphate (S1P), thereby promoting oncogenic processes. "( Targeting sphingosine kinase 1 in carcinoma cells decreases proliferation and survival by compromising PKC activity and cytokinesis.
Fabbro, D; Huwiler, A; Kotelevets, N; Zangemeister-Wittke, U, 2012
)
2.22
"Sphingosine did not inhibit thrombin generation when Gla-domainless factor Xa was used in prothrombinase assays, whereas sphingosine inhibited activation of Gla-domainless prothrombin by factor Xa/factor Va in the absence of phospholipids (IC(50) = 0.49 microm)."( Sphingolipids as bioactive regulators of thrombin generation.
Deguchi, H; Griffin, JH; Yegneswaran, S, 2004
)
1.04
"Phytosphingosine ceramides increase both the membrane thickness and the radius in comparison to pure DMPC ULVs."( Influence of phytosphingosine-type ceramides on the structure of DMPC membrane.
Funari, SS; Garamus, VM; Kiselev, MA; Neubert, R; Wartewig, S; Zbytovská, J, 2005
)
1.12
"Sphingosine kinases catalyze the formation of sphingosine 1-phosphate, a bioactive lipid involved in many aspects of cellular regulation, including the fundamental biological processes of cell growth and survival. "( The calmodulin-binding site of sphingosine kinase and its role in agonist-dependent translocation of sphingosine kinase 1 to the plasma membrane.
Bagley, CJ; Hewitt, NM; Moretti, PA; Pitson, SM; Sutherland, CM; Vadas, MA, 2006
)
2.06
"The sphingosine-induced increase in rigidity and breakdown of the plasma membrane permeability barrier could be responsible for some of the physiological effects of sphingosine."( Sphingosine increases the permeability of model and cell membranes.
Alonso, A; Contreras, FX; Goñi, FM; Sot, J, 2006
)
2.26
"Sphingosine did not activate phospholipase D activity significantly after 10 min."( Interaction of ceramides, sphingosine, and sphingosine 1-phosphate in regulating DNA synthesis and phospholipase D activity.
Brindley, DN; Gómez-Muñoz, A; O'Brien, L; Waggoner, DW, 1995
)
1.31
"Sphingosine did not cause Ca2+ entry from extracellular medium, as also shown by following Mn2+ quenching of Fura-2 fluorescence."( Sphingosine-induced inhibition of capacitative calcium influx in CFPAC-1 cells.
Cavazzoni, M; Orlati, S; Rugolo, M, 1996
)
2.46
"Sphingosine is known to inhibit protein kinase C."( Role of endogenous TNF-alpha and sphingosine in induced DNA synthesis in regenerating rat liver after partial hepatectomy.
Alessenko, AV; Galperin, EI; Khrenov, AV; Platonova, LV; Sakevarashvili, GR; Shingarova, LN; Shono, NI, 1999
)
1.31
"Sphingosine did not cause vasorelaxation, and oleoylethanol-amine, a ceramidase inhibitor, did not affect sphingomyelinase-induced relaxation."( Ceramide-induced vasorelaxation: An inhibitory action on protein kinase C.
Jin, JS; Johns, DG; Webb, RC; Wilde, DW, 1999
)
1.02
"Sphingosine inhibits the increase in phospholipase A2 activity and arachidonic acid release caused by A23187 over the range 5-12.5 microM."( Defining the role of protein kinase c in calcium-ionophore-(A23187)-mediated activation of phospholipase A2 in pulmonary endothelium.
Chakraborti, S; Michael, JR; Sanyal, T, 1992
)
1
"Sphingosine displays multiple biochemical and biological effects, in particular inhibition and activation of protein kinases. "( Sphingosine activation of protein kinases in Jurkat T cells. In vitro phosphorylation of endogenous protein substrates and specificity of action.
Alessenko, AV; Hannun, YA; Khan, WA; Sahyoun, N, 1992
)
3.17
"Sphingosine, assumed to inhibit protein kinase C, inhibited P43 phosphorylation and secretion in parallel."( Collagen-induced platelet activation mainly involves the protein kinase C pathway.
Grelac, F; Karniguian, A; Legrand, YJ; Levy-Toledano, S; Rendu, F, 1990
)
1
"Sphingosine did not inhibit insulin binding to rat adipocytes at concentrations up to 200 microM but decreased hGH binding to its receptors by 44% at 50 microM."( Sphingosine, an inhibitor of protein kinase C, suppresses the insulin-like effects of growth hormone in rat adipocytes.
De Meyts, P; Smal, J, 1989
)
2.44

Treatment

Treatment with sphingosine-1-phosphate (S1P) agonists confers neuroprotective effects in animal models of Parkinson's disease.

ExcerptReferenceRelevance
"Sphingosine treatment increased ceramide and phytoceramide pools without changes in dihydroceramides."( Effects of sphingoid bases on the sphingolipidome in early keratinocyte differentiation.
Farwick, M; Koehler, T; Liebisch, G; Paragh, G; Schmitz, G; Sigruener, A; Tarabin, V, 2013
)
1.11
"Sphingosine-1-phosphate treatment increased the size and number of adipocytes, and increased the expression of adipogenic transcriptional regulators."( The Role of Sphingosine-1-Phosphate in Adipogenesis of Graves' Orbitopathy.
Chae, MK; Kim, SE; Lee, EJ; Lee, JH; Yoon, JS, 2016
)
1.53
"Phytosphingosine-treated cells displayed several features of apoptosis, including increase of sub-G(1) population, DNA fragmentation, and poly(ADP-ribose) polymerase cleavage. "( Phytosphingosine induces apoptotic cell death via caspase 8 activation and Bax translocation in human cancer cells.
Bae, S; Cho, CK; Choi, JA; Choi, WI; Chung, HY; Kang, CM; Kang, JA; Kang, S; Kim, S; Kim, TH; Lee, SJ; Lee, YS; Park, MT, 2003
)
1.35
"Sphingosine treatment of Molt-4 cells, but not WERI-Rb-1 cells, resulted in the loss of the specific E2F bands produced by the interaction of E2F and its specific DNA sequence element on gel-shift assays."( Activation of a retinoblastoma-protein-dependent pathway by sphingosine.
Dbaibo, GS; Hannun, YA; Obeid, LM; Wolff, RA, 1995
)
1.25
"Sphingosine treatment also increased survival."( Ceramide can induce cell death in sensory neurons, whereas ceramide analogues and sphingosine promote survival.
Barrett, GL; Ping, SE, 1998
)
1.25
"Pretreatment with sphingosine-1-phosphate decreased infarct size in isolated hearts subjected to ischemia-reperfusion (P = .01 vs ischemia-reperfusion). "( The effect of sphingosine-1-phosphate on the endothelial glycocalyx during ischemia-reperfusion injury in the isolated rat heart.
Araibi, H; Gwanyanya, A; Kelly-Laubscher, R; van der Merwe, E, 2020
)
1.25
"Treatment with sphingosine-1-phosphate (S1P) agonists confers neuroprotective effects in animal models of Parkinson's disease (PD)."( Sphingosine-1-Phosphate, Motor Severity, and Progression in Parkinson's Disease (MARK-PD).
Böger, R; Choe, CU; Daum, G; Englisch, C; Gerloff, C; Lezius, S; Marmann, K; Niemann, L; Peine, S; Schwedhelm, E; von Lucadou, M, 2021
)
2.42
"Pretreatment with sphingosine caused significant enhancement of LVP- (10 microg/kg) induced bradycardia in polyuria rats compared with control animals (p < 0.01)."( Phospholipid mediators and MgATPase modulation causes changes in the cardiovascular effects of vasopressin in lithium carbonate-induced polyuric rats.
Keshavan, V; Shanthi, M; Tyagi, MG; Vikram, GS, 2004
)
0.65
"Pretreatment with sphingosine, an inhibitor of PKC, resulted in an amplification of initial hormone-stimulated increase in [Ca2+]i and restored the response to rechallenge."( Participation of protein kinase C in desensitization to bradykinin and to carbachol in MDCK cells.
Chase, HS; Lindeman, RP; Luo, H, 1992
)
0.61
"Treatment of sphingosine, a specific inhibitor of protein kinase C, markedly suppressed the incorporation of cystatin alpha into KHG."( Phosphorylated cystatin alpha is a natural substrate of epidermal transglutaminase for formation of skin cornified envelope.
Katunuma, N; Takahashi, M; Tezuka, T, 1992
)
0.64

Toxicity

Sphingosine-1-phosphate (S1P) is a major component of high density lipoprotein (HDL) against myocardial ischaemic-reperfusion injury. We studied the role of two powerful molecular signalling mechanisms involved in the cardioprotective effect of S1P. We also demonstrated that sphingosINE is safe to use for inhalation up to high doses, at least in mice.

ExcerptReferenceRelevance
" No evidence of adverse systemic toxicity was seen up to 20 mg/kg in either species [for rats: Cmax = 12,600 (males) or 17,133 (females) ng/ml, AUC = 3853 (males) or 4365 (females) ng x hr/ml; for dogs: Cmax = 2533 ng/ml, AUC = 2851 ng x hr/ml (no sex differences)]."( Toxicity of the protein kinase C inhibitor safingol administered alone and in combination with chemotherapeutic agents.
Bozigian, HP; Hall, RL; Harrison, SD; Kedderis, LB; Kleeman, JM; Palmer, TE; Susick, RL, 1995
)
0.29
" We examined in primary cultured hippocampal neurons whether the protein kinases PKC, PKA, CaM-II, and cGMP-dependent protein kinase modified the toxic effects of anoxia and NO."( Protein kinases modulate the sensitivity of hippocampal neurons to nitric oxide toxicity and anoxia.
Boniece, IR; Maiese, K; Skurat, K; Wagner, JA, 1993
)
0.29
"An investigation of the toxicity of fumonisin B1 (FB1), a toxic metabolite of Fusarium moniliforme, in broiler chicks was conducted."( The toxicity of purified fumonisin B1 in broiler chicks.
Fletchert, OJ; Henry, MH; Wyatt, RD, 2000
)
0.31
" The 4-HPR and safingol combination was cytotoxic in low-oxygen conditions and was minimally toxic to normal fibroblasts and bone marrow myeloid progenitor cells."( Synergistic cytotoxicity in solid tumor cell lines between N-(4-hydroxyphenyl)retinamide and modulators of ceramide metabolism.
Billups, C; Cabot, MC; Maurer, BJ; Melton, L; Reynolds, CP, 2000
)
0.31
" We previously demonstrated the adverse effect of TNF in the process of reendothelialization as well as the dependence of its effect on cell-cycle regulation."( Loss of cyclin A and G1-cell cycle arrest are a prerequisite of ceramide-induced toxicity in human arterial endothelial cells.
Axel, DI; Karsch, KR; Mayer, P; Shook, KS; Spyridopoulos, I; Viebahn, R, 2001
)
0.31
" Hepatoma cell lines, on the other hand, undergo cell division in culture and are sensitive to the toxic effects of fumonisins."( Role of proliferation in the toxicity of fumonisin B1: enhanced hepatotoxic response in the partially hepatectomized rat.
Li, W; Norred, WP; Riley, RT; Voss, KA, 2000
)
0.31
" After completion of study drug administration, the patients were monitored until day 56 by serial laboratory tests, clinical examinations, and recording of adverse events."( Pharmacodynamics, pharmacokinetics, and safety of multiple doses of FTY720 in stable renal transplant patients: a multicenter, randomized, placebo-controlled, phase I study.
Chodoff, L; Ferguson, RM; Gonwa, TA; Kahan, BD; Karlix, JL; Leichtman, AB; Mulgaonkar, S; Schmouder, RL; Skerjanec, A, 2003
)
0.32
" Compared with placebo-treated patients, FTY720 subjects did not show a major increase in adverse events or a change in renal function."( Pharmacodynamics, pharmacokinetics, and safety of multiple doses of FTY720 in stable renal transplant patients: a multicenter, randomized, placebo-controlled, phase I study.
Chodoff, L; Ferguson, RM; Gonwa, TA; Kahan, BD; Karlix, JL; Leichtman, AB; Mulgaonkar, S; Schmouder, RL; Skerjanec, A, 2003
)
0.32
" Several fumonisins have been isolated through out the years but only fumonisin B1, B2 and B3 are the ones present in naturally contaminated foods, with B1 being the most toxic between them."( Mechanism of action of sphingolipids and their metabolites in the toxicity of fumonisin B1.
Catalá, AI; González, L; Soriano, JM, 2005
)
0.33
" Retinoid-free cationic liposomes were more toxic than the other kinds (anionic and made only of PC) but were also the best delivery system for retinoic acid to induce specific cytotoxic effects on these tumor hepatoma cell lines."( Cytotoxic effect induced by retinoic acid loaded into galactosyl-sphingosine containing liposomes on human hepatoma cell lines.
Díaz, C; Gätjens-Boniche, O; Vargas, E, 2006
)
0.57
" Fumonisin B(1) (FB(1)) is the most toxic and prevalent fumonisin detected in corn and corn-based foods."( S-adenosylmethionine or 5'-methylthioadenosine are unable to prevent fumonisin B1 hepatotoxicity in mice despite increased oxidation in liver.
He, Q; Sharma, RP; Suzuki, H,
)
0.13
" The main toxic effects of these molecules have been well characterized in poultry in the case of acute exposure, but the subclinical and economic effects of chronic exposure are less known."( Chronic toxicity of fumonisins in turkeys.
Bailly, JD; Grosjean, F; Guerre, P; Métayer, JP; Skiba, F; Tardieu, D, 2007
)
0.34
" In our previous study, FB1 was confirmed to be toxic to both liver and kidneys, coupled with simultaneous elevation of sphinganine 1-phosphate."( Elevation of sphingoid base 1-phosphate as a potential contributor to hepatotoxicity in fumonisin B1-exposed mice.
Kim, DH; Lee, YM; Lee, YS; Oh, S; Yoo, HS; Yun, YP, 2007
)
0.34
"Exposure to fumonisins (FB) is known to have toxic and carcinogenic effects in different animal species, and to express toxicity in cells via the induction of oxidative stress."( Aquilegia vulgaris L. extract counteracts oxidative stress and cytotoxicity of fumonisin in rats.
Abdel-Wahhab, MA; El-Nekeety, AA; Hassan, AM; Hassan, NS; Mohamed, SR, 2010
)
0.36
" In clinical trials, fingolimod was generally safe and well tolerated."( Mechanisms of fingolimod's efficacy and adverse effects in multiple sclerosis.
Chun, J; Cohen, JA, 2011
)
0.37
"We studied the role of two powerful molecular signalling mechanisms involved in the cardioprotective effect of sphingosine-1-phosphate (S1P), a major component of high density lipoprotein (HDL) against myocardial ischaemic-reperfusion injury, namely the RISK pathway (Akt/Erk), including its downstream target FOXO-1 and, the SAFE pathway (TNF/STAT-3)."( Interplay between SAFE and RISK pathways in sphingosine-1-phosphate-induced cardioprotection.
Frias, M; Lacerda, L; Lecour, S; Opie, LH; Somers, SJ, 2012
)
0.85
"In conclusion, S1P activates both the SAFE and RISK pathways, therefore suggesting a dual protective signalling in S1P-induced cardioprotection."( Interplay between SAFE and RISK pathways in sphingosine-1-phosphate-induced cardioprotection.
Frias, M; Lacerda, L; Lecour, S; Opie, LH; Somers, SJ, 2012
)
0.64
" Their main toxic effects have been well characterized in poultry, but differences between species have been demonstrated."( Comparative effects of fumonisins on sphingolipid metabolism and toxicity in ducks and turkeys.
Auvergne, A; Bailly, JD; Benlasher, E; Geng, X; Guerre, P; Nguyen, NT; Tardieu, D, 2012
)
0.38
" Several screening studies and a first-dose observation (FDO) period are recommended due to adverse effects observed in clinical trials."( Early tolerability and safety of fingolimod in clinical practice.
Bermel, RA; Cohen, JA; Hara-Cleaver, C; Ontaneda, D; Rudick, RA, 2012
)
0.38
" Adverse events during FDO were self limited and included symptomatic bradycardia (n=3), chest tightness (n=2) and hypertension (n=1)."( Early tolerability and safety of fingolimod in clinical practice.
Bermel, RA; Cohen, JA; Hara-Cleaver, C; Ontaneda, D; Rudick, RA, 2012
)
0.38
"Fingolimod was well tolerated during FDO and adverse events were self limited."( Early tolerability and safety of fingolimod in clinical practice.
Bermel, RA; Cohen, JA; Hara-Cleaver, C; Ontaneda, D; Rudick, RA, 2012
)
0.38
" Safety and tolerability of fingolimod were evaluated by adverse events monitoring, laboratory tests, and ophthalmological and skin assessment."( Evaluation of efficacy, safety and tolerability of fingolimod in patients with the relapsing form of multiple sclerosis - 12-month observation. A preliminary report.
Maciejek, Z; Niezgodzińska-Maciejek, A; Wawrzyniak, S; Wójcik-Drączkowska, H,
)
0.13
" During fingolimod treatment there was no new relapse in any patient and no patient stopped the treatment because of any adverse event."( Evaluation of efficacy, safety and tolerability of fingolimod in patients with the relapsing form of multiple sclerosis - 12-month observation. A preliminary report.
Maciejek, Z; Niezgodzińska-Maciejek, A; Wawrzyniak, S; Wójcik-Drączkowska, H,
)
0.13
"In our study patients fingolimod was effective, safe and well tolerated independently of disease activity and previous treatment."( Evaluation of efficacy, safety and tolerability of fingolimod in patients with the relapsing form of multiple sclerosis - 12-month observation. A preliminary report.
Maciejek, Z; Niezgodzińska-Maciejek, A; Wawrzyniak, S; Wójcik-Drączkowska, H,
)
0.13
" Fingolimod 0·5 mg caused more of the following adverse events versus placebo: lymphopenia (27 [8%] patients vs 0 patients), increased alanine aminotransferase (29 [8%] vs six [2%]), herpes zoster infection (nine [3%] vs three [1%]), hypertension (32 [9%] vs 11 [3%]), first-dose bradycardia (five [1%] vs one [<0·5%]), and first-degree atrioventricular block (17 [5%] vs seven [2%])."( Safety and efficacy of fingolimod in patients with relapsing-remitting multiple sclerosis (FREEDOMS II): a double-blind, randomised, placebo-controlled, phase 3 trial.
Agius, MA; Calabresi, PA; Cappiello, L; Goodin, D; Jeffery, D; Kappos, L; Li, B; Lublin, FD; Radue, EW; Rammohan, KW; Reder, AT; Stites, T; Vollmer, T; von Rosenstiel, P, 2014
)
0.4
"2%) did not experience any adverse event (AE) following fingolimod administration."( Safety of the first dose of fingolimod for multiple sclerosis: results of an open-label clinical trial.
Brogi, D; Comi, G; Guidi, L; Laroni, A; Lugaresi, A; Mancardi, GL; Morra, VB; Pozzilli, C; Raimondi, D; Turrini, R; Uccelli, A, 2014
)
0.4
"These results, in a population who better resembled real-world clinical practice in terms of concomitant diseases and medications, are consistent with previous clinical trials and confirmed that the first dose administration of fingolimod is generally safe and well tolerated."( Safety of the first dose of fingolimod for multiple sclerosis: results of an open-label clinical trial.
Brogi, D; Comi, G; Guidi, L; Laroni, A; Lugaresi, A; Mancardi, GL; Morra, VB; Pozzilli, C; Raimondi, D; Turrini, R; Uccelli, A, 2014
)
0.4
" Frequent adverse effects include fatigue, gastrointestinal disturbance, headache and upper respiratory tract infection."( Overview and safety of fingolimod hydrochloride use in patients with multiple sclerosis.
Goldman, MD; Jones, DE; Ward, MD, 2014
)
0.4
" To preclude OSU-2S-mediated effects on these ubiquitous phosphatases in unintended cells and avoid potential adverse effects, we developed an OSU-2S-targeted delivery of immunonanoparticles (2A2-OSU-2S-ILP), that mediated selective cytotoxicity of CLL but not normal B cells through targeting receptor tyrosine kinase ROR1 expressed in leukemic but not normal B cells."( Tumor antigen ROR1 targeted drug delivery mediated selective leukemic but not normal B-cell cytotoxicity in chronic lymphocytic leukemia.
Andritsos, L; Baskar, S; Byrd, JC; Chen, CS; Chiang, CL; Flynn, J; Frissora, FW; Jones, J; Lee, LJ; Lee, RJ; Mani, R; Mao, Y; Mo, X; Muthusamy, N; Phelps, MA; Rader, C; Wang, J; Wu, Y; Yan, R; Yu, B; Yu, L; Zhao, Y, 2015
)
0.42
"The objective of this study is to evaluate the efficacy of a new mycotoxin inactivator (AdiDetox™) in reducing the toxic effects of fumonisin B1 (FB1) in the diet of rats."( Efficacy of AdiDetox™ in reducing the toxicity of fumonisin B1 in rats.
Blandon, JC; Casas, J; Denli, M; Guynot, ME; Pérez, JF; Salado, S, 2015
)
0.42
" The LD50 of long-chain bases for GE keratinocytes, GF, and DC were considerably higher than their minimal inhibitory concentrations for oral pathogens, a finding important to pursuing their future potential in treating periodontal and oral infections."( Differential cytotoxicity of long-chain bases for human oral gingival epithelial keratinocytes, oral fibroblasts, and dendritic cells.
Bates, AM; Brogden, KA; Cavanaugh, JE; Fischer, CL; Guthmiller, JM; Johnson, GK; Lanzel, EA; Mehalick, LA; Poulsen, C; Walters, KS; Wertz, PW, 2015
)
0.42
" Elevation of liver function tests (LFTs) and reduction in peripheral-blood lymphocyte counts were among the most common adverse events reported in phase II, phase III, and extension studies."( Safety and efficacy of reduced fingolimod dosage treatment.
Khoury, SJ; Sawaya, RA; Yamout, BI; Zeineddine, MM, 2015
)
0.42
" The majority of adverse events were mild and included headache, nausea, and abdominal pain."( Olipudase alfa for treatment of acid sphingomyelinase deficiency (ASMD): safety and efficacy in adults treated for 30 months.
Diaz, GA; Ji, AJ; Jouvin, MH; Lachmann, RH; Nandy, I; Puga, AC; Wasserstein, MP, 2018
)
0.48
" We also demonstrated that sphingosine is safe to use for inhalation up to high doses, at least in mice."( Clinical Development of Sphingosine as Anti-Bacterial Drug: Inhalation of Sphingosine in Mini Pigs has no Adverse Side Effects.
Becker, KA; Carpinteiro, A; Carstens, H; Dubicanac, M; Edwards, MJ; Gulbins, E; Herrmann, D; Hilken, G; Kamler, M; Keitsch, S; Kleuser, B; Kramer, M; Kühn, C; Schumacher, F; Sehl, C; Soddemann, M; Swaidan, A; Verhaegh, R; Wilker, B; Wissmann, A, 2019
)
1.12
" Here, we found that, in tryptophan-prototrophic yeast cells, exogenously added DHS is much more toxic than PHS."( Mitochondrial reactive oxygen species-mediated cytotoxicity of intracellularly accumulated dihydrosphingosine in the yeast Saccharomyces cerevisiae.
Arita, N; Sakamoto, R; Tani, M, 2020
)
0.78
"A major dose-limiting side effect of docetaxel chemotherapy is peripheral neuropathy."( Role of 1-Deoxysphingolipids in docetaxel neurotoxicity.
Becker, KA; Bieberich, E; Bielawski, J; Doolen, S; Goins, L; Gulbins, E; McQuerry, KJ; Spassieva, SD; Sure, U; Taylor, BK; Uerschels, AK, 2020
)
0.56
" These lipids are toxic to the retina and may drive the photoreceptor loss that occurs in MacTel patients."( Toxicity Screens in Human Retinal Organoids for Pharmaceutical Discovery.
Eade, K; Friedlander, M; Giles, S; Harkins-Perry, S, 2021
)
0.62
" Here, we tested whether sphingosine has any adverse effects in the respiratory tract when applied into isolated ventilated and perfused lungs."( Inhaled sphingosine has no adverse side effects in isolated ventilated and perfused pig lungs.
Carstens, H; Gulbins, E; Kalka, K; Kamler, M; Keitsch, S; Kleuser, B; Koch, A; Rauen, U; Reiner, G; Schumacher, F; Sehl, C; Soddemann, M; Verhaegh, R; Wahlers, T; Wilker, B, 2021
)
1.36
" Two toxic targets (PRKCA, FASN), three effective targets (PLA2G10, PTGES, PLA2G1B), and four effective and toxic targets (PTGS1, PTGS2, PLA2G2A, ALOX5) were obtained by metabolomics combined with network analysis and network pharmacology."( Synchronous Investigation of the Mechanism and Substance Basis of Tripterygium Glycosides Tablets on Anti-rheumatoid Arthritis and Hepatotoxicity.
Gao, Y; Ge, J; Mou, F; Qian, Q; Su, S; Wang, Q; Wang, X; Xun, G; Zhang, H, 2022
)
0.72
"Most of the toxic effects of fumonisins can be related to sphingolipid alteration, but there is little sphingolipidomic data in animals fed fumonisins in organs other than the liver."( Targeted sphingolipid analysis in chickens suggests different mechanisms of fumonisin toxicity in kidney, lung, and brain.
Guerre, P; Matard-Mann, M; Nyvall Collén, P, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
"The pharmacokinetic fate of the mycotoxin fumonisin B1 (FB1) was investigated using 4 Holstein cows."( Pilot study on the plasma pharmacokinetics of fumonisin B1 in cows following a single dose by oral gavage or intravenous administration.
Prelusky, DB; Savard, ME; Trenholm, HL, 1995
)
0.29
" Interestingly, FTY720 displays pharmacokinetic characteristics suggesting that therapeutic drug monitoring (TDM) will not be essential for clinical applications."( Update on pharmacokinetic/pharmacodynamic studies with FTY720 and sirolimus.
Kahan, BD, 2002
)
0.31
" A pharmacodynamic model was established."( Pharmacodynamics of single doses of the novel immunosuppressant FTY720 in stable renal transplant patients.
Böhler, T; Brookman, L; Brunkhorst, R; Budde, K; L Schmouder, R; Mayer, T; Nashan, B; Nedelman, J; Neumayer, HH; Skerjanec, A; W Lücker, P, 2003
)
0.32
" Pharmacokinetic measurements revealed that FTY720 displayed linear relations of doses and concentrations over a wide range, but had no effect on CsA exposure."( Pharmacodynamics, pharmacokinetics, and safety of multiple doses of FTY720 in stable renal transplant patients: a multicenter, randomized, placebo-controlled, phase I study.
Chodoff, L; Ferguson, RM; Gonwa, TA; Kahan, BD; Karlix, JL; Leichtman, AB; Mulgaonkar, S; Schmouder, RL; Skerjanec, A, 2003
)
0.32
" We have studied the pharmacodynamic effects of FTY in stable renal allograft recipients taking part in a phase I clinical trial."( Pharmacodynamics of FTY720, the first member of a new class of immune-modulating therapeutics in transplantation medicine.
Böhler, T; Budde, K; Neumayer, HH; Schumann, B; Schütz, M; Waiser, J, 2003
)
0.32
"Both the peak concentration (0."( Single-dose FTY720 pharmacokinetics, food effect, and pharmacological responses in healthy subjects.
Barilla, D; Kovarik, JM; Kraus, G; Schmouder, R; Wang, Y, 2004
)
0.32
" Washout pharmacokinetics after the last dose indicated an elimination half-life averaging 8 days."( Multiple-dose FTY720: tolerability, pharmacokinetics, and lymphocyte responses in healthy subjects.
Barilla, D; Hunt, T; Kovarik, JM; Riviere, GJ; Schmouder, R; Wang, Y, 2004
)
0.32
"To evaluate the potential for a pharmacokinetic drug interaction between the immunomodulator FTY720 and cyclosporine to support the use of this drug combination in organ transplantation."( FTY720 and cyclosporine: evaluation for a pharmacokinetic interaction.
Barilla, D; Berthier, S; Büche, M; Gottlieb, AB; Kovarik, JM; Mayer, T; Rouilly, M; Schmouder, RL; Van Saders, C; Wang, Y,
)
0.13
" Likewise for cyclosporine, FTY720 coadministration did not alter the steady-state Cmax compared with cyclosporine given alone (1452 +/- 308 vs 1376 +/- 149 ng/mL, respectively) or AUC(tau) (6385 +/- 1578 vs 6031 +/- 1051 ng."( FTY720 and cyclosporine: evaluation for a pharmacokinetic interaction.
Barilla, D; Berthier, S; Büche, M; Gottlieb, AB; Kovarik, JM; Mayer, T; Rouilly, M; Schmouder, RL; Van Saders, C; Wang, Y,
)
0.13
" A prior physiology-based pharmacokinetic model fitted the concentration-time course of FTY720 in rats."( On the prediction of the human response: a recycled mechanistic pharmacokinetic/pharmacodynamic approach.
Lowe, PJ; Meno-Tetang, GM, 2005
)
0.33
" Both noncompartmental and population methods were used to estimate pharmacokinetic estimates in the patients."( FTY720, a novel immunomodulator in de novo kidney transplant patients: pharmacokinetics and exposure-response relationship.
Budde, K; Cole, E; Hsu, CH; Neumayer, HH; Schmouder, R; Skerjanec, A; Tedesco, H, 2005
)
0.33
" Compared with healthy controls, severe hepatic-impaired subjects had a doubled area under the concentration time curve (AUC) and 50% prolonged elimination half-life but a similar peak blood concentration."( Fingolimod (FTY720) in severe hepatic impairment: pharmacokinetics and relationship to markers of liver function.
Hartmann, S; Kovarik, JM; Picard, F; Riviere, GJ; Schmidt, HH; Schmouder, RL; Voss, B; Wagner, F; Weiss, M, 2006
)
0.33
" A physiologically based pharmacokinetic model was developed to predict the concentration of FTY720 in various organs of the body."( Physiologically based pharmacokinetic modeling of FTY720 (2-amino-2[2-(-4-octylphenyl)ethyl]propane-1,3-diol hydrochloride) in rats after oral and intravenous doses.
Heining, P; Jusko, WJ; Li, H; Lowe, P; Meno-Tetang, GM; Mis, S; Pyszczynski, N, 2006
)
0.33
"The aim of the study was to determine pharmacokinetic and pharmacodynamic profiles of FTY720 in cats and identify any toxic side effects."( Oral pharmacokinetic and pharmacodynamic effects of FTY720 in cats.
Chen, YJ; Downes, S; Gregory, C; Kyles, A, 2007
)
0.34
"The pharmacokinetic (PK) and pharmacodynamic (PD) parameters of ONO-4641 in humans were estimated using preclinical data in order to provide essential information to better design future clinical studies."( The prediction of human response to ONO-4641, a sphingosine 1-phosphate receptor modulator, from preclinical data based on pharmacokinetic-pharmacodynamic modeling.
Hasegawa, C; Honda, N; Kitagawa, J; Nakade, S; Ogawa, M; Ohno, T, 2010
)
0.62
" The accurate prediction of the pharmacokinetic profile of fingolimod-P determined empirically in 2 large phase 3 trials provides external validation of the model."( Population pharmacokinetics of fingolimod phosphate in healthy participants.
David, OJ; Looby, M; Mercier, F; Schmouder, RL; Wu, K, 2012
)
0.38
" The pharmacokinetic profiles of fingolimod and fingolimod phosphate have been extensively investigated in studies in healthy volunteers, renal transplant recipients (the indication for which fingolimod was initially under clinical development, but the development was subsequently discontinued) and MS patients."( Clinical pharmacokinetics of fingolimod.
David, OJ; Kovarik, JM; Schmouder, RL, 2012
)
0.38
" The authors investigated if this pharmacodynamic effect impacts humoral and cellular immunogenicity."( Pharmacodynamic effects of steady-state fingolimod on antibody response in healthy volunteers: a 4-week, randomized, placebo-controlled, parallel-group, multiple-dose study.
Boulton, C; David, OJ; Meiser, K; Schmouder, R, 2012
)
0.38
"This article examines the characteristics of fingolimod, its pharmacokinetic properties and the efficacy and tolerability in MS."( Pharmacokinetic evaluation of fingolimod for the treatment of multiple sclerosis.
Constantinescu, CS; Tanasescu, R, 2014
)
0.4
" In this investigation, we present a semimechanistic pharmacokinetic model for the interconversion of S1PHK substrates and their respective phosphates in rats and humans with the aim of investigating whether characterization of the rate of phosphorylation in blood platelets constitutes a basis for interspecies scaling using fingolimod as a model compound."( Translational pharmacokinetic modeling of fingolimod (FTY720) as a paradigm compound subject to sphingosine kinase-mediated phosphorylation.
Danhof, M; Luttringer, O; Ploeger, BA; Snelder, N; Stanski, DR, 2014
)
0.62
" Therefore, S1P can also be potentially used as a pharmacodynamic marker to study adjuvant arthritis (AA) rats."( UHPLC-MS/MS analysis of sphingosine 1-phosphate in joint cavity dialysate and hemodialysis solution of adjuvant arthritis rats: Application to geniposide pharmacodynamic study.
Feng, L; Hong, W; Jun, F; Li, D; Ran, D; Wenyu, W; Xiang, Z; Xuejing, D; Yan, W; Zhengrong, Z, 2019
)
0.82

Compound-Compound Interactions

We explored whether TRAIL in combination with phytosphingosine could sensitize cancer cells to TRAIL. We also evaluated whether SphK1 inhibitors could be used as synergetic agents in chemotherapy.

ExcerptReferenceRelevance
"A minor part of sphingomyelins of bovine kidney and small intestine has been shown by mass spectrometry to contain phytosphinogsine in the earlier unknown combination with 2-hydroxy fatty acids."( Presence of phytosphingosine combined with 2-hydroxy fatty acids in sphingomyelins of bovine kidney and intestinal mucosa.
Breimer, ME; Karlsson, KA; Samuelsson, BE, 1975
)
0.59
" The purpose of this study was to define an effective range of FTY720 doses that could be combined with a suboptimal dose (10 mg/kg) of cyclosporin for canine kidney allograft recipients."( An immunosuppressive regimen using FTY720 combined with cyclosporin in canine kidney transplantation.
Amemiya, H; Chiba, K; Hoshino, Y; Kakefuda, T; Kataoka, H; Kawaguchi, T; Rahman, F; Suzuki, S, 1998
)
0.3
"FTY720 alone (10-5000 ng/ml) or in combination with other drugs was added to human peripheral blood lymphocytes (PBLs) undergoing stimulation in vitro with phytohemagglutinin (PHA) or OKT3 monoclonal antibody."( Immunosuppressive effects of FTY720 alone or in combination with cyclosporine and/or sirolimus.
Kahan, BD; Okamoto, M; Qu, X; Stepkowski, SM; Tejpal, N; Wang, ME; Yu, J, 1998
)
0.3
" Using a DA donor-to-LEW recipient rat combination, we assessed the efficacy of peritransplant FTY720 alone or in combination with post-transplant tacrolimus on the survival of cardiac allografts."( Effect of peritransplant FTY720 alone or in combination with post-transplant tacrolimus in a rat model of cardiac allotransplantation.
Afford, SC; Antoniou, EA; D'Silva, M; McMaster, P; Pirenne, J; Xu, M, 1998
)
0.3
" Fourteen days later, patients received the same dose of safingol in combination with a fixed dose of DOX."( A pilot clinical/pharmacological study of the protein kinase C-specific inhibitor safingol alone and in combination with doxorubicin.
Casper, ES; Kelsen, DP; Mullen, E; Saltz, L; Schwartz, GK; Spiess, T; Storniolo, AM; Venuti, R; Ward, D; Woodworth, J; Zervos, P, 1997
)
0.3
" We investigated therapy with FTY combined with tacrolimus (FK) in rat liver transplantation."( Immunosuppressive therapy using FTY720 combined with tacrolimus in rat liver transplantation.
Amemiya, H; Enosawa, S; Funeshima, N; Kitajima, M; Li, XK; Suzuki, S; Tamura, A, 2000
)
0.31
" In this study, we performed adCTLA4Ig transfection combined with FTY720 treatment in heart-grafted rats to determine if the combination could induce a mutual effect on graft survival."( Long-term graft acceptance in rat heart transplantation by CTLA4Ig gene transfection combined with FTY720 treatment.
Amemiya, H; Enosawa, S; Funeshima, N; Kita, Y; Li, XK; Nagai, H; Ogoshi, S; Ohba, M; Okuyama, T; Sasaguri, S; Suzuki, S; Zhang, H, 2001
)
0.31
"MPS in monotherapy and combined with FTY720 resulted in steep dose-response curves."( Efficacy of mycophenolate sodium as monotherapy and in combination with FTY720 in a DA-to-Lewis-rat heart-transplantation model.
Baumlin, Y; Hof, A; Hof, RP; Matsumoto, Y, 2002
)
0.31
"The use of chemical modifiers as radiosensitizers in combination with low-dose irradiation may increase the therapeutic effect on cancer by overcoming a high apoptotic threshold."( Phytosphingosine in combination with ionizing radiation enhances apoptotic cell death in radiation-resistant cancer cells through ROS-dependent and -independent AIF release.
Bae, S; Cho, CK; Choi, JA; Choi, SY; Chung, HY; Kang, CM; Kang, S; Kang, YH; Kim, MJ; Lee, JH; Lee, SJ; Lee, YS; Park, MT, 2005
)
0.84
" In conclusion, the fat-derived hormone adiponectin combined with FTY720 might be a novel combination drug therapy for prevention of small-for-size fatty liver graft injury."( Fat-derived hormone adiponectin combined with FTY720 significantly improves small-for-size fatty liver graft survival.
Fan, ST; Ho, JW; Lam, KS; Lee, TK; Li, XL; Lo, CM; Man, K; Ng, KT; Sun, CK; Xu, A; Zhao, Y, 2006
)
0.33
" We explored whether TRAIL in combination with phytosphingosine could sensitize cancer cells to TRAIL."( Phytosphingosine in combination with TRAIL sensitizes cancer cells to TRAIL through synergistic up-regulation of DR4 and DR5.
Choi, SY; Chung, HY; Jang, YJ; Kim, MJ; Lee, SJ, 2007
)
1.1
" In our mice model, FTY720 administered alone or in combination with CsA during 21 days increased skin allograft survival in a fully mismatched strain combination and did not cause significant changes in renal function."( FTY720 in combination with cyclosporine--an analysis of skin allograft survival and renal function.
Bueno, V; Burdmann, EA; Cury, PM; Silva, FR; Silva, LB, 2006
)
0.33
" In mice, FTY720 administered in combination with CsA during 21 days has prolonged skin allograft survival without causing significant renal changes."( Tacrolimus in combination with FTY720--an analysis of renal and blood parameters.
Bueno, V; Burdmann, EA; Franco, M; Gallo, AP; Silva, LB, 2006
)
0.33
"Although EVR and FTY720 monotherapy delayed the progression of CAN, their combination with CsA had no beneficial effect."( Treatment of chronic allograft nephropathy at late stages using everolimus or FTY720 in combination with cyclosporine.
Baumann, M; Heemann, U; Liu, S; Lutz, J; Roos, M; Schmaderer, C; Strobl, M, 2008
)
0.35
" We investigated whether FTY720 in combination with sirolimus (SRL) could cause renal toxicity in C57BL/6 mice when administered for 21 days."( Sirolimus in combination with FTY720: analysis of urinary and serum parameters.
Bueno, V; Cordeiro, JA; de Franco, MF; Lopes, CT; Pletiskaitz, TM, 2010
)
0.36
" We conducted a phase I trial of safingol (S) alone and in combination with cisplatin (C)."( A phase I clinical trial of safingol in combination with cisplatin in advanced solid tumors.
Cane, LM; Carvajal, RD; Dickson, MA; Gonen, M; Merrill, AH; Schwartz, GK, 2011
)
0.37
"Safingol, the first putative SphK inhibitor to enter clinical trials, can be safely administered in combination with cisplatin."( A phase I clinical trial of safingol in combination with cisplatin in advanced solid tumors.
Cane, LM; Carvajal, RD; Dickson, MA; Gonen, M; Merrill, AH; Schwartz, GK, 2011
)
0.37
"FTY720 (fingolimod), a novel immunomodulator, has demonstrated potential for prevention of acute rejection in combination with cyclosporine."( FTY720 combined with tacrolimus in de novo renal transplantation: 1-year, multicenter, open-label randomized study.
Abramowicz, D; Hoitsma, AJ; Proot, P; Vanrenterghem, Y; Woodle, ES, 2011
)
0.37
"FTY720 combined with tacrolimus and steroids did not show a significant therapeutic advantage over MMF for the prevention of acute rejection in de novo renal transplant recipients."( FTY720 combined with tacrolimus in de novo renal transplantation: 1-year, multicenter, open-label randomized study.
Abramowicz, D; Hoitsma, AJ; Proot, P; Vanrenterghem, Y; Woodle, ES, 2011
)
0.37
" To assess whether the efficacy of a combined oral contraceptive (OC) could be compromised during fingolimod therapy, a steady-state, drug-drug interaction study of fingolimod with ethinylestradiol/levonorgestrel was performed in healthy female volunteers."( Pharmacokinetics of fingolimod (FTY720) and a combined oral contraceptive coadministered in healthy women: drug-drug interaction study results.
David, OJ; den Daas, I; Emotte, C; Jakab, A; Meiser, K; Ocwieja, M; Schmouder, R; Wemer, J, 2012
)
0.38
"To study the effect of the sphingosine kinase 1 (SphK1) inhibitor N,N-dimethylsphingosine (DMS) in combination with chemotherapeutic drugs (DDP, 5-Fu, MMC) on the proliferation of gastric cancer cells (SGC7901) in vitro, and to evaluate whether SphK1 inhibitors could be used as synergetic agents in chemotherapy."( [Antitumor effect of sphingosine kinase 1 inhibitor in combination with chemotherapy on SGC7901 gastric cancer cells in vitro].
Hu, CY; Lan, KH; Lu, Q; Tang, W; Wang, SF; Yin, GJ, 2012
)
0.99
" When 1 micromol/L DMS was used in combination with 5-Fu (1, 5, and 25 microg/ml) for 24 h, the growth inhibition rates of the cancer cells were (16."( [Antitumor effect of sphingosine kinase 1 inhibitor in combination with chemotherapy on SGC7901 gastric cancer cells in vitro].
Hu, CY; Lan, KH; Lu, Q; Tang, W; Wang, SF; Yin, GJ, 2012
)
0.7
"DMS can suppress the proliferation of SGC7901 cells in vitro, and there are evident synergetic effects when it is used in combination with chemotherapeutic drugs."( [Antitumor effect of sphingosine kinase 1 inhibitor in combination with chemotherapy on SGC7901 gastric cancer cells in vitro].
Hu, CY; Lan, KH; Lu, Q; Tang, W; Wang, SF; Yin, GJ, 2012
)
0.7
"The therapeutic efficacy of the novel immunomodulator FTY720 (Fingolimod), alone and in combination with betamethasone ointment, was examined in the NC/Nga mouse model of spontaneous steroid-resistant dermatitis."( Therapeutic approach to steroid-resistant dermatitis using novel immunomodulator FTY720 (Fingolimod) in combination with betamethasone ointment in NC/Nga mice.
Fujita, T; Inoue, M; Iwatsuki, R; Kohno, T; Tsuji, T; Yoshida, Y, 2012
)
0.38
" We investigated the therapeutic efficacy of the novel immunomodulator FTY720 (Fingolimod), alone and in combination with betamethasone valerate ointment, in the NC/Nga mouse model of mite-induced intractable dermatitis."( [Therapeutic approach to mite-induced intractable dermatitis using novel immunomodulator FTY720 (fingolimod) in combination with betamethasone ointment in NC/Nga mice].
Fujita, T; Kohno, T; Tsuji, T; Yoshida, Y, 2012
)
0.38
"The therapeutic capacity of an antibody directed against the T cell receptor (anti-TCR) of the TCR/CD3 complex alone or in combination with fingolimod (FTY720) to reverse the diabetic metabolic state through suppression of autoimmunity and stimulation of β cell regeneration was analyzed in the LEW."( Anti-TCR therapy combined with fingolimod for reversal of diabetic hyperglycemia by β cell regeneration in the LEW.1AR1-iddm rat model of type 1 diabetes.
Akin, M; Arndt, T; Hedrich, HJ; Jörns, A; Lenzen, S; Terbish, T; Wedekind, D; Zu Vilsendorf, AM, 2014
)
0.4
" In the present work, TMZ was combined with a specific SKI, and the cytotoxic effect of each drug alone or in combination was tested on GBM cell lines."( A sphingosine kinase inhibitor combined with temozolomide induces glioblastoma cell death through accumulation of dihydrosphingosine and dihydroceramide, endoplasmic reticulum stress and autophagy.
Choi, J; Kopp-Schneider, A; Noack, J; Régnier-Vigouroux, A; Richter, K, 2014
)
1.12

Bioavailability

ExcerptReferenceRelevance
" Following oral administration of the toxin, no FB1 or known metabolites could be found in the plasma, indicating no or very limited bioavailability in ruminants."( Pilot study on the plasma pharmacokinetics of fumonisin B1 in cows following a single dose by oral gavage or intravenous administration.
Prelusky, DB; Savard, ME; Trenholm, HL, 1995
)
0.29
" 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
" Cholestyramine was tested in vivo to evaluate its capacity to reduce the bioavailability of fumonisins (FBs) in rats fed diet contaminated with toxigenic Fusarium verticillioides culture material."( In vitro and in vivo studies to assess the effectiveness of cholestyramine as a binding agent for fumonisins.
Avantaggiato, G; Chulze, S; Solfrizzo, M; Torres, A; Visconti, A, 2001
)
0.31
"53 l/h/kg, and bioavailability of about 38%."( Pharmacokinetics and cell trafficking dynamics of 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (FTY720) in cynomolgus monkeys after single oral and intravenous doses.
Arima, N; Chiba, K; Heining, P; Jusko, WJ; Li, H; Meno-Tetang, GM, 2002
)
0.31
" Furthermore, it displays high oral bioavailability and a low interindividual coefficient of variation."( FTY720: A new kid on the block for transplant immunosuppression.
Aki, FT; Kahan, BD, 2003
)
0.32
" Isomers of 4,8-sphingadienine degraded from dietary plant cerebrosides appear to be poorly absorbed from the digestive tract."( Digestion of maize sphingolipids in rats and uptake of sphingadienine by Caco-2 cells.
Kinoshita, M; Nagata, J; Ohnishi, M; Saito, M; Sugawara, T, 2003
)
0.32
" From a clinical perspective, the present study identifies new potential therapeutic targets for the treatment of vascular-based, "stroke-like" inner ear pathologies: the enzymes responsible for S1P bioavailability and the S1P receptors."( Sphingosine-1-phosphate modulates spiral modiolar artery tone: A potential role in vascular-based inner ear pathologies?
Arnold, W; Bolz, SS; Lidington, D; Oestreicher, E; Pohl, U; Scherer, EQ, 2006
)
1.78
" However, due to the low bioavailability of fumonisin, these samples pose a variety of analytical challenges and also still require validation as biomarkers."( Biomarkers of exposure to fumonisin mycotoxins: a review.
Sewram, V; Shephard, GS; Van Der Westhuizen, L, 2007
)
0.34
"Fingolimod (FTY720) is a first-in-class orally bioavailable compound that has shown efficacy in advanced clinical trials for the treatment of multiple sclerosis (MS)."( Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis.
Chun, J; Hartung, HP,
)
0.13
" This review focuses on the role S1P plays in endothelial function, its receptors and signalling pathways, and the role its major carrier high-density lipoproteins (HDL) play in its bioavailability and transport."( Endothelial functions of sphingosine-1-phosphate.
Levkau, B; Lucke, S, 2010
)
0.66
" This protection might be mediated by so-called 'inside-out' signalling by S1P, as LNCaP-AI cells exhibit increased expression of S1P(2/3) receptors and reduced lipid phosphate phosphatase expression (compared with androgen-sensitive LNCaP cells) thereby potentially increasing the bioavailability of S1P at S1P(2/3) receptors."( FTY720 and (S)-FTY720 vinylphosphonate inhibit sphingosine kinase 1 and promote its proteasomal degradation in human pulmonary artery smooth muscle, breast cancer and androgen-independent prostate cancer cells.
Bittman, R; Lim, KG; Long, J; Loveridge, C; Pitson, SM; Pyne, NJ; Pyne, S; Tigyi, G; Tonelli, F, 2010
)
0.62
" Thus, Enigmol represents a novel category of sphingoid base analogue that is orally bioavailable and has the potential to be effective against multiple types of cancer."( Enigmol: a novel sphingolipid analogue with anticancer activity against cancer cell lines and in vivo models for intestinal and prostate cancer.
Allegood, JC; Bushnev, A; Dillehay, DL; Liotta, DC; Mays, SG; Merrill, AH; Peng, Q; Pruett, ST; Ramaraju, H; Sullards, MC; Symolon, H, 2011
)
0.37
" The fingolimod-P concentration-time course after either single or multiple doses of fingolimod was described by a 2-compartment model with first-order apparent formation and elimination, lag time in the apparent formation, and dose-dependent relative bioavailability and apparent central volume of distribution."( Population pharmacokinetics of fingolimod phosphate in healthy participants.
David, OJ; Looby, M; Mercier, F; Schmouder, RL; Wu, K, 2012
)
0.38
" Results from these studies have demonstrated that fingolimod is efficiently absorbed, with an oral bioavailability of >90%, and its absorption is unaffected by dietary intake, therefore it can be taken without regard to meals."( Clinical pharmacokinetics of fingolimod.
David, OJ; Kovarik, JM; Schmouder, RL, 2012
)
0.38
" It does not appear that the various formulations differ significantly in terms of bioavailability or efficacy in adults."( First-line disease-modifying therapies in paediatric multiple sclerosis: a comprehensive overview.
Johnston, J; So, TY, 2012
)
0.38
" Inhibition of 1) S1P formation with SK-I, a sphingosine kinase inhibitor, 2) S1P bioavailability with the S1P blocking antibody Sphingomab, LT1002 (but not its negative control, LT1017) or 3) S1P actions through S1PR(1) with the selective S1PR(1) antagonist, W146 (but not its inactive enantiomer, W140) blocked thermal hyperalgesia and infiltration of neutrophils."( Sphingosine 1-phosphate mediates hyperalgesia via a neutrophil-dependent mechanism.
Chen, Z; Cuzzocrea, S; Esposito, E; Finley, A; Sabbadini, R; Salvemini, D, 2013
)
2.09
" Most notably, fingolimod (FTY720, Gilenya, Novartis), an S1P receptor modulator, became the first FDA-approved medicine as an orally bioavailable drug for treating relapsing forms of multiple sclerosis."( Lysophospholipid receptors in drug discovery.
Chun, J; Kihara, Y; Mizuno, H, 2015
)
0.42
" These results indicate that 4,8-sphingadienine that originates from the glucosylceramide of higher plants is poorly absorbed in the intestine because of efflux by P-glycoprotein and can be incorporated into a ceramide moiety, at least in part, in intestinal endothelial cells."( Selective Absorption of Dietary Sphingoid Bases from the Intestine via Efflux by P-Glycoprotein in Rats.
Aida, K; Fujii, A; Hirata, T; Manabe, Y; Sugawara, T; Tsuduki, T, 2017
)
0.46
" Therefore, in the present review, based on available literatures we highlight the present knowledge on the production and bioavailability of these molecules, the mechanism of their regulation of hypertension, and patho-physiological role in malaria."( Malaria link of hypertension: a hidden syndicate of angiotensin II, bradykinin and sphingosine 1-phosphate.
Dhangadamajhi, G; Singh, S, 2021
)
0.85
" Jaspine B has been shown to inhibit sphingomyelin synthase, which synthesizes sphingomyelin from ceramide, a critical signal transducer; however, jaspine B's low bioavailability limits its application as a promising treatment option."( Formulation, Characterization, and In Vitro/In Vivo Efficacy Studies of a Novel Liposomal Drug Delivery System of Amphiphilic Jaspine B for Treatment of Synovial Sarcoma.
Aghazadeh-Habashi, A; Barrott, JJ; Khajeh Pour, S; Mateen, S; Pashikanti, S, 2022
)
0.72

Dosage Studied

Spingosine was dosed to the Simulator of the Human Intestinal Microbial Ecosystem (SHIME) for a period of 11 days. The dose-response for calcium release induced by sphingosine-1-phosphate correlated closely with the concentration required for stimulation of DNA synthesis.

ExcerptRelevanceReference
" 25-Hydroxycholesterol dose-response curves for activation of sphingomyelin synthesis, suppression of sterol-regulated transcription, and activation of cholesteryl ester synthesis were also similar."( 25-Hydroxycholesterol stimulates sphingomyelin synthesis in Chinese hamster ovary cells.
Ridgway, ND, 1995
)
0.29
" Sph-1-P induced intracellular Ca2+ mobilization and the dose-response for Ca2+ release correlated closely with the concentration required for induction of shape change."( Sphingosine-1-phosphate: a platelet-activating sphingolipid released from agonist-stimulated human platelets.
Hakomori, S; Igarashi, Y; Ruan, F; Yatomi, Y, 1995
)
1.73
" 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
)
1.98
" In this study, two sphingosine-activated protein kinases were distinguished by their substrate specificity, their dose-response to sphingosine and the specificity of their activation by sphingosine and dihydrosphingosine stereoisomers."( Regulation of sphingosine-activated protein kinases: selectivity of activation by sphingoid bases and inhibition by non-esterified fatty acids.
Bielawska, A; Hannun, YA; Liotta, D; Menaldiv, D, 1993
)
0.97
"20 mg kg-1), the plasma Sa/So ratio was increased marginally in the one dosed cow, due essentially to a transient increase in Sa concentrations, which rose by approximately 60-65% over average predose levels; So levels remained relatively constant."( Pilot study on the plasma pharmacokinetics of fumonisin B1 in cows following a single dose by oral gavage or intravenous administration.
Prelusky, DB; Savard, ME; Trenholm, HL, 1995
)
0.29
" Treatment of the tumour cells with neutral sphingomyelinase drastically reduced the amount of wild-type p53 fibrosarcoma cell proliferation over 72 h in a clear dose-response (0."( Ceramide triggers p53-dependent apoptosis in genetically defined fibrosarcoma tumour cells.
Aalame, N; Bodis, S; Glanzmann, C; Pruschy, M; Resch, H; Shi, YQ, 1999
)
0.3
" Identical dose-response curves are obtained for the Ca2+ release stimulated by cross-linking FcgammaRIIA, implicating these two enzymes in a common signaling pathway."( Convergence of Fc gamma receptor IIA and Fc gamma receptor IIIB signaling pathways in human neutrophils.
Chuang, FY; Sassaroli, M; Unkeless, JC, 2000
)
0.31
"This is the first report of sphinganine (Sa) and sphingosine (So) levels determined in serum and urine of vervet monkeys (Cercopithecus aethiops) dosed with pure fumonisin B(1) (FB(1))."( The effect of a single gavage dose of fumonisin B(1) on the sphinganine and sphingosine levels in vervet monkeys.
Shephard, GS; van der Westhuizen, L; van Schalkwyk, DJ,
)
0.62
" in the range of the steep part of its dose-response relationship."( The peripheral lymphocyte count predicts graft survival in DA to Lewis heterotopic heart transplantation treated with FTY720 and SDZ RAD.
Baumlin, Y; Hof, A; Hof, RP; Nikolova, Z, 2000
)
0.31
" In this study the disruption in sphinganine (Sa) and sphingosine (So) levels in plasma and urine was measured in vervet monkeys (Cercopithecus aethiops) dosed with repeated gavages of 1mg fumonisin B1 (FB1)/kg body weight three times/week continuously over a 51-day period."( The effect of repeated gavage doses of fumonisin B1 on the sphinganine and sphingosine levels in vervet monkeys.
Shephard, GS; van der Westhuizen, L; van Schalkwyk, DJ, 2001
)
0.79
" We therefore examined whether the same dosage schedule of fumonisin B(1) produced a similar effect in calves."( Fumonisin B(1) increases serum sphinganine concentration but does not alter serum sphingosine concentration or induce cardiovascular changes in milk-fed calves.
Constable, PD; Eppley, RM; Haschek, WM; Mathur, S; Morin, DE; Smith, GW; Tranquilli, WJ; Tumbleson, ME, 2001
)
0.54
" On the day before transplantation we administered FTY720 orally to some of these animals at a dosage of 5 mg/kg and again on the day of transplantation."( Long-term graft acceptance in rat heart transplantation by CTLA4Ig gene transfection combined with FTY720 treatment.
Amemiya, H; Enosawa, S; Funeshima, N; Kita, Y; Li, XK; Nagai, H; Ogoshi, S; Ohba, M; Okuyama, T; Sasaguri, S; Suzuki, S; Zhang, H, 2001
)
0.31
" Drug efficacy and potency was calculated based on dose-response curves of the drug-mediated decrease in CD4(+)/CD8alpha(+)/CD25(+) cells."( Coexpression of CD4 and CD8alpha on rat T-cells in whole blood: a sensitive marker for monitoring T-cell immunosuppressive drugs.
Diaz-Romero, J; Vogt, G; Weckbecker, G, 2001
)
0.31
" S1P did not affect PDGF-stimulated tyrosine phosphorylation of PDGF-beta receptor, but strongly inhibited PDGF-induced Rac activation, with a dose-response relationship similar to that for inhibition of PDGF-elicited chemotaxis."( Sphingosine-1-phosphate, a platelet-derived lysophospholipid mediator, negatively regulates cellular Rac activity and cell migration in vascular smooth muscle cells.
Matsui, O; Okamoto, H; Ryu, Y; Sakurada, S; Sugimoto, N; Takuwa, N; Takuwa, Y; Usui, S, 2002
)
1.76
" Tumor growth was markedly suppressed at a dosage of 5 mg/kg or more without notable side effects."( Marked prevention of tumor growth and metastasis by a novel immunosuppressive agent, FTY720, in mouse breast cancer models.
Azuma, H; Fukui, R; Hoshiga, M; Ichimaru, N; Ishihara, T; Itoh, Y; Katsuoka, Y; Morimoto, J; Nonomura, N; Okuyama, A; Otsuki, Y; Suzuki, S; Takahara, S; Wang, JD, 2002
)
0.31
" The lymphocyte count returned to baseline within 72 h in all dosing cohorts except the highest."( First human trial of FTY720, a novel immunomodulator, in stable renal transplant patients.
Brunkhorst, R; Budde, K; Choudhury, S; Kraus, G; Lücker, PW; Mayer, T; Nashan, B; Neumayer, HH; Schmouder, RL; Skerjanec, A, 2002
)
0.31
" However, comparison with theoretical additive dose-response curves showed additive rather than synergistic effects for both PKC inhibitors."( Antitumor activity of protein kinase C inhibitors and cisplatin in human head and neck squamous cell carcinoma lines.
Balló, H; Balz, V; Bier, H; Gerharz, CD; Grund, A; Hafner, D; Hauser, U; Hoffmann, TK; Leenen, K, 2002
)
0.31
" GCSF at a dosage of 30 to 100 ng/mL, a concentration range that primes superoxide release, stimulated a 60% to 100% increase in gelatinase release from tertiary granules but did not stimulate lactoferrin release from secondary granules."( Granulocyte colony-stimulating factor primes NADPH oxidase in neutrophils through translocation of cytochrome b(558) by gelatinase-granule release.
Boxer, LA; Hinkovska-Galcheva, V; Mansfield, PJ; Shayman, JA, 2002
)
0.31
"FTY720 is a novel immunomodulator that may provide an opportunity for a reduction in calcineurin inhibitor dosage in transplant recipients with renal/hepatic side effects."( Effects of immunosuppressant FTY720 on renal and hepatic hemodynamics in the rat.
Mabuchi, A; Tawadrous, MN; Wheatley, AM; Zimmermann, A, 2002
)
0.31
" Renal function and renal tubular parameters were examined in animals that received repeat high dosage of FTY720."( Effects of immunosuppressant FTY720 on renal and hepatic hemodynamics in the rat.
Mabuchi, A; Tawadrous, MN; Wheatley, AM; Zimmermann, A, 2002
)
0.31
" FTY720 at the same repeat oral dosage was, nevertheless, associated with a significantly lower 24 h sodium excretion and a significantly lower fractional excretion of sodium compared with those in control animals (223."( Effects of immunosuppressant FTY720 on renal and hepatic hemodynamics in the rat.
Mabuchi, A; Tawadrous, MN; Wheatley, AM; Zimmermann, A, 2002
)
0.31
"MPS in monotherapy and combined with FTY720 resulted in steep dose-response curves."( Efficacy of mycophenolate sodium as monotherapy and in combination with FTY720 in a DA-to-Lewis-rat heart-transplantation model.
Baumlin, Y; Hof, A; Hof, RP; Matsumoto, Y, 2002
)
0.31
" Rats were dosed intraperitoneally with fumonisin B1 (FB1) 24 h after sham operation or partial hepatectomy (PH) and were killed 24 h later."( Role of proliferation in the toxicity of fumonisin B1: enhanced hepatotoxic response in the partially hepatectomized rat.
Li, W; Norred, WP; Riley, RT; Voss, KA, 2000
)
0.31
" The lymphocyte count returned to baseline within 72 h in all dosing cohorts except the highest."( Pharmacodynamics of single doses of the novel immunosuppressant FTY720 in stable renal transplant patients.
Böhler, T; Brookman, L; Brunkhorst, R; Budde, K; L Schmouder, R; Mayer, T; Nashan, B; Nedelman, J; Neumayer, HH; Skerjanec, A; W Lücker, P, 2003
)
0.32
" To date, phase I single and multiple dosing studies conducted in stable renal transplant patients have revealed a favorable efficacy and tolerability profile."( FTY720 immunomodulation: optimism for improved transplant regimens.
Ferguson, R, 2004
)
0.32
" In addition, we found that LPA has no effect on neutrophil chemotaxis; however, it has stimulatory effects on neutrophil respiratory burst in a dose-response manner."( Lysophosphatidic acid triggers calcium entry through a non-store-operated pathway in human neutrophils.
Hauser, CJ; Itagaki, K; Kannan, KB, 2005
)
0.33
" Dose-response of intraventricular injection of liposomal NGF showed significant reduction in infarct volume at the dose of 5 and 10 microg/rat of NGF."( Treatment of focal cerebral ischemia with liposomal nerve growth factor.
Chen, WY; Chern, CM; Hsu, LC; Hu, HH; Huang, KJ; Law, SL; Luk, YO; Wong, WJ,
)
0.13
" To assess activity under complex intestinal conditions, sphingosine was dosed to the Simulator of the Human Intestinal Microbial Ecosystem (SHIME) for a period of 11 days."( Characterization of the bactericidal effect of dietary sphingosine and its activity under intestinal conditions.
Bolca, S; Possemiers, S; Van Camp, J; Verstraete, W, 2005
)
0.82
" Thus, the dose-response curves of the proton-induced actions were shifted to the right in the presence of SPC regardless of stereoisoform."( Sphingosylphosphorylcholine antagonizes proton-sensing ovarian cancer G-protein-coupled receptor 1 (OGR1)-mediated inositol phosphate production and cAMP accumulation.
Damirin, A; Hashimoto, K; Komachi, M; Kon, J; Mogi, C; Okajima, F; Sato, K; Tobo, M; Tomura, H; Wang, JQ, 2005
)
0.33
" After direct dosage of FTY720 phosphate, lymphopenia is only transient in this strain, indicating that SPHK2 is constantly required to maintain FTY720 phosphate levels in vivo."( Sphingosine kinase type 2 is essential for lymphopenia induced by the immunomodulatory drug FTY720.
Baumruker, T; Billich, A; Bornancin, F; Kinzel, B; Mechtcheriakova, D; Müller, M; Reuschel, R; Urtz, N; Zemann, B, 2006
)
1.78
" The latter group suffered approximately 30% mortality, which increased to approximately 75% at dosage of 30 mg/kg KA, compared with 10-14% for the other two genotypes at the latter dosage."( Enhanced susceptibility to kainate-induced seizures, neuronal apoptosis, and death in mice lacking gangliotetraose gangliosides: protection with LIGA 20, a membrane-permeant analog of GM1.
Ledeen, RW; Lu, ZH; Meyenhofer, MF; Wang, J; Wang, Y; Wu, G; Xie, X, 2005
)
0.33
" FTY-720 significantly decreased plasma creatinine in a dose-response manner with a maximal reduction of approximately 73 and approximately 69% with doses of 240 and 48 microg/kg, respectively."( Selective sphingosine 1-phosphate 1 receptor activation reduces ischemia-reperfusion injury in mouse kidney.
Awad, AS; Foss, FW; Huang, L; Li, L; Lynch, KR; Macdonald, TL; Okusa, MD; Ye, H, 2006
)
0.74
" The model characterized well FTY720 disposition for this extensive dosing and tissue collection study in the rat."( Physiologically based pharmacokinetic modeling of FTY720 (2-amino-2[2-(-4-octylphenyl)ethyl]propane-1,3-diol hydrochloride) in rats after oral and intravenous doses.
Heining, P; Jusko, WJ; Li, H; Lowe, P; Meno-Tetang, GM; Mis, S; Pyszczynski, N, 2006
)
0.33
" FTY720 was administered by intraperitoneal injection starting at 10 days after tumor cell injection at a dosage of 5 mg/kg/day."( Marked suppression of tumor growth by FTY720 in a rat liver tumor model: the significance of down-regulation of cell survival Akt pathway.
Fan, ST; Ho, JW; Lee, TK; Lo, CM; Man, K; Ng, KT; Poon, RT; Sun, CK; Zhao, Y, 2007
)
0.34
" Cytotoxicity of deferoxamine for neuroblastoma cell lines measured by the DIMSCAN assay achieved dose-response curves similar to data obtained by manual trypan blue counts or colony formation in soft agar but with a wider dynamic range."( A fluorescence microplate cytotoxicity assay with a 4-log dynamic range that identifies synergistic drug combinations.
Frgala, T; Kalous, O; Proffitt, RT; Reynolds, CP, 2007
)
0.34
"03 mg/kg was efficacious, but limiting the dosing period failed to prevent EAE despite a significant decrease in blood lymphocytes."( Brain penetration of the oral immunomodulatory drug FTY720 and its phosphorylation in the central nervous system during experimental autoimmune encephalomyelitis: consequences for mode of action in multiple sclerosis.
Balatoni, B; Beerli, C; Billich, A; Foster, CA; Hiestand, PC; Howard, LM; Persohn, E; Reuschel, R; Schwartz, M; Schweitzer, A, 2007
)
0.34
" This ligand-induced, receptor-mediated cell motility follows a typical bell-shaped dose-response curve, that is, stimulation with low concentrations of S1P enhances cell motility, whereas excess ligand stimulation does not enhance it."( Attenuation of cell motility observed with high doses of sphingosine 1-phosphate or phosphorylated FTY720 involves RGS2 through its interactions with the receptor S1P.
Igarashi, Y; Kohno, T, 2008
)
0.59
"Therapeutic dosing of FTY720 reduces naïve T cells and TCM, but not TEM, in blood, without affecting T cell function."( FTY720 therapy exerts differential effects on T cell subsets in multiple sclerosis.
Antel, J; Bar-Or, A; Brinkmann, V; Goebels, N; Kappos, L; Kristofic, C; Kuhle, J; Lindberg, RL; Mehling, M; Vedrine, C, 2008
)
0.35
" Subsequently, simulations were utilized to design a multiple ascending dose study with adaptive dosing regimens that would meet targeted pharmacodynamic (PD) response thresholds (eg, minimum 40% reduction in lymphocytes) while maintaining CD4 counts above a reasonable safety threshold."( Use of an exposure-response model to aid early drug development of an oral sphingosine 1-phosphate receptor modulator.
Carrothers, TJ; Inaba, S; Moberly, JB; Rohatagi, S; Shimozato, T; Truitt, KE; Zahir, H, 2009
)
0.58
" A recent provocative report indicated that low dosage of the sphingosine analog FTY720 caused lymphopenia in mice persistently infected with lymphocytic choriomeningitis virus (LCMV)-clone 13 (Cl 13) and induced viral clearance within 30 days post-treatment (Premenko-Lanier et al."( Treatment with a sphingosine analog does not alter the outcome of a persistent virus infection.
Marsolais, D; Oldstone, MB; Rosen, H; Walsh, KB; Welch, MJ, 2010
)
0.94
" When cells were treated with 1 microM S1P simultaneously with OGD and recovery, cell viability increases in a dose-response manner."( Involvement of mitochondria on neuroprotective effect of sphingosine-1-phosphate in cell death in an in vitro model of brain ischemia.
Agudo-López, A; Fernández, I; Martínez, AM; Miguel, BG, 2010
)
0.61
" Western blots with anti-PKCalpha exhibited redistribution to membranes in a biphasic dose-response curve: slightly stimulated at the lowest dose, maximal at 300pM 1,25(OH)(2)D(3), and equivalent to control levels at the highest dose, paralleling hormone-mediated phosphate uptake."( Protein kinase C isotypes in signal transduction for the 1,25D3-MARRS receptor (ERp57/PDIA3) in steroid hormone-stimulated phosphate uptake.
Nemere, I; Tunsophon, S, 2010
)
0.36
"Responses were evaluated from dose-response curves of the metabolites and metabolic inhibitors in which growth of HeLa cells, apoptosis based on DAPI fluorescence and cytosolic NADH levels were correlated with sphingomyelinase and spingosine kinase activities and levels of ceramide and sphingosine1-phosphate."( Metabolite modulation of HeLa cell response to ENOX2 inhibitors EGCG and phenoxodiol.
De Luca, T; Morré, DJ; Morré, DM; Watanabe, T; Wu, LY, 2011
)
0.55
" Oral dosing of VPC03090 results in an approximate 1:1 phosphorylated/alcohol species ratio with a half-life of 30 h in mice."( Characterization of a sphingosine 1-phosphate receptor antagonist prodrug.
David, M; Huang, T; Kennedy, PC; Lynch, KR; Macdonald, TL; Mathews, TP; Peyruchaud, O; Tomsig, JL; Zhu, R, 2011
)
0.68
"The frequency of LT1009 dosage was determined initially using an enzyme-linked immunosorbent assay assay measuring LT1009 eye tissue retention in 6 New Zealand White rabbits."( Prevention of ocular scarring after glaucoma filtering surgery using the monoclonal antibody LT1009 (Sonepcizumab) in a rabbit model.
Beattie, AR; Levine, MA; Lukowski, ZL; Meyers, CA; Min, J; Samuelson, DA; Schultz, GS; Sherwood, MB; Stoller, G, 2013
)
0.39
" S1P(1) agonism alone reduced pathological features as did fingolimod (maximally lymphopenic throughout), despite full reversal of lymphopenia within each dosing interval."( S1P(1) receptor modulation with cyclical recovery from lymphopenia ameliorates mouse model of multiple sclerosis.
Cahalan, SM; Cameron, MD; Gonzalez-Cabrera, PJ; Kago, T; Leaf, NB; Nguyen, N; Rosen, H; Sarkisyan, G, 2012
)
0.38
" Dosing recommendations are largely based on tolerability studies, with most children and adolescents tolerating the full adult doses."( First-line disease-modifying therapies in paediatric multiple sclerosis: a comprehensive overview.
Johnston, J; So, TY, 2012
)
0.38
"001) and increased in a dose-response manner as the number of VF increased (P for the trend<0."( Plasma sphingosine 1-phosphate levels and the risk of vertebral fracture in postmenopausal women.
Cho, EH; Kim, BJ; Kim, GS; Kim, SW; Kim, SY; Kim, TH; Koh, JM; Lee, SH; Lee, SY; Lee, YS; Lim, KH, 2012
)
0.83
" Oral dosing of GCFr (3 and 10 mg/[kg·day]) improved TEWL treated with sodium dodecyl sulfate."( Changes in ceramides and glucosylceramides in mouse skin and human epidermal equivalents by rice-derived glucosylceramide.
Hitoe, S; Matsuda, H; Nakamura, S; Shimoda, H; Tanaka, J; Terazawa, S; Yoshikawa, M, 2012
)
0.38
"To make an informed benefit-risk evaluation of a drug, a range of doses needs to be evaluated and its dose-response and exposure-response relationships for safety and effectiveness assessed during drug development (International Conference on Harmonisation E4)."( Is this the dose for you?: the role of modeling.
Bhattaram, A; Huang, SM; Mehrotra, N; Wang, Y, 2013
)
0.39
" The dosage and temporal effect of the ceramide synthase inhibitor FTY720 on the LIRD retina were measured by histological and functional analyses."( Inhibition of de novo ceramide biosynthesis by FTY720 protects rat retina from light-induced degeneration.
Brush, RS; Chen, H; Eckerd, A; Elliott, MH; Huynh, TP; Mandal, NA; Tran, JA, 2013
)
0.39
" Group 3 animals were treated with the same dosage of FTY720 from day 0 to 100."( Early administration of FTY720 prevents chronic airway as well as vascular destruction in experimental rat lung transplantation.
Hirt, SW; Lehle, K; Puehler, T; Schmid, C; von Suesskind-Schwendi, M, 2013
)
0.39
"Astrocytes derived from human fetal CNS specimens and maintained in dissociated cultures were exposed to 100 nM of the biologically active form of FTY720 over a dosing regimen that ranged from a single exposure (with or without washout after 1 h) to daily exposures up to 5 days."( Dual effects of daily FTY720 on human astrocytes in vitro: relevance for neuroinflammation.
Antel, JP; Bar-Or, A; Bernier, LP; Cui, QL; Gris, P; Johnson, TA; Kennedy, TE; Leong, SY; Moore, CS; Séguéla, P; Wu, C, 2013
)
0.39
" Repeated FTY720 dosing concurrently maintained a functional cell response as measured by the inhibition of intracellular calcium release when stimulated by the cytokine IL-1β."( Dual effects of daily FTY720 on human astrocytes in vitro: relevance for neuroinflammation.
Antel, JP; Bar-Or, A; Bernier, LP; Cui, QL; Gris, P; Johnson, TA; Kennedy, TE; Leong, SY; Moore, CS; Séguéla, P; Wu, C, 2013
)
0.39
" Rats were administered an S1P1 inhibitor once daily for 4 weeks and necropsies were conducted at the end of the dosing phase, and clinical pathology and histopathologic examination were performed."( Gastric parietal cell atrophy and depletion after administration of a sphingosine-1-phosphate 1 inhibitor.
Radi, ZA; Vogel, MW, 2014
)
0.64
" The intravenous DMT natalizumab (Tysabri; dosed monthly) provides high therapeutic efficacy and good compliance but is considered a second-line intervention because of the associated increased risk for progressive multifocal leukoencephalopathy."( An update on new and emerging therapies for relapsing-remitting multiple sclerosis.
Weinstock-Guttman, B, 2013
)
0.39
" The risk for serious cardiovascular adverse events at the approved fingolimod dosage appears to be low in patients without pre-existing cardiac conditions."( Fingolimod: a review of its use in relapsing-remitting multiple sclerosis.
Sanford, M, 2014
)
0.4
" The results revealed that appropriate SmimHSO4 dosage and reaction time were 5% and 2h respectively."( Acidic ionic liquid catalyzed crosslinking of oxycellulose with chitosan for advanced biocomposites.
Chen, L; Fan, M; Huang, L; Luo, X; Zhou, Y, 2014
)
0.4
" Repeated oral dosing of the S1PL inhibitor in telemeterized, conscious rats resulted in significant bradycardia within 48 hours of drug treatment, comparable in magnitude to the bradycardia induced by 3 mg/kg fingolimod."( Sphingosine-1-Phosphate (S1P) Lyase Inhibition Causes Increased Cardiac S1P Levels and Bradycardia in Rats.
Banfor, P; Bousquet, P; Duignan, DB; Gintant, G; Harris, CM; Hart, M; Kim, Y; Mittelstadt, S; Segreti, J, 2016
)
1.88
" Defining the best drug dosing regimens to control the extent and duration of lymphopenia is critical to achieve the desired effects."( Selective Sphingosine 1-Phosphate Receptor 1 Agonist Is Protective Against Ischemia/Reperfusion in Mice.
Brait, VH; Gavaldà, A; Godessart, N; Planas, AM; Tarrasón, G, 2016
)
0.84
" Two weeks of NIBR-0213 oral dosing at 30, 100 and 300 mg/kg QD induced moderate pulmonary changes, characterized by alveolar wall thickening, macrophage accumulation, fibrosis, micro-hemorrhage, edema and necrosis."( Pathophysiological Consequences of a Break in S1P1-Dependent Homeostasis of Vascular Permeability Revealed by S1P1 Competitive Antagonism.
Angst, D; Beckmann, N; Beerli, C; Bigaud, M; Bollbuck, B; Bruns, C; Dawson, J; Dincer, Z; Fishli-Cavelti, G; Hersperger, R; Janser, P; Nahler, M; Otto, H; Quancard, J; Rosner, E, 2016
)
0.43
" Here, we showed that valproic acid (VPA), a histone deacetylase inhibitor, enforced the priming effect of S1P at a low dosage for human umbilical cord-derived MSCs (UC-MSCs)."( Valproic acid enforces the priming effect of sphingosine-1 phosphate on human mesenchymal stem cells.
Choi, KC; Heo, J; Ju, H; Kim, IG; Kim, Y; Lee, HY; Lee, S; Lim, J; Oh, YM; Shin, DM; Son, J, 2017
)
0.71
" The localized release dosage of effectors could be controlled by the change of environmental temperature."( Temperature-Gating Titania Nanotubes Regulate Migration of Endothelial Cells.
Bai, J; Du, W; Duan, Y; Gao, C; Liu, Y; Ouyang, H; Wu, S; Zhang, D; Zou, X, 2019
)
0.51
" Another promising strategy includes restoration of ceramide levels in HCC tissues, whereby nanoliposomal ceramides, in particular C6-ceramide, has emerged as an effective therapeutic agent against HCC whose safety and recommended dosing is currently being clinically investigated."( Targeting Ceramide Metabolism in Hepatocellular Carcinoma: New Points for Therapeutic Intervention.
Car, EPM; Grbčić, P; Sedić, M, 2020
)
0.56
" The latest researches showed that S1P can alleviate acute lung injury (ALI) and the inflammation caused by ALI, while the dosage of S1P is still needed to be considered."( [Research advances of the roles of sphingosine-1-phosphate in acute lung injury].
Cui, P; Wang, MY; Xin, HM, 2022
)
1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[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 (1)

ClassDescription
sphing-4-enineA sphingenine in which the C=C double bond is located at the 4-position.
[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 (9)

PathwayProteinsCompounds
Sphingolipid metabolism (integrated pathway)1167
Sphingolipid metabolism overview415
Sphingolipid metabolism: integrated pathway163
SARS-CoV-2 and COVID-19 pathway153
GDNF signaling1338
Synthesis of ceramides and 1-deoxyceramides115
Sphingolipid pathway315
Biochemical pathways: part I0466
Sphingolipids metabolism pathway063

Protein Targets (44)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency25.11895.623417.292931.6228AID2323; AID485281
Chain A, CruzipainTrypanosoma cruziPotency31.62280.002014.677939.8107AID1476
LuciferasePhotinus pyralis (common eastern firefly)Potency33.80780.007215.758889.3584AID588342
acid sphingomyelinaseHomo sapiens (human)Potency70.794614.125424.061339.8107AID504937
endonuclease IVEscherichia coliPotency15.84890.707912.432431.6228AID1708
phosphopantetheinyl transferaseBacillus subtilisPotency79.43280.141337.9142100.0000AID1490
ATAD5 protein, partialHomo sapiens (human)Potency14.12540.004110.890331.5287AID504467
USP1 protein, partialHomo sapiens (human)Potency44.66840.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency9.69450.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency39.81070.180013.557439.8107AID1460
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency11.22020.707912.194339.8107AID720542
glucocerebrosidaseHomo sapiens (human)Potency13.50890.01268.156944.6684AID2101
alpha-galactosidaseHomo sapiens (human)Potency4.46684.466818.391635.4813AID2107
IDH1Homo sapiens (human)Potency29.09290.005210.865235.4813AID686970
Bloom syndrome protein isoform 1Homo sapiens (human)Potency44.66840.540617.639296.1227AID2364; AID2528
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.23410.354828.065989.1251AID504847
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.63100.010039.53711,122.0200AID1479
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.48130.01789.637444.6684AID588834
DNA polymerase betaHomo sapiens (human)Potency35.48130.022421.010289.1251AID485314
mitogen-activated protein kinase 1Homo sapiens (human)Potency22.38720.039816.784239.8107AID1454
DNA polymerase eta isoform 1Homo sapiens (human)Potency35.48130.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency15.17410.004611.374133.4983AID463097; AID624296; AID624297
lamin isoform A-delta10Homo sapiens (human)Potency15.06540.891312.067628.1838AID1459; AID1487
[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)
ubiquitin-conjugating enzyme E2 NHomo sapiens (human)IC50 (µMol)6.31250.873010.721978.4000AID493155; AID493182
C-C chemokine receptor type 6Homo sapiens (human)IC50 (µMol)20.900011.500014.300017.1000AID540334
apelin receptorHomo sapiens (human)IC50 (µMol)66.60001.75003.39008.3500AID588359
bcl-2-related protein A1Mus musculus (house mouse)IC50 (µMol)20.00000.41907.756335.1000AID504689
Protein kinase C alpha typeRattus norvegicus (Norway rat)IC50 (µMol)40.00000.00000.21931.0000AID164979; AID165112; AID165117
Protein kinase C delta typeRattus norvegicus (Norway rat)IC50 (µMol)34.33330.00000.25851.0000AID165112; AID165117
Protein kinase C epsilon typeRattus norvegicus (Norway rat)IC50 (µMol)34.33330.00000.25851.0000AID165112; AID165117
Protein kinase C zeta typeRattus norvegicus (Norway rat)IC50 (µMol)34.33330.00000.25851.0000AID165112; AID165117
cAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)IC50 (µMol)0.09800.01801.09593.1000AID164615
Protein kinase C gamma typeRattus norvegicus (Norway rat)IC50 (µMol)40.00000.00000.26401.1000AID164979; AID165112; AID165117
Protein kinase C beta typeRattus norvegicus (Norway rat)IC50 (µMol)40.00000.00000.21641.1000AID164979; AID165112; AID165117
Protein kinase C eta typeRattus norvegicus (Norway rat)IC50 (µMol)34.33330.00000.25851.0000AID165112; AID165117
Sphingosine kinase 2Homo sapiens (human)IC50 (µMol)1.56000.35603.535210.0000AID420342
Sphingosine kinase 1Homo sapiens (human)IC50 (µMol)3.86000.00081.30397.1000AID420341
Protein kinase C theta typeRattus norvegicus (Norway rat)IC50 (µMol)34.33330.00000.25851.0000AID165112; AID165117
[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)
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)76.28000.06008.9128130.5170AID1902; AID1914
Estrogen receptorRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
Estrogen receptor betaRattus norvegicus (Norway rat)EC50 (µMol)150.00000.006022.3670130.5170AID1914
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

Processvia Protein(s)Taxonomy
blood vessel developmentSphingosine kinase 2Homo sapiens (human)
positive regulation of cytokine production involved in immune responseSphingosine kinase 2Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine kinase 2Homo sapiens (human)
sphinganine-1-phosphate biosynthetic processSphingosine kinase 2Homo sapiens (human)
sphingosine metabolic processSphingosine kinase 2Homo sapiens (human)
brain developmentSphingosine kinase 2Homo sapiens (human)
cell population proliferationSphingosine kinase 2Homo sapiens (human)
positive regulation of cell population proliferationSphingosine kinase 2Homo sapiens (human)
sphingolipid biosynthetic processSphingosine kinase 2Homo sapiens (human)
negative regulation of cell growthSphingosine kinase 2Homo sapiens (human)
positive regulation of interleukin-13 productionSphingosine kinase 2Homo sapiens (human)
positive regulation of interleukin-6 productionSphingosine kinase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionSphingosine kinase 2Homo sapiens (human)
positive regulation of mast cell activation involved in immune responseSphingosine kinase 2Homo sapiens (human)
positive regulation of apoptotic processSphingosine kinase 2Homo sapiens (human)
regulation of canonical NF-kappaB signal transductionSphingosine kinase 2Homo sapiens (human)
positive regulation of mast cell degranulationSphingosine kinase 2Homo sapiens (human)
transcription initiation-coupled chromatin remodelingSphingosine kinase 2Homo sapiens (human)
sphingosine biosynthetic processSphingosine kinase 2Homo sapiens (human)
positive regulation of protein kinase C signalingSphingosine kinase 2Homo sapiens (human)
positive regulation of calcium ion importSphingosine kinase 2Homo sapiens (human)
regulation of reactive oxygen species biosynthetic processSphingosine kinase 2Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateSphingosine kinase 2Homo sapiens (human)
regulation of cytochrome-c oxidase activitySphingosine kinase 2Homo sapiens (human)
positive regulation of ceramide biosynthetic processSphingosine kinase 2Homo sapiens (human)
regulation of ATP biosynthetic processSphingosine kinase 2Homo sapiens (human)
phosphorylationSphingosine kinase 2Homo sapiens (human)
negative regulation of apoptotic processSphingosine kinase 1Homo sapiens (human)
positive regulation of fibroblast proliferationSphingosine kinase 1Homo sapiens (human)
blood vessel developmentSphingosine kinase 1Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine kinase 1Homo sapiens (human)
protein acetylationSphingosine kinase 1Homo sapiens (human)
sphingosine metabolic processSphingosine kinase 1Homo sapiens (human)
inflammatory responseSphingosine kinase 1Homo sapiens (human)
brain developmentSphingosine kinase 1Homo sapiens (human)
cell population proliferationSphingosine kinase 1Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationSphingosine kinase 1Homo sapiens (human)
regulation of tumor necrosis factor-mediated signaling pathwaySphingosine kinase 1Homo sapiens (human)
phosphorylationSphingosine kinase 1Homo sapiens (human)
calcium-mediated signalingSphingosine kinase 1Homo sapiens (human)
regulation of endocytosisSphingosine kinase 1Homo sapiens (human)
sphingolipid biosynthetic processSphingosine kinase 1Homo sapiens (human)
positive regulation of cell growthSphingosine kinase 1Homo sapiens (human)
positive regulation of cell migrationSphingosine kinase 1Homo sapiens (human)
positive regulation of protein ubiquitinationSphingosine kinase 1Homo sapiens (human)
regulation of interleukin-1 beta productionSphingosine kinase 1Homo sapiens (human)
positive regulation of interleukin-17 productionSphingosine kinase 1Homo sapiens (human)
response to tumor necrosis factorSphingosine kinase 1Homo sapiens (human)
intracellular signal transductionSphingosine kinase 1Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusSphingosine kinase 1Homo sapiens (human)
negative regulation of apoptotic processSphingosine kinase 1Homo sapiens (human)
positive regulation of angiogenesisSphingosine kinase 1Homo sapiens (human)
positive regulation of mitotic nuclear divisionSphingosine kinase 1Homo sapiens (human)
positive regulation of mitotic cell cycleSphingosine kinase 1Homo sapiens (human)
positive regulation of smooth muscle contractionSphingosine kinase 1Homo sapiens (human)
sphingosine biosynthetic processSphingosine kinase 1Homo sapiens (human)
sphingoid catabolic processSphingosine kinase 1Homo sapiens (human)
regulation of phagocytosisSphingosine kinase 1Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activitySphingosine kinase 1Homo sapiens (human)
cellular response to hydrogen peroxideSphingosine kinase 1Homo sapiens (human)
DNA biosynthetic processSphingosine kinase 1Homo sapiens (human)
regulation of neuroinflammatory responseSphingosine kinase 1Homo sapiens (human)
negative regulation of ceramide biosynthetic processSphingosine kinase 1Homo sapiens (human)
positive regulation of p38MAPK cascadeSphingosine kinase 1Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionSphingosine kinase 1Homo sapiens (human)
regulation of microglial cell activationSphingosine kinase 1Homo sapiens (human)
regulation of endosomal vesicle fusionSphingosine kinase 1Homo sapiens (human)
cellular response to growth factor stimulusSphingosine kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
diacylglycerol-dependent serine/threonine kinase activityProtein kinase C delta typeRattus norvegicus (Norway rat)
protein serine/threonine kinase activitycAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
cAMP-dependent protein kinase activitycAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
lipid kinase activitySphingosine kinase 2Homo sapiens (human)
protein bindingSphingosine kinase 2Homo sapiens (human)
ATP bindingSphingosine kinase 2Homo sapiens (human)
sphinganine kinase activitySphingosine kinase 2Homo sapiens (human)
D-erythro-sphingosine kinase activitySphingosine kinase 2Homo sapiens (human)
small GTPase bindingSphingosine kinase 2Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine kinase 2Homo sapiens (human)
histone bindingSphingosine kinase 2Homo sapiens (human)
magnesium ion bindingSphingosine kinase 1Homo sapiens (human)
lipid kinase activitySphingosine kinase 1Homo sapiens (human)
DNA bindingSphingosine kinase 1Homo sapiens (human)
protein bindingSphingosine kinase 1Homo sapiens (human)
calmodulin bindingSphingosine kinase 1Homo sapiens (human)
ATP bindingSphingosine kinase 1Homo sapiens (human)
lipid bindingSphingosine kinase 1Homo sapiens (human)
sphinganine kinase activitySphingosine kinase 1Homo sapiens (human)
acetyltransferase activitySphingosine kinase 1Homo sapiens (human)
D-erythro-sphingosine kinase activitySphingosine kinase 1Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine kinase 1Homo sapiens (human)
protein phosphatase 2A bindingSphingosine kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
cytosolProtein kinase C delta typeRattus norvegicus (Norway rat)
cytosolProtein kinase C zeta typeRattus norvegicus (Norway rat)
nucleoplasmcAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
cytosolcAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
nucleusSphingosine kinase 2Homo sapiens (human)
nucleoplasmSphingosine kinase 2Homo sapiens (human)
cytoplasmSphingosine kinase 2Homo sapiens (human)
mitochondrionSphingosine kinase 2Homo sapiens (human)
mitochondrial inner membraneSphingosine kinase 2Homo sapiens (human)
lysosomal membraneSphingosine kinase 2Homo sapiens (human)
endoplasmic reticulumSphingosine kinase 2Homo sapiens (human)
cytosolSphingosine kinase 2Homo sapiens (human)
membraneSphingosine kinase 2Homo sapiens (human)
nucleosomeSphingosine kinase 2Homo sapiens (human)
intracellular membrane-bounded organelleSphingosine kinase 2Homo sapiens (human)
membraneSphingosine kinase 2Homo sapiens (human)
cytoplasmSphingosine kinase 2Homo sapiens (human)
presynapseSphingosine kinase 1Homo sapiens (human)
nucleusSphingosine kinase 1Homo sapiens (human)
nucleoplasmSphingosine kinase 1Homo sapiens (human)
cytoplasmSphingosine kinase 1Homo sapiens (human)
cytosolSphingosine kinase 1Homo sapiens (human)
plasma membraneSphingosine kinase 1Homo sapiens (human)
clathrin-coated pitSphingosine kinase 1Homo sapiens (human)
endocytic vesicleSphingosine kinase 1Homo sapiens (human)
early endosome membraneSphingosine kinase 1Homo sapiens (human)
presynapseSphingosine kinase 1Homo sapiens (human)
intracellular membrane-bounded organelleSphingosine kinase 1Homo sapiens (human)
membraneSphingosine kinase 1Homo sapiens (human)
cytoplasmSphingosine kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (93)

Assay IDTitleYearJournalArticle
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.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1627821Downregulation of CD98 expression level in mouse FL5.12A cells at 2.5 uM measured at 3 hrs by flow cytometric analysis2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Effects of stereochemistry, saturation, and hydrocarbon chain length on the ability of synthetic constrained azacyclic sphingolipids to trigger nutrient transporter down-regulation, vacuolation, and cell death.
AID499003Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 I183F mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499024Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 N334S mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499004Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 I276F mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499005Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 T257I T416A mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499010Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 D314Y mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID401373Antimicrobial activity against Prorocentrum micans at 5 ppm1998Journal of natural products, Jun-26, Volume: 61, Issue:6
New ceramide from marine sponge Haliclona koremella and related compounds as antifouling substances against macroalgae.
AID464144Antifungal activity against Candida glabrata by broth microdilution method2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
Synthesis and chain-dependent antifungal activity of long-chain 2H-azirine-carboxylate esters related to dysidazirine.
AID357403Resistance index, ratio of IC50 for 2-amino-4-(4-heptyloxyphenyl)-2-methylbutanol-resistant human Jurkat SBR1 mutant cells to IC50 for human wild type Jurkat cells2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID164979In vitro inhibition of [32P] incorporation into histones by rat brain partially purified Protein kinase C in the presence of PMA, [Ca2+] and phosphatidylserine.1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Substituted 2-(aminomethyl)piperidines: a novel class of selective protein kinase C inhibitors.
AID499023Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 G370E mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499007Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 V269I G370R mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499012Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A153T D314Y mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499008Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 G370E mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499009Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 N334S mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID101364Median growth inhibitory concentration of compound tested in vitro against human leukemia 60 cells2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Antitumour activity of sphingoid base adducts of phenethyl isothiocyanate.
AID499022Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 V269I G370R mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499006Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 V269I mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID390922Antibacterial activity against methicillin-resistant Staphylococcus aureus2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: polycationic lipids with potent gram-positive activity.
AID49951Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 5 ug/mL before dilution replating; growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID681583TP_TRANSPORTER: cell accumulation (digoxin-sensitive) in Caco-2 cells2004Bioscience, biotechnology, and biochemistry, Dec, Volume: 68, Issue:12
Efflux of sphingoid bases by P-glycoprotein in human intestinal Caco-2 cells.
AID49963Minimum inhibitory concentration against Candida glabrata2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID401370Antifouling activity against Ulva conglobata spores assessed as germination and attachment rate at 5 ppm1998Journal of natural products, Jun-26, Volume: 61, Issue:6
New ceramide from marine sponge Haliclona koremella and related compounds as antifouling substances against macroalgae.
AID165117Displacement of [3H]PDBU from protein kinase C1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.
AID401376Antimicrobial activity against Oscillatoria amphibia at 5 ppm1998Journal of natural products, Jun-26, Volume: 61, Issue:6
New ceramide from marine sponge Haliclona koremella and related compounds as antifouling substances against macroalgae.
AID390921Antibacterial activity against Staphylococcus aureus2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: polycationic lipids with potent gram-positive activity.
AID357404Resistance index, ratio of IC50 for 2-amino-4-(4-heptyloxyphenyl)-2-methylbutanol-resistant human Jurkat SBR2 mutant cells to IC50 for human wild type Jurkat cells2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID499002Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 R177H mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID305218Effect on rate of phosphorylation of human recombinant SPHK1 expressed in HEK293 cells2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
AID1627822Induction of vacuolation in mouse FL5.12A cells assessed as vacuolation score at 2.5 uM measured at 3 hrs by fluorescence microscopic analysis2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Effects of stereochemistry, saturation, and hydrocarbon chain length on the ability of synthetic constrained azacyclic sphingolipids to trigger nutrient transporter down-regulation, vacuolation, and cell death.
AID1627820Cytotoxicity against mouse FL5.12A cells after 48 hrs by DAPI staining-based flow cytometric analysis2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Effects of stereochemistry, saturation, and hydrocarbon chain length on the ability of synthetic constrained azacyclic sphingolipids to trigger nutrient transporter down-regulation, vacuolation, and cell death.
AID499011Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 P394S mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID49947Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 12 ug/mL before dilution replating; growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID499028Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A153T D314Y R177H mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499027Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A153T D314Y mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID49826Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 0.3 ug/mL before dilution replating; growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID499015Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A81E mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID49827Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 10 ug/mL before dilution replating; growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID499000Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A81E mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499001Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A153T mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID390923Antibacterial activity against Escherichia coli2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: polycationic lipids with potent gram-positive activity.
AID499014Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 containing wild type sequence E351S2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID101365Median toxic concentration of compound tested in vitro against human leukemia 60 cells2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Antitumour activity of sphingoid base adducts of phenethyl isothiocyanate.
AID499026Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 P394S mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID49952Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 6 ug/mL before dilution replating; growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID357405Resistance index, ratio of IC50 for 2-amino-4-(4-heptyloxyphenyl)-2-methylbutanol-resistant human Jurkat SBR3 mutant cells to IC50 for human wild type Jurkat cells2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID401369Antifouling activity against Ulva conglobata spores assessed as germination and attachment rate at 1 ppm1998Journal of natural products, Jun-26, Volume: 61, Issue:6
New ceramide from marine sponge Haliclona koremella and related compounds as antifouling substances against macroalgae.
AID499016Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A153T mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID165112Inhibitory activity against protein kinase C of rat brain1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.
AID49950Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 3 ug/mL before dilution replating; growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID401374Antimicrobial activity against Skeletonema costatum at 5 ppm1998Journal of natural products, Jun-26, Volume: 61, Issue:6
New ceramide from marine sponge Haliclona koremella and related compounds as antifouling substances against macroalgae.
AID499013Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 A153T D314Y R177H mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID420341Inhibition of SphK12009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Iodophenyl tagged sphingosine derivatives: synthesis and preliminary biological evaluation.
AID357393Inhibition of 2-amino-4-(4-heptyloxyphenyl)-2-methylbutanol-resistant human Jurkat SBR2 mutant cells proliferation after 18 hrs by MTT assay2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID499021Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 V269I mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID498999Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 containing wild type sequence E351S2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
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.
AID499018Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 I183F mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID401372Antimicrobial activity against Branchiomonas submaria at 5 ppm1998Journal of natural products, Jun-26, Volume: 61, Issue:6
New ceramide from marine sponge Haliclona koremella and related compounds as antifouling substances against macroalgae.
AID164615Inhibition of cAMP-dependent kinase PKA(Protein kinase A) catalytic subunit at 100 uM1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Substituted 2-(aminomethyl)piperidines: a novel class of selective protein kinase C inhibitors.
AID357394Inhibition of human 2-amino-4-(4-heptyloxyphenyl)-2-methylbutanol-resistant human Jurkat SBR3 mutant cells proliferation after 18 hrs by MTT assay2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID357391Cell viability of Sphk2-knock out mouse embryonic fibroblasts assessed as resistant cells after 18 hrs by propidium iodide exclusion assay2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID305219Effect on rate of phosphorylation of human recombinant SPHK2 expressed in HEK293 cells2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors.
AID420342Inhibition of SphK22009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Iodophenyl tagged sphingosine derivatives: synthesis and preliminary biological evaluation.
AID357392Inhibition of 2-amino-4-(4-heptyloxyphenyl)-2-methylbutanol-resistant human Jurkat SBR1 mutant cells proliferation after 18 hrs by MTT assay2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID499025Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 D314Y mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID499017Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 R177H mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID357402Inhibition of wild type human Jurkat cells after 18 hrs by MTT assay2007The Journal of biological chemistry, May-25, Volume: 282, Issue:21
Essential requirement for sphingosine kinase 2 in a sphingolipid apoptosis pathway activated by FTY720 analogues.
AID499019Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 I276F mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID623346Cytotoxicity against human SHG44 at 50 uM after 24 hrs by cell counting kit-8 assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Diastereoselective synthesis and bioactivity of long-chain anti-2-amino-3-alkanols.
AID499020Ratio of Kcat to Km of Activity of Rhodococcus sp. M777 Endoglycoceramidase 2 T257I T416A mutant2009Nature chemical biology, Jul, Volume: 5, Issue:7
Designer enzymes for glycosphingolipid synthesis by directed evolution.
AID49949Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 30 ug/mL before dilution replating; no growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
AID390919Antibacterial activity against Candida albicans2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: polycationic lipids with potent gram-positive activity.
AID49948Fungistatic activity of bifunctional sphingolipids against Candida glabrata at a concentration of 1 ug/mL before dilution replating; growth in media2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
Antifungal activity of bifunctional sphingolipids. Intramolecular synergism within long-chain alpha,omega-bis-aminoalcohols.
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.
AID1346644Mouse TRPM7 (ChaK subfamily)2013British journal of pharmacology, Mar, Volume: 168, Issue:6
Sphingosine and FTY720 are potent inhibitors of the transient receptor potential melastatin 7 (TRPM7) channels.
AID1346619Human TRPM3 (Transient Receptor Potential channels)2005Molecular pharmacology, Mar, Volume: 67, Issue:3
Activation of the melastatin-related cation channel TRPM3 by D-erythro-sphingosine [corrected].
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,164)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990493 (6.04)18.7374
1990's1183 (14.49)18.2507
2000's2682 (32.85)29.6817
2010's3100 (37.97)24.3611
2020's706 (8.65)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 50.09

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index50.09 (24.57)
Research Supply Index9.04 (2.92)
Research Growth Index4.95 (4.65)
Search Engine Demand Index134.97 (26.88)
Search Engine Supply Index3.12 (0.95)

This Compound (50.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials117 (1.41%)5.53%
Reviews1,072 (12.88%)6.00%
Case Studies70 (0.84%)4.05%
Observational20 (0.24%)0.25%
Other7,046 (84.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]