Page last updated: 2024-12-08

o-(chloroacetylcarbamoyl)fumagillol

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Description

O-(Chloroacetylcarbamoyl)fumagillol: Semisynthetic analog of fumagillin (a cyclohexane-sesquiterpene antibiotic isolated from ASPERGILLUS FUMIGATUS) that inhibits angiogenesis. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

O-(chloroacetylcarbamoyl)fumagillol : A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative. [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 CID369976
CHEMBL ID424278
CHEBI ID90748
SCHEMBL ID1652694
MeSH IDM0182531

Synonyms (48)

Synonym
NCI60_014346
nsc 642492
drg-0148
carbamic acid, (chloroacetyl)-, 5-methoxy-4-(2-methyl-3-(3-methyl-2-butenyl)oxiranyl)-1-oxaspiro(2.5)oct-6-yl ester, (3r-(3alpha,4alpha(2r*,3r*),5beta,6beta))-
o-chloroacetylcarbamoylfumagillol
ccris 8049
carbamic acid, (3r,4s,5s,6r)-5-methoxy-4-[ (2r,3r)-2-methyl-3-(3-methyl-2-butenyl)oxiranyl]-1-oxaspiro[2.5]oct-6-yl ester
nsc642492
nsc-642492
agm-1470
carbamic acid, (chloroacetyl)-, (3r,4s,5s,6r)-5-methoxy-4-[(2r,3r)-2-methyl-3-(3-methyl-2-butenyl)oxiranyl]-1-oxaspiro[2.5]oct-6-yl ester
129298-91-5
[(3r,6r,7s,8s)-7-methoxy-8-[(2r,3r)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-2-oxaspiro[2.5]octan-6-yl] n-(2-chloroacetyl)carbamate
o-(chloroacetylcarbamoyl)fumagillol
agm 1470
tnp-470
tnp 470
chembl424278 ,
bdbm17446
(3r,4s,5s,6r)-5-methoxy-4-[(2r,3r)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl n-(2-chloroacetyl)carbamate
chebi:90748 ,
DB08633
unii-x47gr46481
x47gr46481 ,
tox21_303433
cas-129298-91-5
dtxsid0041141 ,
NCGC00257293-01
dtxcid00819891
tnp-470 [mi]
carbamic acid, n-(2-chloroacetyl)-, (3r,4s,5s,6r)-5-methoxy-4-((2r,3r)-2-methyl-3-(3-methyl-2-buten-1-yl)-2-oxiranyl)-1-oxaspiro(2.5)oct-6-yl ester
BRD-K53597484-001-01-9
CCG-208103
SCHEMBL1652694
(3r,4s,5s,6r)-5-methoxy-4-((2r,3r)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (2-chloroacetyl)carbamate
(3r,4s,5s,6r)-5-methoxy-4-[(2r,3r)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl (chloroacetyl)carbamate
(chloroacetyl)carbamic acid (3r,4s,5s,5r)-5-methoxy-4-[(2r,3r)-2-methyl-3-(3-methyl-2-butenyl)oxiranyl]-1-oxaspiro[2.5]oct-6-yl ester
J-005665
tnp-470, >=98% (hplc)
CS-8106
MSHZHSPISPJWHW-PVDLLORBSA-N
HY-101932
Q27097825
carbamic acid, n-(2-chloroacetyl)-, (3r,4s,5s,6r)-5-methoxy-4-[(2r,3r)-2-methyl-3-(3-methyl-2-buten-1-yl)-2-oxiranyl]-1-oxaspiro[2.5]oct-6-yl ester
[(3r,4s,5s,6r)-5-methoxy-4-[(2r,3r)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] n-(2-chloroacetyl)carbamate
MS-26845
agm-1470; nsc 642492
AKOS040742752

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Bone neoplasms, such as osteosarcoma, exhibit a propensity for systemic metastases resulting in adverse clinical outcome."( Enhanced anti-tumor activity and safety profile of targeted nano-scaled HPMA copolymer-alendronate-TNP-470 conjugate in the treatment of bone malignances.
Benayoun, L; Kopeček, J; Kopečková, P; Pan, H; Satchi-Fainaro, R; Segal, E; Shaked, Y, 2011
)
0.37

Pharmacokinetics

ExcerptReferenceRelevance
"To characterize the pharmacokinetic profile of TNP-470, a synthetic analog of fumagillin that is a potent inhibitor of angiogenesis and inhibits neovascularization in several solid tumor models."( The pharmacokinetics of TNP-470, a new angiogenesis inhibitor.
Figg, WD; Lush, RM; Pluda, JM; Reed, E; Saville, MW; Wyvill, K; Yarchoan, R,
)
0.13
" The mean plasma half-life (t(1/2)) of TNP-470 and its principal metabolite, AGM-1883, were extremely short (harmonic mean, t(1/2) of 2 and 6 min, respectively) with practically no drug detectable in the plasma by 60 min after the end of the infusion."( A Phase I and pharmacokinetic study of TNP-470 administered weekly to patients with advanced cancer.
Bhargava, P; Dahut, W; Figuera, M; Hawkins, MJ; Kato, A; Marshall, JL; Ong, VS; Phipps, K; Rizvi, N; Yoe, J, 1999
)
0.3
" Statistical analyses of pharmacokinetic and pharmacodynamic end points in the control and TNP-470 treatment groups were completed by nonparametric tests."( Pharmacodynamic-mediated reduction of temozolomide tumor concentrations by the angiogenesis inhibitor TNP-470.
Chu, J; Gallo, JM; Li, S; Ma, J; Pulfer, S; Reed, K, 2001
)
0.31
" TNP-470 was administered with paclitaxel to adults with solid tumors to define the safety and optimal dose of the combination regimen and to assess pharmacokinetic interactions."( Safety and pharmacokinetic effects of TNP-470, an angiogenesis inhibitor, combined with paclitaxel in patients with solid tumors: evidence for activity in non-small-cell lung cancer.
Allgood, V; Blumenschein, GR; Crane, EA; Dordal, M; Fossella, FV; Fritsche, HA; Goodin, T; Herbst, RS; Hinton, L; Hong, WK; Khuri, FR; Madden, TL; Meyers, CA; Newman, RA; Puduvalli, VK; Seabrooke, LF; Tran, HT, 2002
)
0.31
"The combination of TNP-470 and paclitaxel, each at full single-agent dose, seems well tolerated, with minimal pharmacokinetic interaction between the two agents."( Safety and pharmacokinetic effects of TNP-470, an angiogenesis inhibitor, combined with paclitaxel in patients with solid tumors: evidence for activity in non-small-cell lung cancer.
Allgood, V; Blumenschein, GR; Crane, EA; Dordal, M; Fossella, FV; Fritsche, HA; Goodin, T; Herbst, RS; Hinton, L; Hong, WK; Khuri, FR; Madden, TL; Meyers, CA; Newman, RA; Puduvalli, VK; Seabrooke, LF; Tran, HT, 2002
)
0.31
" No alterations in the pharmacokinetic disposition of carboplatin were noted."( Clinical and pharmacokinetic study of TNP-470, an angiogenesis inhibitor, in combination with paclitaxel and carboplatin in patients with solid tumors.
Blumenschein, GR; Fossella, FV; Herbst, RS; Lu, C; Madden, T; Meyers, CA; Munden, R; Papadimitrakopoulou, V; Puduvalli, VK; Smythe, LG; Tran, HT; Truong, M; Zinner, R, 2004
)
0.32
" To that end, a novel method, based on physiologically based hybrid pharmacokinetic models, is presented to predict human tumor drug concentrations."( Pharmacokinetic model-predicted anticancer drug concentrations in human tumors.
Bookman, MA; Gallo, JM; Guo, P; Li, S; Ma, J; Orlansky, A; Pulfer, S; Vicini, P; Zhou, F, 2004
)
0.32

Compound-Compound Interactions

ExcerptReferenceRelevance
"Effects of a newly developed angiogenesis inhibitor, TNP-470 (AGM-1470) alone and in combination with cisplatinum on tumor-bearing rats were investigated."( [Anti-tumor effects of an angiogenesis inhibitor, TNP-470 (AGM-1470) alone and in combination with cisplatinum, and changes in serum copper levels in liver cancer bearing rats].
Matsuoka, S, 1996
)
0.29
" In vitro studies with isolated monkey liver microsomes confirmed these drug-drug metabolic interactions detected at the cellular level."( Metabolic drug interactions between angiogenic inhibitor, TNP-470 and anticancer agents in primary cultured hepatocytes and microsomes.
Bynon, S; Eckoff, D; Placidi, L; Scott, EC; Sommadossi, JP, 1999
)
0.3
" m When TNP-470 was combined with combreAp, no significant lengthening of the growth delay, irrespective of the tumor size, was present with the applied schedule."( In vivo antitumor effect of vascular targeting combined with either ionizing radiation or anti-angiogenesis treatment.
Ahmed, B; Anné, J; Lambin, P; Landuyt, W; Nuyts, S; Op de Beeck, M; Rijnders, A; Theys, J; van den Bogaert, W; van Oosterom, A, 2001
)
0.31
" In mice bearing transplantable Lewis lung cancer the additive antiangiogenic, but not cytostatic, effect of genistein combined with cyclophosphamide (CY) was observed, since the treatment with genistein alone reduced tumour blood supply in 35% (tumour weight in 36%), with CY in 38% (tumour weight in 70%) and with both compounds in 61% (tumour weight in 75%)."( Antiangiogenic and antitumour effects in vivo of genistein applied alone or combined with cyclophosphamide.
Boratynski, J; Grynkiewicz, G; Opolski, A; Radzikowski, C; Ryczynski, A; Wietrzyk, J,
)
0.13
" Furthermore, they imply efficiency of daily administration of nontoxic doses of chemotherapy, and a possible additive effect when chemotherapy is combined with angiogenesis inhibitors."( CHS 828 inhibits neuroblastoma growth in mice alone and in combination with antiangiogenic drugs.
Bäckman, U; Christofferson, R; Jonsson, E; Larsson, R; Svensson, A, 2002
)
0.31
" TNP-470 was administered with paclitaxel to adults with solid tumors to define the safety and optimal dose of the combination regimen and to assess pharmacokinetic interactions."( Safety and pharmacokinetic effects of TNP-470, an angiogenesis inhibitor, combined with paclitaxel in patients with solid tumors: evidence for activity in non-small-cell lung cancer.
Allgood, V; Blumenschein, GR; Crane, EA; Dordal, M; Fossella, FV; Fritsche, HA; Goodin, T; Herbst, RS; Hinton, L; Hong, WK; Khuri, FR; Madden, TL; Meyers, CA; Newman, RA; Puduvalli, VK; Seabrooke, LF; Tran, HT, 2002
)
0.31
"To investigate the short-term effects of TNP-470 in combination with cisplatin in a rat model of bladder cancer."( Short-term effects of TNP-470 in combination with cisplatin in the rat model of bladder cancer.
Kakehi, Y; Uetsuki, H; Yamashita, M; Zhang, X,
)
0.13
" This study was designed to investigate the effects of angiogenesis inhibitor TNP-470 in combination with 5-fluorouracil (5-FU) on the growth of human colon cancer cell line, LOVO, in vitro and in vivo."( [Inhibitory effects of TNP-470 in combination with 5-fluorouracil on growth of human colon cancer].
Fan, YF; Huang, ZH; Nie, J, 2002
)
0.31
" In vivo, human colon cancer xenografts were transplanted into BALB/C nude mice and treated with TNP-470 alone and combination with 5-FU."( [Inhibitory effects of TNP-470 in combination with 5-fluorouracil on growth of human colon cancer].
Fan, YF; Huang, ZH; Nie, J, 2002
)
0.31
" Expression of VEGF in tumors was clearly inhibited by TNP-470 in combination with 5-FU or 5-FU alone compared to the control."( [Inhibitory effects of TNP-470 in combination with 5-fluorouracil on growth of human colon cancer].
Fan, YF; Huang, ZH; Nie, J, 2002
)
0.31
"TNP-470 suppressed the growth of LOVO cells and human colon cancer xenografts and the angiogenesis; TNP-470 in combination with 5-FU might product synergetic effect."( [Inhibitory effects of TNP-470 in combination with 5-fluorouracil on growth of human colon cancer].
Fan, YF; Huang, ZH; Nie, J, 2002
)
0.31
" The present study was designed to determine the toxicity and pharmacokinetics of carboplatin in combination with TNP-470 in comparison with the doublet regimen of paclitaxel and carboplatin in patients with solid tumors."( Clinical and pharmacokinetic study of TNP-470, an angiogenesis inhibitor, in combination with paclitaxel and carboplatin in patients with solid tumors.
Blumenschein, GR; Fossella, FV; Herbst, RS; Lu, C; Madden, T; Meyers, CA; Munden, R; Papadimitrakopoulou, V; Puduvalli, VK; Smythe, LG; Tran, HT; Truong, M; Zinner, R, 2004
)
0.32
" This study was designed to observe the synergetic inhibitory effect of fumagillol (TNP-470) in combination with cyclophosphamide (CTX) on metastasis of lung adenocarcinoma cell line LA795 xenograft in mouse, and to explore the related mechanism of suppressing tumor metastasis by TNP-470."( [Inhibitory effect of fumagillol combined with cyclophosphamide on metastasis of lung adenocarcinoma cell line LA795 xenograft in mice].
Duan, BC; He, JB; Ou, LW; Song, JT; Wang, XH; Wang, Z; Zhang, P, 2005
)
0.33
"05), 10(-6) mg/ml gemcitabine in combination with 10(-4) mg/ml TNP-470 had significant effect (P<0."( Inhibition of expression of vascular endothelial growth factor and its receptors in pulmonary adenocarcinoma cell by TNP-470 in combination with gemcitabine.
Tu, LF; Wang, LH; Wang, XF; Zhou, JY, 2006
)
0.33
" This study firstly examined the antitumor effect of angiogenesis inhibitor combined with ultrasound (US) irradiation for human cancer in vivo and evaluated its vascularity using color Doppler US in real time with a microbubble US contrast agent."( Antitumor effect of TNP-470, an angiogenesis inhibitor, combined with ultrasound irradiation for human uterine sarcoma xenografts evaluated using contrast color Doppler ultrasound.
Emoto, M; Iwasaki, H; Kawarabayashi, T; Tachibana, K, 2007
)
0.34
"This study investigated the effect of TNP-470 in combination with carmustine (BCNU) on the growth of subcutaneously implanted human glioblastoma xenografts in nude mice."( Inhibitory effects of TNP-470 in combination with BCNU on tumor growth of human glioblastoma xenografts.
Chen, J; Jiang, X; Yao, D; Zhang, F; Zhao, H; Zhu, X, 2010
)
0.36
" The antitumor and anti-angiogenic effects of metronomic doxifluridine (delivered via oral gavage) in combination with TNP-470 were evaluated in vivo."( Metronomic doxifluridine chemotherapy combined with the anti-angiogenic agent TNP-470 inhibits the growth of human uterine carcinosarcoma xenografts.
Choijamts, B; Emoto, M; Kawarabayashi, T; Miyamoto, S; Naganuma, Y; Nakajima, K; Ogata, S; Shirota, K, 2011
)
0.37

Dosage Studied

ExcerptRelevanceReference
"The TNP-470 dosage was increased in 13 sequential cohorts using a modified Fibonacci escalation scheme (4."( The pharmacokinetics of TNP-470, a new angiogenesis inhibitor.
Figg, WD; Lush, RM; Pluda, JM; Reed, E; Saville, MW; Wyvill, K; Yarchoan, R,
)
0.13
"6 ng/ml at the lowest dosage (4."( The pharmacokinetics of TNP-470, a new angiogenesis inhibitor.
Figg, WD; Lush, RM; Pluda, JM; Reed, E; Saville, MW; Wyvill, K; Yarchoan, R,
)
0.13
" We speculate that antiangiogenic therapy may be a useful therapeutic modality in the treatment of advanced neuroblastoma once side effects and appropriate dosage requirements are determined."( TNP-470 antiangiogenic therapy for advanced murine neuroblastoma.
Nagabuchi, E; Une, Y; VanderKolk, WE; Ziegler, MM, 1997
)
0.3
" Alternate-day dosing was as effective as consecutive day administration."( Angiogenesis inhibitor TNP-470 inhibits murine cutaneous wound healing.
Anderson, GL; Bond, SJ; Gupta, SC; Klein, SA; Yacoub, OA, 1999
)
0.3
"9% at the dosage of 15 mg/kg, 30 mg/kg and 60 mg/kg, respectively."( [Experimental study of the effect of angiogenesis inhibitor TNP-470 on the growth and metastasis of gastric cancer in vivo].
Lin, Y; Liu, B; Yin, H, 1998
)
0.3
"In the preventive protocol, with TNP-470 administration at a dosage of 60 mg/kg of body weight, the onset of arthritis was delayed and its clinical intensity was rather mild; 100% of placebo-treated transgenic mice developed arthritis that led to severe articular destruction."( Suppression of arthritis and protection from bone destruction by treatment with TNP-470/AGM-1470 in a transgenic mouse model of rheumatoid arthritis.
Chopin, M; de Bandt, M; Elbim, C; Gaudry, M; Gougerot-Pocidalo, MA; Grossin, M; Pla, M; Weber, AJ, 2000
)
0.31
"029) for each dosing method, respectively."( The angiogenesis inhibitor tnp-470 effectively inhibits human neuroblastoma xenograft growth, especially in the setting of subclinical disease.
Barr, R; Carpentieri, D; Grupp, SA; Maris, JM; Shusterman, S; Zhao, H, 2001
)
0.31
" One day after the last dose of vehicle or TNP-470, a steady-state dosing regimen of TMZ was administered with subsequent collection and high-performance liquid chromatography analysis of plasma and either tumor homogenate or tumor microdialysis steady-state TMZ concentrations, and in some cases [5-(3-methyltriazen-1-yl)imidazole-4-carboximide] MTIC, its active metabolite."( Pharmacodynamic-mediated reduction of temozolomide tumor concentrations by the angiogenesis inhibitor TNP-470.
Chu, J; Gallo, JM; Li, S; Ma, J; Pulfer, S; Reed, K, 2001
)
0.31
" Then, TNP-470 was administered continuously by subcutaneous injection pump at a dosage of 30 mg/kg/week."( The effect of angiogenesis inhibitor TNP-470 against postoperative lung metastasis following removal of orthotopic transplanted human colon cancer: an experimental study.
Oda, H; Ogata, Y; Shirouzu, K, 2001
)
0.31
" TNP-470 was administered in several dosing and scheduling regimens, and its effects on tumor growth, metastasis, intratumor neovascularization, and mRNA expression of angiogenic factors were determined in both nonestablished and established tumors."( Frequent administration of angiogenesis inhibitor TNP-470 (AGM-1470) at an optimal biological dose inhibits tumor growth and metastasis of metastatic human transitional cell carcinoma in the urinary bladder.
Chikazawa, M; Fukata, S; Inoue, K; Shuin, T; Yoshikawa, C, 2002
)
0.31
" In this study, we investigated whether antitumor efficacy of angiogenesis inhibitor, TNP-470 [O-(chloroacetyl-carbamoyl) fumagillol], could be improved by optimizing the dosing schedule."( Optimizing the dosing schedule of TNP-470 [O-(chloroacetyl-carbamoyl) fumagillol] enhances its antitumor and antiangiogenic efficacies.
Koyanagi, S; Kuramoto, Y; Nakagawa, H; Ohdo, S; Shimeno, H; Soeda, S, 2003
)
0.32
"Rats were treated with vehicle or with TNP-470 at low dosage (10 mg/kg), medium dosage (20 mg/kg), or high dosage (40 mg/kg)."( Angiogenesis inhibitor TNP-470 (AGM-1470) suppresses vascular smooth muscle cell proliferation after balloon injury in rats.
Hoshino, Y; Ishikawa, S; Kurabayashi, M; Maeno, T; Morishita, Y; Nagai, R; Ogata, T; Sekiguchi, K; Takei, H, 2003
)
0.32
" Combining medium dosage of angiogensis inhibitor with chemical drug may have synergistic result in inhibiting ACC growth."( [Combining of TNP-470 and 5-Fu in inhibition of adenoid cystic carcinoma in nude mice model].
Li, JQ; Meng, M; Meng, N; Nong, XL; Wang, DZ; Zhang, H; Zhou, N, 2004
)
0.32
"Antiangiogenic therapy shows significant anti-tumor and anti-metastatic effects, and is helpful to reduce the dosage of cytotoxic drugs and the side effects."( Antiangiogenic therapy for human pancreatic carcinoma xenografts in nude mice.
Huang, WG; Jia, L; Yuan, SZ; Zhang, MH, 2005
)
0.33
" TNP-470 dosage was escalated in CT-26-bearing animals until an antiangiogenic effect could be observed."( TNP-470 fails to block the onset of angiogenesis and early tumor establishment in an intravital minimal disease model.
Bennek, J; Celik, I; Cernaianu, G; Cross, M; Dansranjavin, T; Erbstösser, K; Frank, S; Hauss, J; Leonhardt, S; McIvor, Z; Rothe, K; Scholz, G; Tannapfel, A; Troebs, RB; Wittekind, C; Witzigmann, H, 2006
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
methionine aminopeptidase 2 inhibitorAny methionyl aminopeptidase inhibitor that inhibits the action of methionyl aminopeptidase 2.
retinoic acid receptor alpha antagonistA retinoic acid receptor antagonist that antagonises retinoic acid receptor alpha.
angiogenesis inhibitorAn agent and endogenous substances that antagonize or inhibit the development of new blood vessels.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
EC 1.5.1.3 (dihydrofolate reductase) inhibitorAn EC 1.5.1.* (oxidoreductase acting on donor CH-NH group, NAD(+) or NADP(+) as acceptor) inhibitor that interferes with the action of dihydrofolate reductase (EC 1.5.1.3).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
sesquiterpenoidAny terpenoid derived from a sesquiterpene. The term includes compounds in which the C15 skeleton of the parent sesquiterpene has been rearranged or modified by the removal of one or more skeletal atoms (generally methyl groups).
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
semisynthetic derivativeAny organic molecular entity derived from a natural product by partial chemical synthesis.
spiro-epoxideAn oxaspiro compound in which a carbon atom of an epoxide ring is the only common member of two rings.
[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 (1)

PathwayProteinsCompounds
Ac/N-end rule pathway109

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency18.78240.006038.004119,952.5996AID1159521; AID1159523
AR proteinHomo sapiens (human)Potency17.62160.000221.22318,912.5098AID1259243; AID1259247; AID743053
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency0.10560.001022.650876.6163AID1224838
progesterone receptorHomo sapiens (human)Potency0.14920.000417.946075.1148AID1346784
retinoid X nuclear receptor alphaHomo sapiens (human)Potency10.05910.000817.505159.3239AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency21.53250.001530.607315,848.9004AID1224841; AID1259401
pregnane X nuclear receptorHomo sapiens (human)Potency10.56210.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency1.68660.000229.305416,493.5996AID743075; AID743078
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency11.43960.001019.414170.9645AID743094; AID743140
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency1.23140.023723.228263.5986AID743222; AID743223
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency10.07570.057821.109761.2679AID1159526; AID1159528
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency6.66330.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency13.73690.042027.378961.6448AID743210; AID743228
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency2.43460.000627.21521,122.0200AID743202; AID743219
Cellular tumor antigen p53Homo sapiens (human)Potency18.78240.002319.595674.0614AID651631; AID720552
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency18.78240.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency18.78240.011912.222168.7989AID651632
[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)
Methionine aminopeptidase 2Homo sapiens (human)IC50 (µMol)0.59300.00060.96835.6000AID270591; AID424804; AID620249; AID746915
Methionine aminopeptidase 2Homo sapiens (human)Ki0.00100.00100.00100.0010AID1797624; AID296847
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (144)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
protein processingMethionine aminopeptidase 2Homo sapiens (human)
peptidyl-methionine modificationMethionine aminopeptidase 2Homo sapiens (human)
N-terminal protein amino acid modificationMethionine aminopeptidase 2Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (45)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
RNA bindingMethionine aminopeptidase 2Homo sapiens (human)
aminopeptidase activityMethionine aminopeptidase 2Homo sapiens (human)
initiator methionyl aminopeptidase activityMethionine aminopeptidase 2Homo sapiens (human)
protein bindingMethionine aminopeptidase 2Homo sapiens (human)
metalloexopeptidase activityMethionine aminopeptidase 2Homo sapiens (human)
metal ion bindingMethionine aminopeptidase 2Homo sapiens (human)
metalloaminopeptidase activityMethionine aminopeptidase 2Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (27)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
cytoplasmMethionine aminopeptidase 2Homo sapiens (human)
cytosolMethionine aminopeptidase 2Homo sapiens (human)
plasma membraneMethionine aminopeptidase 2Homo sapiens (human)
cytoplasmMethionine aminopeptidase 2Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID46864Tested in vitro for its ability to inhibit cell proliferation of calf pulmonary artery endothelial cells measured calorimetrically by SRB method2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Design and synthesis of highly potent fumagillin analogues from homology modeling for a human MetAP-2.
AID486188Antiproliferative activity human Bel7402 cells after 20 hrs by MTT assay2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis and inhibitory evaluation of cyclohexen-2-yl- and cyclohexyl-substituted phenols and quinones to endothelial cell and cancer cells.
AID745731Inhibition of methionine aminopeptidase in HUVEC assessed as increase in unprocessed 14-3-3gamma level at 0.1 to 10 uM by immunoblotting analysis in presence of cycloheximide2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID620248Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.
AID486186Antiproliferative activity HUVEC after 20 hrs by MTT assay2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis and inhibitory evaluation of cyclohexen-2-yl- and cyclohexyl-substituted phenols and quinones to endothelial cell and cancer cells.
AID362336Antiangiogenic activity in chick embryo chorioallantoic membrane assessed as number of eggs showing 3 mm avascular zone at 10 ug2008Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16
TX-2152: a conformationally rigid and electron-rich diyne analogue of FTY720 with in vivo antiangiogenic activity.
AID448541Antiparasitic activity against Plasmodium falciparum W2 infected in human erythrocytes after 72 hrs by FACS2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antiparasitic activities of novel, orally available fumagillin analogs.
AID248343Inhibitory concentration against Lymphoma EC4 cells measured for endothelial cell proliferation activity 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Total synthesis and antiangiogenic activity of cyclopentane analogues of fumagillol.
AID745722Inhibition of methionine aminopeptidase in human HeLa cells assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to DMSO-treated control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID248803Inhibitory concentration against Calf pulmonary artery endothelial cells (CPAE) measured for endothelial cell proliferation activity 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Total synthesis and antiangiogenic activity of cyclopentane analogues of fumagillol.
AID745675Inhibition of methionine aminopeptidase 1 in HDFa cells assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to DMSO-treated control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID486187Antiproliferative activity human A549 cells after 20 hrs by MTT assay2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis and inhibitory evaluation of cyclohexen-2-yl- and cyclohexyl-substituted phenols and quinones to endothelial cell and cancer cells.
AID745726Inhibition of methionine aminopeptidase in HUVEC assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID746915Inhibition of MetAP2 (unknown origin) after 4 hrs2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Synthesis and antitumor activity of 1,3,4-oxadiazole possessing 1,4-benzodioxan moiety as a novel class of potent methionine aminopeptidase type II inhibitors.
AID745720Inhibition of methionine aminopeptidase in human PC3 cells assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to DMSO-treated control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID745729Inhibition of methionine aminopeptidase in HUVEC assessed as increase in unprocessed 14-3-3gamma level at 0.1 to 10 uM by immunoblotting analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID486190Antiproliferative activity human CCC-HPF1 cells after 20 hrs by MTT assay2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis and inhibitory evaluation of cyclohexen-2-yl- and cyclohexyl-substituted phenols and quinones to endothelial cell and cancer cells.
AID620247Antiproliferative activity against human SW1116 cells after 24 hrs by MTT assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.
AID448542Antiparasitic activity against Trypanosoma brucei 427 after 48 hrs2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antiparasitic activities of novel, orally available fumagillin analogs.
AID248394Inhibitory concentration against Murine leukemia P388 measured for endothelial cell proliferation activity 2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Total synthesis and antiangiogenic activity of cyclopentane analogues of fumagillol.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID745660Inhibition of methionine aminopeptidase 1 in HEK293 cells expressing 3xFLAG-tagged BTF3 assessed as increase in [35S]-Met in solution at 100 nM after 30 mins by scintillation counting analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID362337Antiangiogenic activity in chick embryo chorioallantoic membrane assessed as number of eggs showing 3 mm avascular zone at 1 ug2008Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16
TX-2152: a conformationally rigid and electron-rich diyne analogue of FTY720 with in vivo antiangiogenic activity.
AID448540Antiparasitic activity against Entamoeba histolytica HMI:IMSS trophozoites after 60 hrs2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antiparasitic activities of novel, orally available fumagillin analogs.
AID346541Antiangiogenic activity against HUVEC assessed as growth inhibition by NCI antiangiogenesis assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of dihydroartemisinin and dihydroartemisitene acetal dimers showing anticancer and antiprotozoal activity.
AID424804Inhibition of methionine aminopeptidase 22009Journal of natural products, Mar-27, Volume: 72, Issue:3
A selective account of effective paradigms and significant outcomes in the discovery of inspirational marine natural products.
AID620249Inhibition of MetAP2 after 4 hrs2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.
AID362338Antiangiogenic activity in chick embryo chorioallantoic membrane assessed as number of eggs showing 3 mm avascular zone at 5 ug2008Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16
TX-2152: a conformationally rigid and electron-rich diyne analogue of FTY720 with in vivo antiangiogenic activity.
AID745723Inhibition of methionine aminopeptidase in human Jurkat E6-1 cells assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to DMSO-treated control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID270593Inhibition of VEGF and FGF-stimulated angiogenesis in mouse at 30 mg/kg by Matrigel plug assay2006Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo.
AID448543Inhibition of human MetAP2 assessed as residual activity at 800 nM after 8 hrs by Met-AMC based fluorescence assay2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Antiparasitic activities of novel, orally available fumagillin analogs.
AID745724Inhibition of methionine aminopeptidase in HUVEC assessed as accumulation of unprocessed 14-3-3gamma at 1 nM after 24 hrs by immunoblotting analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID745690Inhibition of methionine aminopeptidase 1 in HEK293 cells expressing 3xFLAG-tagged TXNL1 assessed as increase in [35S]-Met in solution at 100 nM after 30 mins by scintillation counting analysis relative to control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID620246Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.
AID154144Tested in vitro for its ability to inhibit cell proliferation of murine leukemia P388D1 cells measured calorimetrically by MTT method2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Design and synthesis of highly potent fumagillin analogues from homology modeling for a human MetAP-2.
AID346542Antiangiogenic activity against HUVEC assessed as inhibition of VEGF-induced cell migration by NCI antiangiogenesis assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of dihydroartemisinin and dihydroartemisitene acetal dimers showing anticancer and antiprotozoal activity.
AID486189Antiproliferative activity human MCF7 cells after 20 hrs by MTT assay2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis and inhibitory evaluation of cyclohexen-2-yl- and cyclohexyl-substituted phenols and quinones to endothelial cell and cancer cells.
AID620245Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.
AID270595Ulceration in mouse at 30 mg/kg2006Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo.
AID270589Antiproliferative activity against BAEC2006Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo.
AID590353Antiproliferative activity against human HUVEC cells after 96 hrs by MTT assay2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Identification, structural properties and chelating capacity of miltipolone as a broad-spectrum inhibitor to cancer cells.
AID424803Inhibition of methionine aminopeptidase 12009Journal of natural products, Mar-27, Volume: 72, Issue:3
A selective account of effective paradigms and significant outcomes in the discovery of inspirational marine natural products.
AID746914Antiproliferative against HUVEC after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Synthesis and antitumor activity of 1,3,4-oxadiazole possessing 1,4-benzodioxan moiety as a novel class of potent methionine aminopeptidase type II inhibitors.
AID270591Inhibition of human MetAP22006Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo.
AID1384754Antiangiogenic activity in Sprague-Dawley rat thoracic aorta ring assessed as inhibition of microvessels outgrowth at 50 uM after 5 days2018Journal of natural products, 08-24, Volume: 81, Issue:8
Antiangiogenic Activity and Chemical Derivatization of the Neurotoxic Acetogenin Annonacin Isolated from Asimina triloba.
AID346543Antiangiogenic activity against HUVEC assessed as inhibition of capillary-like structure formation by NCI antiangiogenesis assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of dihydroartemisinin and dihydroartemisitene acetal dimers showing anticancer and antiprotozoal activity.
AID745721Inhibition of methionine aminopeptidase in HEK293 cells assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to DMSO-treated control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID296847Inhibition of human recombinant MetAP22007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
AID745719Inhibition of methionine aminopeptidase in human MCF7 cells assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to DMSO-treated control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID745717Inhibition of methionine aminopeptidase 1 in HUVEC assessed as increase in ratio of unprocessed 14-3-3gamma to total 14-3-3gamma at 0.1 uM after 24 hrs by immunoblotting analysis relative to DMSO-treated control2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells.
AID296851Growth inhibition of HUVEC cells by XTT assay2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
AID67454Tested in vitro for its ability to inhibit cell proliferation of lymphoma EL-4 cells measured calorimetrically by MTT method2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Design and synthesis of highly potent fumagillin analogues from homology modeling for a human MetAP-2.
AID1799538Enzyme Inhibiton Assay from Article 10.1016/j.chembiol.2009.01.006: \\Fumagillin and fumarranol interact with P. falciparum methionine aminopeptidase 2 and inhibit malaria parasite growth in vitro and in vivo.\\2009Chemistry & biology, Feb-27, Volume: 16, Issue:2
Fumagillin and fumarranol interact with P. falciparum methionine aminopeptidase 2 and inhibit malaria parasite growth in vitro and in vivo.
AID1797624Enzyme Inhibition Assay from Article 10.1021/jm061182w: \\Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.\\2007Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (434)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's191 (44.01)18.2507
2000's204 (47.00)29.6817
2010's36 (8.29)24.3611
2020's3 (0.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.06

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index8.06 (24.57)
Research Supply Index6.19 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (2.10%)5.53%
Reviews46 (9.66%)6.00%
Case Studies2 (0.42%)4.05%
Observational0 (0.00%)0.25%
Other418 (87.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase II Study of Gemcitabine-Based Chemoradiation and TNP-470 for Patients With Locally Advanced, Nonmetastatic Adenocarcinoma of the Pancreas [NCT00038701]Phase 26 participants (Actual)Interventional1999-08-31Terminated(stopped due to Slow accrual.)
A Phase I Study of TNP-470 in the Treatment of AIDS-Associated Kaposi's Sarcoma [NCT00000763]Phase 142 participants InterventionalCompleted
[information is prepared from clinicaltrials.gov, extracted Sep-2024]