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Drug-Target Interaction

Drug

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PubChem ID:159324
Structure:
Synonyms:
(R)-( )-R-115777
(R)-( )-R115777
(R)-6-(Amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone
192185-72-1
1x81
2 (1H))-Quinolinone,6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-, 2(1H )-quinolinone
6-[(R)-amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chloro
6-[(R)-amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one
6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE
D03720
JAN
LS-184411
LS-187005
LS-187640
NSC-702818
R-115777
R115777
Tipifarnib
Tipifarnib (USAN/INN)
Tipifarnib [USAN]
Zarnestra

Target

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Uniprot ID:Q6GXA5_MOUSE
Synonyms:
Matrix metalloproteinase 2
EC-Numbers:-
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

14676133
The farnesyltransferase inhibitor R115777 reduces hypoxia and matrix metalloproteinase 2 expression in human glioma xenograft.. Caroline Delmas; Dave End; Philippe Rochaix; Gilles Favre; Christine Toulas; Elizabeth Cohen-Jonathan (2003) Clinical cancer research : an official journal of the American Association for Cancer Research display abstract
PURPOSE: The high-grade primary brain tumors, glioblastoma, of extremely bad prognosis contain large regions of hypoxia known to be involved in the chemo- and radioresistance. We demonstrated previously that radioresistant human wild-type Ras U87 glioblastoma can be radiosensitized in vitro by the specific farnesyltransferase inhibitor R115777. The aim of this study was to analyze the effect of this compound on the hypoxic status and the vascularization of this tumor. EXPERIMENTAL DESIGN: U87 xenografts bearing mice were treated with 100 mg/kg of R115777 b.i.d. during 4 days. Hypoxia was assessed by measuring the binding of hypoxic cell marker pentafluorinated 2-nitroimidazole. Immunohistochemistry was performed to analyze angiogenesis and metalloproteinase-2 expression. RESULTS: We demonstrated here that R115777 treatment induced a significant oxygenation of U87 xenografts (P