RATIONAL DESIGN OF POTENT CARBOXYLIC-ACID BASED BISUBSTRATE INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE

被引：30

作者：

BHIDE, RS

PATEL, DV

PATEL, MM

ROBINSON, SP

HUNIHAN, LW

GORDON, EM

机构：

[1] Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton

[2] Bristol-Meyers Squibb Pharmaceutical Research Institute, Wallingford

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(01)80111-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Bisubstrate analog inhibitors in which a substrate mimetic tripeptide is attached to a homologated farnesyl carboxylic acid were synthesized and evaluated for in vitro inhibition versus ras farnesyl protein transferase (FPT). Our results demonstrate that such bisubstrate analogs are potent inhibitors of FPT.

引用

页码：2107 / 2112

页数：6

共 12 条

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