LOCAL CONSTRAINED SHIFTY PSEUDOPEPTIDES INHIBITORS OF RAS-FARNESYL TRANSFERASE

被引：10

作者：

BYK, G ^{[1
]}

DUCHESNE, M ^{[1
]}

PARKER, F ^{[1
]}

LELIEVRE, Y ^{[1
]}

GUITTON, JD ^{[1
]}

CLERC, FF ^{[1
]}

BECQUART, J ^{[1
]}

TOCQUE, B ^{[1
]}

SCHERMAN, D ^{[1
]}

机构：

[1] DEPT BIOTECHNOL, F-94403 VITRY, FRANCE

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期

关键词：

D O I：

10.1016/0960-894X(95)00482-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pseudopeptide analogues related to the C-terminal tetrapeptide of ras-protein (Cys-Val-X-Met) were synthesized and evaluated for inhibition of ras farnesyl transferase (FTase). We demonstrate that the introduction of a shifty amino acid related to Cys instead of Cys-Val and a tetrahydroisoquinoline carboxylic acid (TIC) instead of Phe lead to potent inhibitors of FTase on isolated enzyme or on cell based tests. One of the pseudopeptides, conceived as a prodrug, suppressed specifically the ability of ras transformed cells to form colonies in soft agar.

引用

页码：2677 / 2682

页数：6

共 18 条

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