Farnesyltransferase inhibitors versus Ras inhibitors

被引：74

作者：

Gibbs, JB ^{[1
]}

Graham, SL ^{[1
]}

Hartman, GD ^{[1
]}

Koblan, KS ^{[1
]}

Kohl, NE ^{[1
]}

Omer, CA ^{[1
]}

Oliff, A ^{[1
]}

机构：

[1] Merck Res Labs, W Point, PA 19486 USA

来源：

CURRENT OPINION IN CHEMICAL BIOLOGY | 1997年 / 1卷 / 02期

关键词：

D O I：

10.1016/S1367-5931(97)80010-5

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Over the past few yeats, the idea that farnesyl-protein transferase (FPTase) inhibitors might be effective antiproliferative/antitumor agents has been realized in studies of cultured cells and in rodent models of cancer. Most of the studies with FPTase inhibitors have focused on inhibiting the growth of ras-transformed cells in vitro or the growth of ras-dependent tumors in mice. More recently, it has been recognized that the antiproliferative effect of FPTase inhibitors may extend beyond ras-driven tumors. It now seems likely that the ability of FPTase inhibitors to reverse the malignant phenotype results, at least in part, from inhibiting the farnesylation of proteins other than Ras. (C) Current Biology Ltd ISSN 1367-5931.

引用

页码：197 / 203

页数：7

共 51 条

[1]

Bernhard EJ, 1996, CANCER RES, V56, P1727

[2] Modulation of Ras and a-factor function by carboxyl-terminal proteolysis [J].