Inhibitors of protein prenylation 2000

被引：47

作者：

Bell, IM ^{[1
]}

机构：

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

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2000年 / 10卷 / 12期

关键词：

cancer therapy; farnesyltransferase; farnesyltransferase inhibitor; geranylgeranyltransferase; protein prenylation; ras oncogene;

D O I：

10.1517/13543776.10.12.1813

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The development of farnesyltransferase inhibitors (FTIs) was conceived of as a rational approach to the design of new cancer chemotherapeutics and the first examples of this class are currently being evaluated in Phase II and Phase III clinical trials. This review summarises the scientific and patent literature published in the 14 month period from March 1999, since the previous review [1]. In addition to a survey of novel prenyl transferase inhibitors, recent clinical data and developments in related biochemistry and biology are described.

引用

页码：1813 / 1831

页数：19

共 72 条

[51]

2-6

[52] Probing the hydrophobic pocket of farnesyltransferase: Aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors [J].