Analogs of farnesyl pyrophosphate incorporating internal benzoylbenzoate esters: Synthesis, inhibition kinetics and photoinactivation of yeast protein farnesyltransferase

被引：23

作者：

Turek, TC ^{[1
]}

Gaon, I ^{[1
]}

Distefano, MD ^{[1
]}

机构：

[1] UNIV MINNESOTA,DEPT CHEM,MINNEAPOLIS,MN 55455

来源：

TETRAHEDRON LETTERS | 1996年 / 37卷 / 28期

关键词：

D O I：

10.1016/0040-4039(96)00972-0

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The syntheses of two analogs (la and Ib) of farnesyl pyrophosphate incorporating photoactive benzoylbenzoate esters are described. Both la and 1b are competitive inhibitors of yeast protein farnesyltransferase with respect to farnesyl pyrophosphate and have Ki values of 3300 nM and 880 nM, respectively. Upon photolysis for two hours, la and Ib inactivate the enzyme by 46% and 11%, respectively. These compounds should be useful for a variety of studies of protein prenyltransferases. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：4845 / 4848

页数：4

共 17 条

[1]

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