Synthesis and evaluation of peptidic maleimides as transglutaminase inhibitors

被引：29

作者：

Halim, Dany ^{[1
]}

Caron, Karine ^{[1
]}

Keillor, Jeffrey W. ^{[1
]}

机构：

[1] Univ Montreal, Dept Chim, Montreal, PQ H3C 3J7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 02期

基金：

加拿大自然科学与工程研究理事会;

关键词：

transglutaminase; maleimide; inhibition kinetics;

D O I：

10.1016/j.bmcl.2006.10.061

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A series of novel transglutaminase inhibitors was prepared, based on the scaffold of a commonly used peptide substrate and bearing an electrophilic maleimide group. These compounds were evaluated in vitro and shown to lead to irreversible inactivation of tissue transglutaminase. Comparison with inhibitors studied previously provides insight into the steric environment of the enzyme active site. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：305 / 308

页数：4

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