(-)-FR182877 is a potent and selective inhibitor of carboxylesterase-1

被引：49

作者：

Adam, GC

Vanderwal, CD

Sorensen, EJ

Cravatt, BF

机构：

[1] Skaggs Inst Chem Biol, La Jolla, CA 92037 USA

[2] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA

[3] Scripps Res Inst, Dept Cell Biol, La Jolla, CA 92037 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 44期

关键词：

activity-based profiling; hydrolases; inhibitors; natural products; proteomics;

D O I：

10.1002/anie.200352576

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Activity-based profiling and reporter-group-tagged compounds were used to identify carboxylesterase-1 (CE-1) as a specific target of the natural product (-)-FR182877 (see scheme). Now that a target is known, specific modification of the lactone natural product may lead to even more effective inhibitors of CE-1.

引用

页码：5480 / 5484

页数：5

共 42 条

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