The first potent inhibitor of mammalian group X secreted phospholipase A2:: Elucidation of sites for enhanced binding

被引：104

作者：

Smart, Brian P. ^{[1
]}

Oslund, Rob C. ^{[1
]}

Walsh, Laura A. ^{[1
]}

Gelb, Michael H. ^{[1
]}

机构：

[1] Univ Washington, Dept Chem & Biochem, Seattle, WA 98195 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 10期

关键词：

D O I：

10.1021/jm060136t

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using the X-ray structure of human group X secreted phospholipase A(2) (hGX), we carried out structure-based design of indole-based inhibitors and prepared the compounds using a new synthetic route. The most potent compound inhibited hGX and the mouse orthologue with an IC50 of 75 nM. This compound is the most potent hGX inhibitor reported to date and was also found to inhibit a subset of the other mouse and human sPLA(2)s.

引用

页码：2858 / 2860

页数：3

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