1,3-dioxane-4,6-dione-5-carboxamide-based inhibitors of human group IIA phospholipase A2:: X-ray structure of the complex and interfacial selection of inhibitors from a structural library.

被引：9

作者：

Bryant, MD

Flick, KE

Koduri, RS

Wilton, DC

Stoddard, BL

Gelb, MH

机构：

[1] Fred Hutchinson Canc Res Ctr, Seattle, WA 98104 USA

[2] Univ Washington, Dept Chem, Seattle, WA 98195 USA

[3] Univ Washington, Dept Biochem, Seattle, WA 98195 USA

[4] Univ Southampton, Dept Biochem, Southampton SO9 3TU, Hants, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(99)00147-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A library of 109 1,3-dioxane-4,6-dione-5-carboxamides was prepared by solution-phase methods as potential inhibitors of human group IIa phospholipase A(2). Tight binding inhibitors were found by an interfacial affinity selection method. The crystal structure of the secreted phospholipase A, containing one of the inhibitors was determined, and it reveals the inhibitor-calcium bidendate coordination. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1097 / 1102

页数：6

共 18 条

[1] Distinct roles in signal transduction for each of the phospholipase A(2) enzymes present in P388D(1) macrophages [J].