Chelator Fragment Libraries for Targeting Metalloproteinases

被引：68

作者：

Agrawal, Arpita ^{[3
]}

Johnson, Sherida L. ^{[1
,2
]}

Jacobsen, Jennifer A. ^{[3
]}

Miller, Melissa T. ^{[3
]}

Chen, Li-Hsing ^{[1
,2
]}

Pellecchia, Maurizio ^{[1
,2
]}

Cohen, Seth M. ^{[3
]}

机构：

[1] Burnham Inst Med Res, Canc Res Ctr, La Jolla, CA 92037 USA

[2] Burnham Inst Med Res, Infect & Inflammatory Dis Ctr, La Jolla, CA 92037 USA

[3] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA

来源：

CHEMMEDCHEM | 2010年 / 5卷 / 02期

基金：

美国国家科学基金会; 美国国家卫生研究院;

关键词：

chelators; fragment-based lead design; libraries; metalloproteins; zinc; ANTHRAX LETHAL FACTOR; SMALL-MOLECULE INHIBITORS; ZINC-BINDING GROUPS; HISTONE DEACETYLASE; IDENTIFICATION; DESIGN;

D O I：

10.1002/cmdc.200900516

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(Chemical Equation Presented) A chelator fragment library based on a variety of metal binding groups was screened against a metalloproteinase. Lead hits were identified and an expanded library of select compounds was synthesized, resulting in numerous high-affinity hits against several metalloprotein targets. The findings clearly demonstrate that chelators can be used to generate libraries suitable for fragment-based lead design (FBLD) directed at important metalloproteins. © 2010 Wiley-VCH Verlag GmbH& Co. KGaA.

引用

页码：195 / 199

页数：5

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