Dynamic combinatorial mass spectrometry leads to metallo-β-lactamase inhibitors

被引：39

作者：

Lienard, Benoit M. R. ^{[1
,3
]}

Hueting, Rebekka ^{[1
,3
]}

Lassaux, Patricia ^{[2
]}

Galleni, Moreno ^{[2
]}

Frere, Jean-Marie ^{[2
]}

Schofield, Christopher J. ^{[1
,3
]}

机构：

[1] Univ Oxford, Chem Res Lab, Oxford OX1 3TA, England

[2] Univ Liege, Ctr Ingn Proteines, B-4000 Liege, Belgium

[3] OCISB, Oxford OX1 3TA, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 03期

关键词：

D O I：

10.1021/jm070866g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The use of protein ESI mass spectrometry under non-denaturing conditions to analyze a dynamic combinatorial library of thiols/disulfides with the BcII metallo-beta-lactamase enabled the rapid identification of an inhibitor with a K-i of < 1 mu M. The study exemplifies the utility of protein-MS for screening dynamic mixtures of potential enzyme-inhibitors.

引用

页码：684 / 688

页数：5

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