Dynamic Combinatorial Mass Spectrometry Leads to Metallo-β-lactamase Inhibitors

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• 作者：Beno&#xee ; t M. R. Li&#xe9 ; nard ; Rebekka Hü ; ting ; Patricia Lassaux ; Moreno Galleni ; Jean-Marie Fr&#xe8 ; re ; Christopher J. Schofield
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：February 14, 2008
• 年：2008
• 卷：51
• 期：3
• 页码：684 - 688
• 全文大小：446K
• 年卷期：v.51,no.3(February 14, 2008)
• ISSN：1520-4804

文摘

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