Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)
Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)
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DOI：
10.1039/c5cc02594j
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发表时间：
2015-01-01
影响因子：
4.9
通讯作者：
Chen, Sheng
中科院分区：
文献类型：
--
作者：
Chiou, Jiachi;Wan, Shengbiao;Chen, Sheng
我们报告发现一个有前途的NDM-1抑制剂，ebselen，通过基于细胞的筛选方法。酶促动力学研究和ESI-MS分析表明，依布硒啉通过与NDM-1活性位点的Cys（221）残基形成S-Se键结合，从而表现出一种新的广谱抑制机制。
We report the discovery of a promising NDM-1 inhibitor, ebselen, through a cell-based screening approach. Enzymatic kinetic study and ESI-MS analysis suggested that ebselen could bind to NDM-1 by forming a S-Se bond with the Cys(221) residue at the active site, thereby exhibiting a new inhibition mechanism with broad spectrum inhibitory potential.