依布硒啉作为新型德里金属β-内酰胺酶（NDM-1）的强效共价抑制剂。
Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1).
作者信息
Chiou Jiachi, Wan Shengbiao, Chan Kin-Fai, So Pui-Kin, He Dandan, Chan Edward Wai-chi, Chan Tak-hang, Wong Kwok-yin, Tao Jiang, Chen Sheng
机构信息
Shenzhen Key Laboratory for Food Biological Safety Control, Food Safety and Technology Research Centre, The Hong Kong Polytechnic University, Shenzhen Research Institute, Shenzhen, P.R. China.
出版信息
Chem Commun (Camb). 2015 Jun 11;51(46):9543-6. doi: 10.1039/c5cc02594j.
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.
我们通过基于细胞的筛选方法报告了一种有前景的NDM-1抑制剂依布硒啉的发现。酶动力学研究和电喷雾电离质谱分析表明，依布硒啉可通过与活性位点的半胱氨酸（221）残基形成S-Se键与NDM-1结合，从而展现出具有广谱抑制潜力的新抑制机制。
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