Disulfiram as a potent metallo-β-lactamase inhibitor with dual functional mechanisms

被引：36

作者：

Chen, Cheng ^{[1
]}

Yang, Ke-Wu ^{[1
]}

Wu, Lin-Yu ^{[2
]}

Li, Jia-Qi ^{[1
]}

Sun, Le-Yun ^{[1
]}

机构：

[1] Northwest Univ, Coll Chem & Mat Sci, Innovat Lab Chem Biol, Minist Educ,Key Lab Synthet & Nat Funct Mol Chem, Xian 710127, Peoples R China

[2] Northwest Normal Univ, Coll Chem & Chem Engn, Lanzhou 730070, Gansu, Peoples R China

来源：

CHEMICAL COMMUNICATIONS | 2020年 / 56卷 / 18期

基金：

中国国家自然科学基金;

关键词：

Chemical bonds - Zinc compounds;

D O I：

10.1039/c9cc09074f

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

We report a promising NDM-1 inhibitor, disulfiram, which can covalently bind to NDM-1 by forming an S-S bond with the Cys208 residue. Its copper-containing metabolite in vivo, Cu(DTC)(2), also inactivated NDM-1 through oxidizing the Zn(ii) thiolate site of the enzyme, therefore exhibiting dual functional inhibitory potential against B1 and B2 subclass M beta Ls.

引用

页码：2755 / 2758

页数：4

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