Structure-based design of covalent inhibitors targeting metallo-β-lactamases

被引：9

作者：

Chen, Cheng ^{[1
]}

Yang, Ke-Wu ^{[1
]}

机构：

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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2020年 / 203卷

基金：

中国国家自然科学基金;

关键词：

Antibiotic resistance; Metallo-beta-lactamases; Covalent inhibitor; DELHI METALLO-BETA-LACTAMASE-1 NDM-1; ACID-DERIVATIVES; RESISTANCE; ANTIBIOTICS; HYDROLYSIS; DISCOVERY; COMPLEX; UPDATE; ENZYME;

D O I：

10.1016/j.ejmech.2020.112573

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The emergence and prevalence of metallo-beta-lactamases (M beta Ls)-mediated bacterial resistance has seriously threatened the global health today. M beta Ls are deemed to be one of the most worrying bacterial resistance factors that hydrolyze nearly all beta-lactam antibiotics. However, none of M beta L inhibitors have appeared in clinic to date. This review surveys the common covalent targets in B1 and B2 M beta Ls, summarizes all covalent inhibitors of M beta Ls and their inhibition modes as of 2020, highlights the importance of the rational design of covalent M beta L inhibitor guided by the crystal structure and the development of dual-action covalent M beta L/S beta L inhibitors based on lysine residue of M beta Ls and serine residue of S beta Ls, and describes the approaches to discern the covalent inhibition mechanism to guide the development of future therapeutics. (C) 2020 Elsevier Masson SAS. All rights reserved.

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页数：11

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