Enzyme Inhibitors: The Best Strategy to Tackle Superbug NDM-1 and Its Variants.
Enzyme Inhibitors: The Best Strategy to Tackle Superbug NDM-1 and Its Variants.
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DOI：
10.3390/ijms23010197
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发表时间：
2021-12-24
影响因子：
5.6
通讯作者：
Zhang X
中科院分区：
文献类型：
--
作者：
Li X;Zhao D;Li W;Sun J;Zhang X
多药细菌耐药性危及临床有效的抗菌治疗，并继续造成重大的公共卫生问题，近年来在世界范围内已升级到前所未有的水平。β-内酰胺类抗生素因其广谱性而成为抗病原菌感染的重要武器。抗生素耐药基因（antibiotic resistance genes，ARGs）的出现严重限制了β-内酰胺类抗生素的应用。其中，新德里金属-β-内酰胺酶-1（NDM-1）由于其底物混杂性、变体的出现和可转移性而代表了最令人不安的发展。鉴于β-内酰胺抗生素与NDM-1介导的耐药性的临床相关性，发现和开发用于NDM-1细菌感染的组合药物（包括NDM-1抑制剂）似乎特别有吸引力和紧迫。本文综述了近年来NDM-1抑制剂的研究进展。详细概括了现有抑制剂的晶体结构、酶活性中心和催化机制、变体和全球分布、作用机制以及支架的开发，为寻找潜在的临床有效的抗耐药菌NDM-1抑制剂提供了参考。
Multidrug bacterial resistance endangers clinically effective antimicrobial therapy and continues to cause major public health problems, which have been upgraded to unprecedented levels in recent years, worldwide. β-Lactam antibiotics have become an important weapon to fight against pathogen infections due to their broad spectrum. Unfortunately, the emergence of antibiotic resistance genes (ARGs) has severely astricted the application of β-lactam antibiotics. Of these, New Delhi metallo-β-lactamase-1 (NDM-1) represents the most disturbing development due to its substrate promiscuity, the appearance of variants, and transferability. Given the clinical correlation of β-lactam antibiotics and NDM-1-mediated resistance, the discovery, and development of combination drugs, including NDM-1 inhibitors, for NDM-1 bacterial infections, seems particularly attractive and urgent. This review summarizes the research related to the development and optimization of effective NDM-1 inhibitors. The detailed generalization of crystal structure, enzyme activity center and catalytic mechanism, variants and global distribution, mechanism of action of existing inhibitors, and the development of scaffolds provides a reference for finding potential clinically effective NDM-1 inhibitors against drug-resistant bacteria.
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