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Potential Inhibitors Against NDM-1 Type Metallo-β-Lactamases: An Overview.
Microbial Drug Resistance ( IF 2.6 ) Pub Date : 2020-12-03 , DOI: 10.1089/mdr.2019.0315
Smriti Sharma 1, 2 , Sumit Sharma 2, 3 , Parvinder Pal Singh 2, 3 , Inshad Ali Khan 1, 2
Affiliation  

A new member of the class metallo-β-lactamase (MBL), New Delhi metallo-beta-lactamase 1 (NDM-1) has emerged recently as a leading threat to the treatment of infections that have spread in all major Gram-negative pathogens. The enzyme inactivates antibiotics of the carbapenem family, which are a mainstay for the treatment of antibiotic-resistant bacterial infections. This review provides information about NDM-1 spatial structure, potential features of the active site, and its mechanism of action. It also enlists the inhibitors/compounds/drugs against NDM-1 in various development phases. Understanding their mode of inhibition and the structure-activity relationship would be beneficial for development, synthesis, and even increasing biological efficacy of inhibitors, making them more promising drug candidates.

中文翻译:

NDM-1 型金属-β-内酰胺酶的潜在抑制剂:概述。

金属-β-内酰胺酶 (MBL) 类的新成员新德里金属-β-内酰胺酶 1 (NDM-1) 最近已成为治疗已在所有主要革兰氏阴性病原体中传播的感染的主要威胁. 该酶使碳青霉烯类抗生素失活,碳青霉烯类抗生素是治疗耐抗生素细菌感染的中流砥柱。这篇综述提供了有关 NDM-1 空间结构、活性位点的潜在特征及其作用机制的信息。它还在各个开发阶段招募了针对 NDM-1 的抑制剂/化合物/药物。了解它们的抑制模式和构效关系将有利于抑制剂的开发、合成,甚至提高其生物学功效,使它们成为更有前景的候选药物。
更新日期:2020-12-04
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