Clinical Microbiology Division, Council of Scientific and Industrial Research (CSIR)-Indian Institute of Integrative Medicine, Jammu Tawi, India.
Academy of Scientific and Innovative Research, Council of Scientific and Industrial Research (CSIR)-Indian Institute of Integrative Medicine, Jammu Tawi, India.
Microb Drug Resist. 2020 Dec;26(12):1568-1588. doi: 10.1089/mdr.2019.0315. Epub 2020 Jun 2.
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.
一种新的金属β-内酰胺酶（MBL）成员——新德里金属β-内酰胺酶 1（NDM-1）最近出现，成为所有主要革兰氏阴性病原体传播的感染治疗的主要威胁。该酶使碳青霉烯类抗生素失活，而碳青霉烯类抗生素是治疗抗生素耐药细菌感染的主要药物。本文综述了 NDM-1 的空间结构、活性位点的潜在特征及其作用机制。还列出了处于不同研发阶段的针对 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有助于抑制剂的开发、合成，甚至提高其生物效力，使它们成为更有前途的候选药物。
