超级细菌NDM-1及其抑制剂的研究进展

An update on New Delhi metallo-β-lactamase-1 and its inhibitors

细菌中抗生素耐药性的迅速发展威胁着将人类带回到"后抗生素时代"。新德里金属β-内酰胺酶(NDM-1)几乎可以水解所有的β-内酰胺抗生素,包括碳青霉烯。携带blaNDM-1基因的细菌被称为超级细菌,至今临床上仍缺乏针对NDM-1的抑制剂。新型NDM-1抑制剂的研发是一个具有挑战性但值得深入研究的领域。本文对NDM-1及其抑制剂研究进展进行阐述,为后续研发提供借鉴。

The rapid development of antibiotic resistance among bacterial pathogens has threatened to take humans back to the"pre-antibiotic era".The New Delhi metallo-β-lactamase(NDM-1)hydrolyzes nearly allβ-lactam antibiotics including carbapenems.Bacterial strains carrying blaNDM-1 gene are termed"superbugs"and clinical inhibitors of NDM-1 have not yet been identified.Discovery of novel NDM-1 inhibitors is a challenging but rewarding research area.This review focuses on the structural characteristics and catalytic mechanisms of NDM-1,and comprehensively summarizes the development of NDM-1 inhibitors in order to facilitate the further development of NDM-1 inhibitors.