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金属碳青霉烯酶的作用机制及其抑制剂研究进展 被引量:8

Research progress i n catalytic mechanism of metallo-carbapenemases and their inhibitors
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摘要 碳青霉烯类抗生素是临床治疗革兰阴性菌感染的最后一道防线之一。近年来随着碳青霉烯类抗生素在临床的大量使用,以及耐药基因在质粒水平迅速传播,其耐药率逐年上升。造成耐药的原因主要是产生碳青霉烯酶,其中金属碳青霉烯酶属于B类碳青霉烯酶,可以水解除单环β-内酰胺类抗生素之外的几乎所有β-内酰胺类抗生素,目前尚无有效的抑制剂上市。本文就金属碳青霉烯酶的种类结构,作用机制及其抑制剂3个方面作简要综述。 Carbapenems were considered as one of the last line of defense against serious infections caused by Gram-negative pathogens.In recent years,with the wide use of carbapenems in clinical practice and the spread of plasmid-mediated genes of resistance,the incidence of carbapenem-resistant isolates is increasing.The production of carbapenemases is the main cause of drug resistance.Metallo-carbapenemases,belonging to the B subclass of the carbapenemases,are the most versatile family of β-lactamases which are able to hydrolyze carbapenems and almost all other β-lactams,except for aztreonam.There are no effective inhibitors against metallo-carbapenemases for clinical use so far.The structures and catalytic mechanisms of metallo-carbapenemases and their inhibitors were reviewed in this paper.
出处 《中国抗生素杂志》 CAS CSCD 北大核心 2017年第11期923-931,共9页 Chinese Journal of Antibiotics
基金 国家科技部重大新药创制(No.2014ZX09507-002)
关键词 金属碳青霉烯酶 作用机制 酶抑制剂 Metallo-carbapenemases Catalytic mechenism Inhibitors
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