摘要
金属β-内酰胺酶(MBLs)尤其是NDM-1型金属酶介导的细菌耐药性在全球范围内不断扩散,给人类健康带来日益严重的威胁。虽然使用抑制剂阻止酶的水解作用是临床上应对产β-内酰胺酶耐药菌的重要手段,并已成功上市了奥格门汀等药物,但临床所用抑制剂仅对丝氨酸β-内酰胺酶有效,对MBLs尤其是NDM-1没有效果。本综述概述了近年来NDM-1抑制剂的研究进展,介绍了MBLs抑制剂筛选新方法,以期为研究者们提供新的思路,更有效地设计或筛选出活性较好的MBLs抑制剂。
Metallo-β-1actamases（MBLs）, especially NDM-lmediated antibiotic resistance in the global has bring an increasingly threat to the human health. Although it has been an importent strategy in clinic that use inhibitors to prevent the hydrolysis effect of -β-1actamases produced by -β-1actam resistant bacteria, and has led the successful marketed drugs as Augmentin etc., these drugs only effective on serine-β-1actamases, but has poor effect on MBLs especially NDM-1 type metal-β-Lactamase. In this review, we summarized the current researches on NDM-1 inhibitors, as well as the new screening methods of MBLs inhibitor. We hope to provide researchers with new ideas to effectively design or screen out more MBLs Inhibitors with better activity.
出处
《国外医药（抗生素分册）》
CAS
2018年第2期91-98,共8页
World Notes on Antibiotics
基金
国家基础科学人才培养基金(项目名称:中国药科大学药学基地科研训练及科研能力提高项目,批准号:J1310032)
关键词
金属酶
NDM-1
抑制剂
筛选方法
metallo-β-lactamases
NDM-1 inhibitors
screening methods
