摘要
β-内酰胺类抗生素,作为一线抗生素被广泛用于各类细菌感染的临床治疗.由位于质粒的基因blaNDM-1编码的新德里金属-β-内酰胺酶-1可高效水解几乎所有β-内酰胺类抗生素,对β-内酰胺类抗生素的应用造成了极大的威胁,开发有效的抑制剂新德里金属-β-内酰胺酶-1抑制剂迫在眉睫.而抑制剂分子的设计改造工作的开展有赖于对新德里金属-β-内酰胺酶-1结构和催化功能的研究,本综述旨在总结目前有关新德里金属-β-内酰胺酶-1结构、催化机理及其抑制剂的相关研究进展,为基于新德里金属-β-内酰胺酶-1结构的药物分子设计、改造等研究提供帮助.
As the first-line antibiotics,[3 -lactam antibiotics are widely used in the clinical treatment of vari-ous infections. New Delhi metallo- P- lactamase-1 （ NDM -1） encoded by gene blaNDM-1 in plasmid D N A can hydrolyze nearly all kinds of β -lactam antibiotics,posing a critical threat to the application of β- lactamase. It is of great urgency to design novel NDM -1 inhibitors. The design and modification of inhibitor molecules are closely related to the research of both structural information and catalytic mechanism of NDM -1. In this review, structure, catalytic mechanism and inhibitors of NDM -1 all are summarized, which will be helpful for the design and modification of drug molecules targeting NDM -1.
出处
《成都大学学报（自然科学版）》
2017年第2期115-124,共10页
Journal of Chengdu University（Natural Science Edition）
基金
国家自然科学基金(31600591
11247018)资助项目
关键词
细菌耐药
NDM-1
催化机理
抑制剂
药物设计
antimicrobial resistance
NDM -1
catalytic mechanism
inhibitor
drug design
