摘要
近年来,由于抗生素的滥用,使耐药菌株广泛出现,已成为威胁人类健康的重大问题。研发具有新的作用机制的抗菌药物迫在眉睫。抗菌药物资源匮乏,究其原因,主要是由于有效的药物作用靶点数量不足,远远不能满足当前防治的需要。因此抗菌药物作用靶标的筛选是新型抗菌药物研发的关键一步。细菌细胞壁的主要成分是肽聚糖,肽聚糖是病原菌生存所必需的。Mur酶(Mur A-F)是肽聚糖生物合成必不可少的酶,可以以此为靶标发现新的抗生素。本文详细介绍了Mur A-F抑制剂的研究现状,并总结了临床上缺少成功抑制剂的原因和所面临的挑战。
In recent years, owing to the abuse of antibiotics, the widespread of resistant bacterial strains became a serious threat to public health. This status demands development of new antibacterial agents with novel mechanisms of action. The reason for the limited new antibacterials is the small number of effective therapeutic targets, which cannot meet the current needs for the multiple drug-resistant treatment. Screening for new targets is the key step in the development of novel antibacterial agents. Peptidoglycan is the main component of the cell wall of bacteria, which is essential for survival of pathogenic bacteria. Within the biochemical pathway for peptidoglycan biosynthes is the Murligases, described in this review as highly potential targets for the development of new classes of antibacterial agents. This review provides an in-depth insight into the recent developments in the field of inhibitors of the Mur enzymes（Mur A-F）. Moreover, the reasons for the lack of candidate inhibitors and the challenges to overcome the hurdles are also discussed.
出处
《药学学报》
CAS
CSCD
北大核心
2017年第3期362-370,共9页
Acta Pharmaceutica Sinica
基金
北京市自然科学基金(7164279)
NSFC-NIH(中美)国际合作与交流项目(81261120417)
关键词
肽聚糖
抗生素
Mur酶
酶抑制剂
药物发现
peptidoglycan
antibiotics
Mur enzyme
enzyme inhibitor
drug discovery
