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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, the emergence of drug-resistant strains due to the abuse of antibiotics has become a major issue that threatens human health. It is imminent to develop antibacterial drugs that have a new mechanism of action. The lack of antibacterial drug resources, the reason is mainly due to the lack of effective drug targets, far from meeting the needs of the current prevention and treatment. Therefore, the screening of antimicrobial drug targets is a key step in the development of new antimicrobial drugs. The main component of the bacterial cell wall is peptidoglycan, which is necessary for the survival of pathogenic bacteria. Mur A-F is an enzyme essential for peptidoglycan biosynthesis and can be used as a target for the discovery of new antibiotics. This article describes in detail the current state of research on Mur A-F inhibitors and summarizes the reasons and challenges of the lack of successful inhibitors clinically.