Liu Fan, Meng Hao-yi, Sun Zheng-yang, Li Dan-yang, Jin Yuan-yuan, Yang Zhao-yong, Wu Shao-jie, Chen Jing
Yao Xue Xue Bao. 2017 Mar;52(3):362-70.
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 (MurA-F). Moreover, the reasons for the lack of candidate inhibitors and the challenges to overcome the hurdles are also discussed.
近年来，由于抗生素的滥用，耐药菌株的广泛传播对公众健康构成了严重威胁。这种状况要求开发具有新作用机制的新型抗菌剂。新型抗菌剂数量有限的原因是有效治疗靶点数量少，无法满足当前多重耐药治疗的需求。筛选新靶点是新型抗菌剂开发的关键步骤。肽聚糖是细菌细胞壁的主要成分，对病原菌的生存至关重要。在肽聚糖生物合成的生化途径中，Mur连接酶是本综述中描述的新型抗菌剂开发的极具潜力的靶点。本综述深入探讨了Mur酶（MurA-F）抑制剂领域的最新进展。此外，还讨论了缺乏候选抑制剂的原因以及克服障碍所面临的挑战。
