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新型抗微生物药物的发现进展,这些药物针对细菌细胞分裂蛋白 FtsZ 的组装。

Advances in the discovery of novel antimicrobials targeting the assembly of bacterial cell division protein FtsZ.

机构信息

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, PR China.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, PR China.

出版信息

Eur J Med Chem. 2015 May 5;95:1-15. doi: 10.1016/j.ejmech.2015.03.026. Epub 2015 Mar 14.

Abstract

Currently, wide-spread antimicrobials resistance among bacterial pathogens continues being a dramatically increasing and serious threat to public health, and thus there is a pressing need to develop new antimicrobials to keep pace with the bacterial resistance. Filamentous temperature-sensitive protein Z (FtsZ), a prokaryotic cytoskeleton protein, plays an important role in bacterial cell division. It as a very new and promising target, garners special attention in the antibacterial research in the recent years. This review describes not only the function and dynamic behaviors of FtsZ, but also the known natural and synthetic inhibitors of FtsZ. In particular, the small molecules recently developed and the future directions of ideal candidates are highlighted.

摘要

目前,细菌病原体的广泛抗生素耐药性继续对公共健康构成日益严重的威胁,因此迫切需要开发新的抗生素以跟上细菌耐药性的步伐。丝状温度敏感蛋白 Z(FtsZ)是一种原核细胞骨架蛋白,在细菌细胞分裂中发挥重要作用。作为一个非常新的有前途的靶点,近年来在抗菌研究中引起了特别关注。本综述不仅描述了 FtsZ 的功能和动态行为,还描述了已知的天然和合成 FtsZ 抑制剂。特别强调了最近开发的小分子以及理想候选物的未来方向。

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