自然杂志 ›› 2021, Vol. 43 ›› Issue (5): 335-342.doi: 10.3969/j.issn.0253-9608.2021.05.003

• 免疫化学专刊 • 上一篇    下一篇

抗结核药物靶点的结构研究进展

陈晓博 ①② ,李俊 ①②   

  1. ①上海科技大学 免疫化学研究所,上海 201210;②上海科技大学 生命科学与技术学院,上海 201210
  • 收稿日期:2021-06-16 出版日期:2021-10-22 发布日期:2021-10-22
  • 通讯作者: 李俊,通信作者,研究方向:结构生物学。E-mail: lijun1@shanghaitech.edu.cn

Progress on structures of anti-tuberculosis drug targets

CHEN Xiaobo , LI Jun   

  1. ①Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, China; ②School of Life
    Science and Technology, ShanghaiTech University, Shanghai 201210, China
  • Received:2021-06-16 Online:2021-10-22 Published:2021-10-22

摘要: 结核病(tuberculosis)是一种严重威胁人类生命健康的传染性疾病,主要由结核分枝杆菌( Mycobacterium tuberculosis )感染引起。当前结核病的耐药性问题突出,新药的研发刻不容缓。研究抗结核药物靶点的结构将助力药物的开发工作。文章总结了在结核杆菌细胞壁合成和能量代谢这两个重要生理过程中关键药物靶点的最新结构研究进展,分析了这些膜蛋白及其复合物的结构与功能的关系和已知药物分子作用于靶点的精确作用方式,以及对于抗结核新药设计的重要价值。

关键词: 结核病, 药物靶点, 结构生物学, 细胞壁, 糖基转移酶, 呼吸链

Abstract: Tuberculosis, mainly caused by the pathogenic bacteria Mycobacterium tuberculosis , is an infectious disease that seriously threats human life and health. The even worse situation currently is the drug resistance problem. Thus, new anti-tuberculosis drugs are urgently needed. Studies on the structures of anti-tuberculosis drug targets will assist in drug development. This paper summarizes
the latest research progress on structures of the crucial drug targets involved in the two important physiology processes of cell wall biosynthesis and energy metabolism in Mycobacterium tuberculosis , and also analyzes the structure-function relation of these
membrane proteins and their complexes as well as the precise mode of actions of the known drug molecules on these targets, and the important value for the design of new anti-tuberculosis drugs.