University of Bristol, School of Chemistry, Cantock's Close, Bristol, BS8 1TS, UK.
Org Biomol Chem. 2022 Oct 12;20(39):7694-7712. doi: 10.1039/d2ob01381a.
Vancomycin is the best-known of the glycopeptide group antibiotics (GPAs), a family of agents which operate by binding the C-terminal deptide D-Ala-D-Ala. This anionic epitope is an interesting target because it plays a central role in bacterial cell wall synthesis, and is not readily modified by evolution. Accordingly, vancomycin has been in use for >60 years but has only provoked limited resistance. Agents which mimic vancomycin but are easier to synthesise and modify could serve as valuable weapons against pathogenic bacteria, broadening the scope of the GPAs and addressing the resistance that does exist. This article gives an overview of vancomycin's structure and action, surveys past work on vancomycin mimicry, and makes the case for renewed effort in the future.
万古霉素是糖肽类抗生素(GPA)中最著名的一种,该类抗生素通过与 C 末端肽 D-Ala-D-Ala 结合而发挥作用。这个带负电荷的表位是一个有趣的靶标,因为它在细菌细胞壁合成中起核心作用,而且不易被进化修饰。因此,万古霉素已经使用了超过 60 年,但只引起了有限的耐药性。模仿万古霉素但更容易合成和修饰的药物可以作为对抗致病菌的有价值武器,扩大 GPA 的范围,并解决现有的耐药性问题。本文概述了万古霉素的结构和作用,调查了过去关于万古霉素模拟的工作,并为未来的研究提出了建议。