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基于结构的微管靶向剂的发现和合理设计。

Structure-based discovery and rational design of microtubule-targeting agents.

机构信息

Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut, CH-5232 Villigen PSI, Switzerland; University of Basel, Biozentrum, 4056 Basel, Switzerland.

Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut, CH-5232 Villigen PSI, Switzerland.

出版信息

Curr Opin Struct Biol. 2024 Aug;87:102845. doi: 10.1016/j.sbi.2024.102845. Epub 2024 May 27.

DOI:10.1016/j.sbi.2024.102845
PMID:38805950
Abstract

Microtubule-targeting agents (MTAs) have demonstrated remarkable efficacy as antitumor, antifungal, antiparasitic, and herbicidal agents, finding applications in the clinical, veterinary, and agrochemical industry. Recent advances in tubulin and microtubule structural biology have provided powerful tools that pave the way for the rational design of innovative small-molecule MTAs for future basic and applied life science applications. In this mini-review, we present the current status of the tubulin and microtubule structural biology field, the recent impact it had on the discovery and rational design of MTAs, and exciting avenues for future MTA research.

摘要

微管靶向剂 (MTAs) 已被证明在抗肿瘤、抗真菌、抗寄生虫和除草方面具有显著的疗效,在临床、兽医和农用化学品行业得到了应用。最近在微管蛋白和微管结构生物学方面的进展提供了强大的工具,为未来基础和应用生命科学应用中创新的小分子 MTA 的合理设计铺平了道路。在这篇迷你综述中,我们介绍了微管蛋白和微管结构生物学领域的现状,以及它对 MTA 的发现和合理设计的最新影响,以及未来 MTA 研究的令人兴奋的途径。

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