Department of Organic Chemistry, Faculty of Chemistry, Warsaw University of Technology, Noakowskiego 3, 00-664, Warsaw, Poland; The Nencki Institute of Experimental Biology Polish Academy of Sciences, Poland.
Department of Organic Chemistry, Faculty of Chemistry, Warsaw University of Technology, Noakowskiego 3, 00-664, Warsaw, Poland.
Biomed Pharmacother. 2021 Jan;133:110973. doi: 10.1016/j.biopha.2020.110973. Epub 2020 Dec 2.
Microtubules (composed of α- and β-tubulin heterodimers) ubiquitous cellular polymers are important components of the cytoskeleton and play diverse roles within the cell, such as maintenance of cell structure, protein trafficking or chromosomal segregation during cell division. The polymers of tubulin play a pivotal role in mitosis and are regarded as an excellent target for chemotherapeutic agents to treat cancer. This review presents a brief overview of the synthesis and mechanism of action of new compounds targeting the dynamic of microtubule - tubulin polymerization/depolymerization. It is divided into the following parts: section I concerns targeting microtubules- tubulin-binding drugs derivatives of stilbene. In section II there are presented photoswitchable inhibitors of microtubule dynamics. Section III concerns using macrocyclic compounds as tubulin inhibitors. In this review, the authors focused primarily on reports produced inthe last five years and the latest strategies in this field.
微管（由α-和β-微管蛋白异二聚体组成）是普遍存在的细胞聚合物，是细胞骨架的重要组成部分，在细胞内发挥多种作用，如维持细胞结构、蛋白质运输或细胞分裂过程中的染色体分离。微管蛋白聚合物在有丝分裂中起着关键作用，被认为是治疗癌症的化疗药物的一个极好靶点。本文简要概述了针对微管-微管蛋白聚合/解聚动力学的新型化合物的合成和作用机制。它分为以下几部分：第一部分涉及靶向微管-微管蛋白结合药物的芪衍生物。第二部分介绍了微管动力学的光开关抑制剂。第三部分涉及大环化合物作为微管蛋白抑制剂的应用。在这篇综述中，作者主要关注了过去五年内的报道和该领域的最新策略。
