微管蛋白秋水仙碱位点抑制剂研究进展

Recent Development of Colchicine Binding Site Inhibitors

微管蛋白是细胞骨架的主要成分,参与了细胞过程的许多环节。秋水仙碱位点抑制剂(CSIs)是一类重要的微管蛋白聚合抑制剂。目前已经有许多CSIs作为抗肿瘤药物被发现或设计、合成,并取得了很大的进展。本研究主要就CSIs的作用机制、共同结构特征以及各种类型CSIs的构效关系作一综述。

Microtubules are cytoskeletal components which play important roles in a number of cellular processes.Colchicine binding site inhibitors（CSIs） is one of the major classes of tubulin polymerization inhibitors.Many CSIs have been discovered,designed or synthesized as anticancer agents in the past several years and great progress has been made.We discuss the insights gained so far relevant to the mechanism of CSIs and their common structures.The recent development of CSIs with their biological activity and structure-activity relationship is also reviewed.