吲哚类微管蛋白秋水仙碱结合位点抑制剂的研究进展

Recent Progress in Research on Indole-based Tubulin Inhibitors at Colchicine Binding Sites

癌症威胁着人类健康和生命,开发安全有效的抗肿瘤药物尤为重要.由α-微管蛋白(α-tubulin)与β-微管蛋白(β-tubulin)组装而成的微管是细胞内骨架的主要构成部分,在维持细胞形状、有丝分裂和运动中起着关键作用,是抗肿瘤药物研发的重要靶点之一.本文就吲哚类微管蛋白聚集抑制剂的研究进展进行分类、归纳并总结,期望为高活性微管蛋白秋水仙碱结合位点抑制剂的合理设计提供有用的参考.

Cancer is a threat to human health and life,so it is very important to develop safe and effective anti-tumor drugs.Microtubules,which are assembled byα-tubulin andβ-tubulin,are the major components of the intracellular skeleton and play a key role in maintaining cell shape,mitosis and motility,and are one of the important targets for anti-tumor drug development.In this paper,the research progress of indole tubulin aggregation inhibitors was classified,summarized and expected to provide useful reference for rational design of effective microtubulin polymerization inhibitors for the colchicine binding site.