作用于秋水仙碱位点的微管蛋白抑制剂的研究进展

Progress in the study of tubulin inhibitors binding to the colchicine-site

微管是细胞骨架的主要组成部分,在维持细胞形态、细胞分裂、信号转导等过程中起着重要作用,因此,微管蛋白是一个非常有前景的新型化疗药物的靶标。秋水仙素结合位点抑制剂(CBSIs)通过抑制微管蛋白聚合和抑制微管形成发挥生物效应。近年来,人们对作用于此靶点的抑制剂开展了一系列的研究,并且取得了一定的进展,本文总结了多种不同结构类型的作用于秋水仙碱位点的抑制剂及其研究概况。

Microtubule is one of the key components of the cytoskeleton and plays an important role in the processes of maintaining the cell morphology, cell division, signal transduction, thus tubulin dynamics is a promising target for new chemotherapeutic agents. Colchicine binding site inhibitors（CBSIs） exert their biological effects by inhibiting： tubulin assembly and suppressing microtubule formation. CBSIs have been modi- fied as to improve pharmacokinetic properties, and tested in order to find a highly potent,low toxicity agent for treatment of cancers. This review summarized recent research progress of many kinds of tubulin inhibitors which bind to the colchicine-site with different structures.