微管蛋白活性抑制剂研究进展

Development of Research on Microtubule Inhibitors

由微管蛋白聚集而成的微管是组成纺锤体的主要成分．微管蛋白聚集或微管解聚的抑制将导致细胞有丝分裂中止．很多天然产物通过结合在微管蛋白的ＣＬＣ部位或ＶＬＢ部位而抑制其聚集；少数化合物通过抑制微管的解聚而使细胞有丝分裂中止．本文对近年来微管活性抑制剂的研究进展进行了总结，着重讨论了化合物结构和活性的关系以及新的抑制微管活性化合物．大多数微管活性抑制剂都是抗肿瘤活性化合物．以微管蛋白为靶点筛选抗肿瘤药物是有效的途径之一．

Microtubule is the major component of the spindle.Inhibition of the assembly or disassembly on the protein tubulin,which is the dominant part of microtubules,can cause cells to be arrested in the mitosis stage.Many natural products inhibit the tubulin's polymerization by binding onto its CLC site or VLB site,while a few compounds show their inhibitive action by halting microtubule's disassembly.This review reports the research development of the microtubule inhibitors in recent years,particularly stressing the structure activity relationship and novel antimicrotubule active compounds derived from natural sources.Most of microtubule inhibitors are also anticancer agents.Using the microtubule inhibition mode is an effective method for screening anticancer drugs.