阅读量：

315

作者：

孙囡囡，周有骏

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摘要：

作用于微管蛋白秋水仙碱位点的抑制剂的研究是目前抗肿瘤药物研究的热点之一.已有十多个药物进入临床研究,显示出良好的开发前景.但该类药物的详细分子作用机制鲜有报道.本文综述了微管蛋白秋水仙碱的结合位点的结构,及其与不同结构类型抑制剂的结合方式,以及由此产生的生物活性和抗肿瘤作用.为深入研究开发这一类靶向微管蛋白的抗肿瘤药物提供参考.;Colchicine bonding site inhibitors (CBSI) as antitumor drugs acting on microtubule achieved a great breakthrough and attracted a lot attention, with more than a dozen drugs in clinical studies, it showed a good prospect. But its molecular mechanism of action has been reported rarely. In order to provide some useful information for the research of this anticancer drugs targeting on colchicine bonding site, this paper reviews the detailed mechanism of how CBSI influences microtubules dynamics to exert anti-tumor activity, including the colchicine binding sites on microtubules, the structural changes when tubulin combined with CSBI, biological effects resulting from structural alterations in tubulin caused by CBSI and the subsequent antineoplastic effects.

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