微管蛋白抑制剂概述，这些抑制剂与秋水仙素结合位点相互作用。
An overview of tubulin inhibitors that interact with the colchicine binding site.
机构信息
Department of Pharmaceutical Sciences, Health Science Center, University of Tennessee, 847 Monroe Ave, Memphis, TN 38163, USA.
出版信息
Pharm Res. 2012 Nov;29(11):2943-71. doi: 10.1007/s11095-012-0828-z. Epub 2012 Jul 20.
Abstract
Tubulin dynamics is a promising target for new chemotherapeutic agents. The colchicine binding site is one of the most important pockets for potential tubulin polymerization destabilizers. Colchicine binding site inhibitors (CBSI) exert their biological effects by inhibiting tubulin assembly and suppressing microtubule formation. A large number of molecules interacting with the colchicine binding site have been designed and synthesized with significant structural diversity. CBSIs have been modified as to chemical structure as well as pharmacokinetic properties, and tested in order to find a highly potent, low toxicity agent for treatment of cancers. CBSIs are believed to act by a common mechanism via binding to the colchicine site on tubulin. The present review is a synopsis of compounds that have been reported in the past decade that have provided an increase in our understanding of the actions of CBSIs.
摘要
微管动力学是新化疗药物的一个有前途的靶点。秋水仙素结合位点是潜在的微管聚合稳定剂的最重要口袋之一。秋水仙素结合位点抑制剂（CBSI）通过抑制微管组装和抑制微管形成来发挥其生物学作用。已经设计和合成了大量与秋水仙素结合位点相互作用的分子，具有显著的结构多样性。CBSI 的化学结构和药代动力学性质都经过了修饰，并进行了测试，以寻找一种高效、低毒的癌症治疗药物。CBSI 被认为通过与微管上的秋水仙素结合位点结合而发挥共同作用。本综述概述了过去十年中报道的化合物，这些化合物增加了我们对 CBSI 作用的理解。
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