靶向秋水仙碱结合位点的基于新型天然产物和优势骨架的微管蛋白抑制剂
Novel Natural Product- and Privileged Scaffold-Based Tubulin Inhibitors Targeting the Colchicine Binding Site.
作者信息
Dong Mengqi, Liu Fang, Zhou Hongyu, Zhai Shumei, Yan Bing
机构信息
School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China.
School of Environment, Guangzhou Key Laboratory of Environmental Exposure and Health and Guangdong Key Laboratory of Environmental Pollution and Health, Jinan University, Guangzhou 510632, China.
出版信息
Molecules. 2016 Oct 15;21(10):1375. doi: 10.3390/molecules21101375.
Tubulin inhibitors are effective anticancer agents, however, there are many limitations to the use of available tubulin inhibitors in the clinic, such as multidrug resistance, severe side-effects, and generally poor bioavailability. Thus, there is a constant need to search for novel tubulin inhibitors that can overcome these limitations. Natural product and privileged structures targeting tubulin have promoted the discovery and optimization of tubulin inhibitors. This review will focus on novel tubulin inhibitors derived from natural products and privileged structures targeting the colchicine binding site on tubulin.
微管蛋白抑制剂是有效的抗癌药物，然而，临床中使用现有的微管蛋白抑制剂存在许多局限性，如多药耐药性、严重的副作用以及普遍较差的生物利用度。因此，一直需要寻找能够克服这些局限性的新型微管蛋白抑制剂。针对微管蛋白的天然产物和优势结构推动了微管蛋白抑制剂的发现和优化。本综述将聚焦于源自天然产物和针对微管蛋白上秋水仙碱结合位点的优势结构的新型微管蛋白抑制剂。
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