抗肿瘤新靶点CDK9及其抑制剂的研究进展

Advances in research on a novel antitumor target CDK9 and its inhibitors

摘要: 细胞周期蛋白依赖性激酶9(CDK9)是细胞周期蛋白依赖性激酶家族中的一员。与其他CDKs不同，CDK9主要在转录延伸的调控中发挥作用，而不影响细胞周期过程。目前已有多种CDK9抑制剂进入了临床研究。本文介绍了CDK9的结构特征和作用机制，比较了CDK9与其他CDKs的蛋白结构差异，综述了CDK9非选择性抑制剂和选择性抑制剂的构效关系及研究进展。

Abstract: The cyclin-dependent protein kinase 9(CDK9)is a member of the family of cyclin-dependent protein kinases. Different from other CDKs, CDK9 mainly works on the transcription regulation and has no affects on the cell cycle progress. There are many kinds of CDK9 inhibitors in the clinical research. The detailed structure and action mechanism of CDK9, its difference of protein structure from other CDKs, several selective or nonselective CDK9 inhibitors, as well as their structure-activity relationship(SAR)are discussed in this paper.