细胞周期蛋白依赖性激酶-9及其抑制剂的研究进展

Advances in research of CDK9 and their inhibitors

细胞周期蛋白依赖性激酶-9(cyclin-dependent kinase-9,CDK9)是一种丝氨酸/苏氨酸蛋白激酶,在细胞转录过程中起着重要的作用。它的活化能够磷酸化RNA聚合酶Ⅱ的C-末端结构域和一些转录因子,进而促进转录延长。最近研究表明,CDK9与艾滋病、癌症、炎症等疾病的发病过程有关。因此,CDK9有望成为治疗这些疾病的新靶点。本文综述了CDK9在这些病理过程中所起到的作用以及当前CDK9抑制剂的研究进展,旨在为CDK9抑制剂类抗肿瘤药物的研发提供参考。

Cyclin-dependent kinase 9（ CDK9） is a kind of Ser/Thr kinase,playing a crucial role in transcription regulation. Its activation can phosphorylate the C-teriminal domain of RNA polymerase-Ⅱ and some transcription regulations factors,in turn promote the elongation of transcription. Recently,studies show that CDK9 is associated with some pathological processes such as AIDs,cancer,inflammation. As such,CDK9 is expected to become a new therapeutic target for these diseases prevention and/or treatment. This review highlights the roles of CDK9 in these pathological processes and the research progress of CDK9 inhibitors,with the aim to provide a guidance for further research in CDK9 inhibitors.