Huang Zhi, Wang Tianqi, Wang Cheng, Fan Yan
Department of Medicinal Chemistry, School of Medicine, Nankai University 94 Weijin Road Tianjin 300071 China
Anhui Province Key Laboratory of Medical Physics and Technology, Institute of Health and Medical Technology, Hefei Institutes of Physical Science, Chinese Academy of Sciences Hefei 230031 China.
RSC Med Chem. 2022 Apr 20;13(6):688-710. doi: 10.1039/d2md00040g. eCollection 2022 Jun 22.
Cyclin dependent kinase 9 (CDK9) plays an essential role in regulating transcriptional elongation. Aberrations in CDK9 activity have been observed in various cancers, which make CDK9 an attractive therapeutic target for cancers. This led to an intensive development of small-molecule CDK9 inhibitors or new emerging strategies, such as proteolysis targeting chimeras (PROTACs). Here, we review the CDK9 modulators in cancer not only for research purposes, but also for therapeutic applications.
细胞周期蛋白依赖性激酶9（CDK9）在调节转录延伸中起关键作用。在多种癌症中均观察到CDK9活性异常，这使得CDK9成为极具吸引力的癌症治疗靶点。这促使了小分子CDK9抑制剂或新出现的策略（如靶向嵌合体的蛋白酶体降解技术，PROTACs）的深入研发。在此，我们综述了癌症中的CDK9调节剂，不仅用于研究目的，也用于治疗应用。
