细胞周期蛋白依赖激酶9
酶
激酶
癌症研究
生物
癌症治疗
癌症
化学
计算生物学
蛋白激酶A
生物化学
细胞周期蛋白依赖激酶2
遗传学
作者
Dipanjan Karati,Kaka Saheb Ramoo Mahadik,Piyush Trivedi,Dileep Kumar
标识
DOI:10.2174/1871520622666220615125826
摘要
Cyclin Dependent Kinase 9 (CDK9), which controls transcriptional elongation, is a promising pharmacological target for a variety of cancerous cells, specifically those characterized by transcriptional dysregulation. CDK9 promotes the pause or release of RNA polymerase II, a rate-limiting stage in normal transcriptional regulation that is often disturbed in cancers. New indications suggest that selective CDK9 antagonism may be beneficial in the treatment of some cancers. CDK9 modulators (inhibitors and degraders) have gained a lot of attention recently, and many molecules are currently in clinical trials. In this review, the CDK9 antagonists under clinical and preclinical trials have been discussed, as well as the structure-activity relationship has been studied, which will help scientists generate more target- specific drug molecules in the future with less toxicity.
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