Review Article

Molecular Insights on Selective and Specific Inhibitors of Cyclin Dependent Kinase 9 Enzyme (CDK9) for the Purpose of Cancer Therapy

Author(s):

Dipanjan Karati, Kaka Saheb Ramoo Mahadik, Piyush Trivedi and Dileep Kumar*   Pages 383 - 403 ( 21 )

Abstract:

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.

Keywords:

CDK9, selective CDK9 inhibitors, apoptosis, cyclin T and K, cancer, SAR.

Affiliation:

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