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

Author:

Kumar Dileep123ORCID,Karati Dipanjan1,Mahadik Kaka Saheb Ramoo1,Trivedi Piyush4

Affiliation:

1. Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be) University, Pune, Maharashtra, 411038, India

2. Department of Entomology, University of California, Davis, One Shields Ave, Davis, CA 95616. USA

3. UC Davis Comprehensive Cancer Centre, University of California, Davis, One Shields Ave, Davis, CA 95616, USA

4. Center for Innovation and Translational Research, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Erandwane, Pune- 411038, Maharashtra, India

Abstract

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 gotten 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.

Publisher

Bentham Science Publishers Ltd.

Subject

Cancer Research,Pharmacology,Molecular Medicine

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