Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2016 May 13

PMID 27171036

Citations 50

Authors

Yogesh A Sonawane

Margaret A Taylor

John Victor Napoleon

Sandeep Rana

Jacob I Contreras

Amarnath Natarajan

Affiliations

Soon will be listed here.

Abstract

Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly 2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has emerged as a druggable target for the development of cancer therapeutics. CDK9 plays a crucial role in transcription regulation; specifically, CDK9 mediated transcriptional regulation of short-lived antiapoptotic proteins is critical for the survival of transformed cells. Focused chemical libraries based on a plethora of scaffolds have resulted in mixed success with regard to the development of selective CDK9 inhibitors. Here we review the regulation of CDK9, its cellular functions, and common core structures used to target CDK9, along with their selectivity profile and efficacy in vitro and in vivo.

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