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J Med Chem. 2016 Oct 13;59(19):8667-8684. Epub 2016 Jun 3.

Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.

Author information

1
Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center , Omaha, Nebraska 68198-6805, United States.

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.

PMID:
27171036
PMCID:
PMC5636177
DOI:
10.1021/acs.jmedchem.6b00150
[Indexed for MEDLINE]
Free PMC Article

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