期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 19, 页码 8667-8684出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00150
关键词
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资金
- Nebraska Research Initiative
- Fred and Pamela Buffet Cancer Center
- GAANN predoctoral fellowship
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 therapeutic.: 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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