Open AccessCyclin Dependent Kinase 9 Inhibitors for Cancer Therapy
Author(s) -
Yogesh A. Sonawane,
Margaret Taylor,
John V. Napoleon,
Sandeep Rana,
Jacob I. Contreras,
Amarnath Natarajan
Publication year - 2016
Publication title -
journal of medicinal chemistry
Language(s) - Uncategorized
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/acs.jmedchem.6b00150
Subject(s) - druggability , cyclin dependent kinase , chemistry , kinase , cyclin dependent kinase 9 , drug discovery , microbiology and biotechnology , in vivo , cancer research , computational biology , cell , protein kinase a , cyclin dependent kinase 2 , biochemistry , biology , cell cycle , genetics , gene
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.