Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy

Yogesh A. Sonawane, Margaret A. Taylor, John Victor Napoleon, Sandeep Rana, Jacob I. Contreras, Amarnath Natarajan

Research output: Contribution to journalReview article

60 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)8667-8684
Number of pages18
JournalJournal of Medicinal Chemistry
Volume59
Issue number19
DOIs
StatePublished - Oct 13 2016

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Fingerprint Dive into the research topics of 'Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy'. Together they form a unique fingerprint.

  • Cite this

    Sonawane, Y. A., Taylor, M. A., Napoleon, J. V., Rana, S., Contreras, J. I., & Natarajan, A. (2016). Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. Journal of Medicinal Chemistry, 59(19), 8667-8684. https://doi.org/10.1021/acs.jmedchem.6b00150