2. Academic Validation
  3. Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)

  • Chem Commun (Camb). 2017 Jul 4;53(54):7577-7580. doi: 10.1039/c7cc03879h.
Caroline M Robb 1,  Jacob I Contreras,  Smit Kour,  Margaret A Taylor,  Mohammad Abid,  Yogesh A Sonawane,  Muhammad Zahid,  Daryl J Murry,  Amarnath Natarajan,  Sandeep Rana
Affiliations

Affiliation

  • 1 Eppley Institute for Research in Cancer and Allied Diseases, Omaha, Nebraska 68022, USA. anatarajan@unmc.edu sandeep.rana@unmc.edu.
PMID: 28636052 DOI: 10.1039/c7cc03879h
Abstract

Cyclin-dependent kinase 9 (CDK9), a member of the cyclin-dependent protein kinase (CDK) family, is involved in transcriptional elongation of several target genes. CDK9 is ubiquitously expressed and has been shown to contribute to a variety of malignancies such as pancreatic, prostate and breast cancers. Here we report the development of a heterobifunctional small molecule proteolysis targeting chimera (PROTAC) capable of Cereblon (CRBN) mediated proteasomal degradation of CDK9. In HCT116 cells, it selectively degrades CDK9 while sparing other CDK family members. This is the first example of a PROTAC that selectively degrades CDK9.

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