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

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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.

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

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Publication details

The article was received on 19 May 2017, accepted on 14 Jun 2017 and first published on 14 Jun 2017


Article type: Communication
DOI: 10.1039/C7CC03879H
Citation: Chem. Commun., 2017, Advance Article
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    Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)

    C. M. Robb, J. I. Contreras, S. Kour, M. A. Taylor, M. Abid, Y. A. Sonawane, M. Zahid, D. J. Murry, A. Natarajan and S. Rana, Chem. Commun., 2017, Advance Article , DOI: 10.1039/C7CC03879H

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