Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8

Philippe Bergeron, Michael F.T. Koehler, Elizabeth M. Blackwood, Krista Bowman, Kevin Clark, Ron Firestein, James R. Kiefer, Klaus Maskos, Mark L. McCleland, Linda Orren, Sreemathy Ramaswamy, Laurent Salphati, Steve Schmidt, Elisabeth V. Schneider, Jiansheng Wu, Maureen Beresini

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

Abstract

Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.

Original languageEnglish
Pages (from-to)595-600
Number of pages6
JournalACS Medicinal Chemistry Letters
Volume7
Issue number6
DOIs
Publication statusPublished - Jun 2016
Externally publishedYes

Keywords

  • CDK8
  • DMG-out
  • inhibitor
  • Sorafenib

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