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

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.

SUBMITTER: Bergeron P

PROVIDER: S-EPMC4904263 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature

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

Bergeron Philippe P Koehler Michael F T MF Blackwood Elizabeth M EM Bowman Krista K Clark Kevin K Firestein Ron R Kiefer James R JR Maskos Klaus K McCleland Mark L ML Orren Linda L Ramaswamy Sreemathy S Salphati Laurent L Schmidt Steve S Schneider Elisabeth V EV Wu Jiansheng J Beresini Maureen M

ACS medicinal chemistry letters 20160405 6

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. ...[more]

PMID: 27326333

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