Concepedia

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 K. Bowman, Kevin Clark, Ron Firestein, James R. Kiefer, K. Maskos, Mark L. McCleland, Linda Orren,

ACS Medicinal Chemistry Letters · 2016 · 62 citations · 15 references

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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.

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