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

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

doi:10.1021/acsmedchemlett.6b00044

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

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Schneider, Elisabeth V.
Huber, Robert / Structure Research, Max Planck Institute of Biochemistry, Max Planck Society;

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引用

Bergeron, P., Koehler, M. F. T., Blackwood, E. M., Bowman, K., Clark, K., Firestein, R., Kiefer, J. R., Maskos, K., McCleland, M. L., Orren, L., Ramaswamy, S., Salphati, L., Schmidt, S., Schneider, E. V., Wu, J., & Beresini, M. (2016). Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. ACS Medicinal Chemistry Letters, 7(6), 595-600. doi:10.1021/acsmedchemlett.6b00044.

引用: https://hdl.handle.net/11858/00-001M-0000-002B-00F9-F

要旨

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.