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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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4904263 | PMC |
http://dx.doi.org/10.1021/acsmedchemlett.6b00044 | DOI Listing |
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