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Article

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases

9 Dec 2016

Abstract excerpt

Mediator-associated kinases CDK8/19 are context-dependent drivers or suppressors of tumorigenesis. Their inhibition is predicted to have pleiotropic effects, but it is unclear whether this will impact on the clinical utility of CDK8/19 inhibitors. We discovered two series of potent chemical probes with high selectivity for CDK8/19. Despite pharmacodynamic evidence for robust on-target activity, the compounds...

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PMID: 27935476
DOI: 10.7554/elife.20722

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