Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

[Image: see text] The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putative oncogene. Here we report the discovery of 109 (CCT251921), a potent, selective, and orally bioavailable inhi...

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Gepubliceerd in:J Med Chem
Hoofdauteurs: Mallinger, Aurélie, Schiemann, Kai, Rink, Christian, Stieber, Frank, Calderini, Michel, Crumpler, Simon, Stubbs, Mark, Adeniji-Popoola, Olajumoke, Poeschke, Oliver, Busch, Michael, Czodrowski, Paul, Musil, Djordje, Schwarz, Daniel, Ortiz-Ruiz, Maria-Jesus, Schneider, Richard, Thai, Ching, Valenti, Melanie, de Haven Brandon, Alexis, Burke, Rosemary, Workman, Paul, Dale, Trevor, Wienke, Dirk, Clarke, Paul A., Esdar, Christina, Raynaud, Florence I., Eccles, Suzanne A., Rohdich, Felix, Blagg, Julian
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: American Chemical Society 2016
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5362750/
https://ncbi.nlm.nih.gov/pubmed/26796641
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b01685
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