Cargando…
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease
There is unmet need for chemical tools to explore the role of the Mediator complex in human pathologies ranging from cancer to cardiovascular disease. Here we determine that CCT251545, a small molecule WNT-pathway inhibitor discovered through cell-based screening, is a potent and selective chemical...
Autores principales: | Dale, Trevor, Clarke, Paul A., Esdar, Christina, Waalboer, Dennis, Adeniji-Popoola, Olajumoke, Ortiz-Ruiz, Maria-Jesus, Mallinger, Aurélie, Samant, Rahul S., Czodrowski, Paul, Musil, Djordje, Schwarz, Daniel, Schneider, Klaus, Stubbs, Mark, Ewan, Ken, Fraser, Elizabeth, TePoele, Robert, Court, Will, Box, Gary, Valenti, Melanie, de Haven Brandon, Alexis, Gowan, Sharon, Rohdich, Felix, Raynaud, Florence, Schneider, Richard, Poeschke, Oliver, Blaukat, Andree, Workman, Paul, Schiemann, Kai, Eccles, Suzanne A., Wienke, Dirk, Blagg, Julian |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
2015
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4677459/ https://www.ncbi.nlm.nih.gov/pubmed/26502155 http://dx.doi.org/10.1038/nchembio.1952 |
Ejemplares similares
-
Discovery of Potent,
Selective, and Orally Bioavailable
Small-Molecule Modulators of the Mediator Complex-Associated Kinases
CDK8 and CDK19
por: Mallinger, Aurélie, et al.
Publicado: (2016) -
2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with
Potent, Selective Affinity for CDK8/19
por: Mallinger, Aurélie, et al.
Publicado: (2016) -
Discovery of Potent, Orally
Bioavailable, Small-Molecule
Inhibitors of WNT Signaling from a Cell-Based Pathway Screen
por: Mallinger, Aurélie, et al.
Publicado: (2015) -
Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases
por: Clarke, Paul A, et al.
Publicado: (2016) -
Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor
por: Whittaker, Steven R., et al.
Publicado: (2018)