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Development of a selective CDK7 covalent inhibitor reveals predominant cell cycle phenotype

Cyclin-dependent kinase 7 (CDK7) regulates both cell cycle and transcription, but its precise role remains elusive. We previously described THZ1, a CDK7 inhibitor, which dramatically inhibits super-enhancer associated gene expression. However, potent CDK12/13 off-target activity obscured CDK7s contr...

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Detalhes bibliográficos
Publicado no:Cell Chem Biol
Main Authors: Olson, Calla M., Liang, Yanke, Leggett, Alan, Park, Woojun D., Li, Lianbo, Mills, Caitlin E., Elsarrag, Selma Z., Ficarro, Scott B., Zhang, Tinghu, Düster, Robert, Geyer, Matthias, Sim, Taebo, Marto, Jarrod A., Sorger, Peter K., Westover, Ken D., Lin, Charles Y., Kwiatkowski, Nicholas, Gray, Nathanael S.
Formato: Artigo
Idioma:Inglês
Publicado em: 2019
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6588464/
https://ncbi.nlm.nih.gov/pubmed/30905681
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.chembiol.2019.02.012
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