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Discovery of a PCAF Bromodomain Chemical Probe

The p300/CBP‐associated factor (PCAF) and related GCN5 bromodomain‐containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine‐base...

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Detalles Bibliográficos
Autores principales: Moustakim, Moses, Clark, Peter G. K., Trulli, Laura, Fuentes de Arriba, Angel L., Ehebauer, Matthias T., Chaikuad, Apirat, Murphy, Emma J., Mendez‐Johnson, Jacqui, Daniels, Danette, Hou, Chun‐Feng D., Lin, Yu‐Hui, Walker, John R., Hui, Raymond, Yang, Hongbing, Dorrell, Lucy, Rogers, Catherine M., Monteiro, Octovia P., Fedorov, Oleg, Huber, Kilian V. M., Knapp, Stefan, Heer, Jag, Dixon, Darren J., Brennan, Paul E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5412877/
https://www.ncbi.nlm.nih.gov/pubmed/27966810
http://dx.doi.org/10.1002/anie.201610816