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Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains

[Image: see text] Small-molecule inhibitors that target bromodomains outside of the bromodomain and extra-terminal (BET) sub-family are lacking. Here, we describe highly potent and selective ligands for the bromodomain module of the human lysine acetyl transferase CBP/p300, developed from a series o...

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Detalles Bibliográficos
Autores principales: Hay, Duncan A., Fedorov, Oleg, Martin, Sarah, Singleton, Dean C., Tallant, Cynthia, Wells, Christopher, Picaud, Sarah, Philpott, Martin, Monteiro, Octovia P., Rogers, Catherine M., Conway, Stuart J., Rooney, Timothy P. C., Tumber, Anthony, Yapp, Clarence, Filippakopoulos, Panagis, Bunnage, Mark E., Müller, Susanne, Knapp, Stefan, Schofield, Christopher J., Brennan, Paul E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4183655/
https://www.ncbi.nlm.nih.gov/pubmed/24946055
http://dx.doi.org/10.1021/ja412434f