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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Hauptverfasser: 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.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2014
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4183655/
https://ncbi.nlm.nih.gov/pubmed/24946055
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja412434f
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