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

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 of 5-isoxazolyl-ben...

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Main Authors: Hay, D, Fedorov, O, Martin, S, Singleton, D, Tallant, C, Wells, C, Picaud, S, Philpott, M, Monteiro, O, Rogers, C, Conway, S, Rooney, T, Tumber, A, Yapp, C, Filippakopoulos, P, Bunnage, M, Müller, S, Knapp, S, Schofield, C, Brennan, P
格式: Journal article
语言:English
出版: American Chemical Society 2014