Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.

The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET (bromodomain and extra terminal domain) bromodomain fa...

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Bibliographic Details
Main Authors: Hewings, D, Fedorov, O, Filippakopoulos, P, Martin, S, Picaud, S, Tumber, A, Wells, C, Olcina, M, Freeman, K, Gill, A, Ritchie, A, Sheppard, D, Russell, A, Hammond, E, Knapp, S, Brennan, P, Conway, S
Format: Journal article
Language:English
Published: 2013