Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.

Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging BAZ2B bromodomain u...

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Main Authors: Ferguson, F, Fedorov, O, Chaikuad, A, Philpott, M, Muniz, JR, Felletar, I, von Delft, F, Heightman, T, Knapp, S, Abell, C, Ciulli, A
格式: Journal article
語言:English
出版: 2013