Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

The posttranslational modification of chromatin through acetylation at selected histone lysine residues is governed by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The significance of this subset of the epigenetic code is interrogated and interpreted by an acetyllysine-specifi...

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Bibliographic Details
Main Authors: Fish, P, Filippakopoulos, P, Bish, G, Brennan, P, Bunnage, M, Cook, A, Federov, O, Gerstenberger, B, Jones, H, Knapp, S, Marsden, B, Nocka, K, Owen, DR, Philpott, M, Picaud, S, Primiano, M, Ralph, M, Sciammetta, N, Trzupek, J
Format: Journal article
Language:English
Published: 2012