Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit

Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit

The acetyl post-translational modification of chromatin at selected histone lysine residues is interpreted by an acetyl-lysine specific interaction with bromodomain reader modules. Here we report the discovery of the potent, acetyl-lysine-competitive, and cell active inhibitor PFI-3 that binds to ce...

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Main Authors: Gerstenberger, BS, Trzupek, JD, Tallant, C, Fedorov, O, Filippakopoulos, P, Brennan, PE, Fedele, V, Martin, S, Picaud, S, Rogers, C, Parikh, M, Taylor, A, Samas, B, O'Mahony, A, Berg, E, Pallares, G, Torrey, AD, Treiber, DK, Samardjiev, IJ, Nasipak, BT, Padilla-Benavides, T, Wu, Q, Imbalzano, AN, Nickerson, JA, Bunnage, ME, Müller, S, Knapp, S, Owen, DR
Format: Journal article
Language:English
Published: American Chemical Society 2016

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