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...

Full description

Bibliographic Details
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

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

Similar Items