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 cer...

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Publicado no:J Med Chem
Main Authors: Gerstenberger, Brian S., Trzupek, John D., Tallant, Cynthia, Fedorov, Oleg, Filippakopoulos, Panagis, Brennan, Paul E., Fedele, Vita, Martin, Sarah, Picaud, Sarah, Rogers, Catherine, Parikh, Mihir, Taylor, Alexandria, Samas, Brian, O’Mahony, Alison, Berg, Ellen, Pallares, Gabriel, Torrey, Adam V., Treiber, Daniel K., Samardjiev, Ivan J., Nasipak, Brian T., Padilla-Benavides, Teresita, Wu, Qiong, Imbalzano, Anthony N., Nickerson, Jeffrey A., Bunnage, Mark E., Müller, Susanne, Knapp, Stefan, Owen, Dafydd R.
Formato: Artigo
Idioma:Inglês
Publicado em: 2016
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5034155/
https://ncbi.nlm.nih.gov/pubmed/27115555
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b00012
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