1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

[Image: see text] The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure–activity relationship (SAR) of the first potent, selective series...

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Pubblicato in:ACS Med Chem Lett
Autori principali: Demont, Emmanuel H., Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D., Fallon, David, Gordon, Laurie J., Grandi, Paola, Hobbs, Clare I., Hussain, Jameed, Jones, Emma J., Le Gall, Armelle, Michon, Anne-Marie, Mitchell, Darren J., Prinjha, Rab K., Roberts, Andy D., Sheppard, Robert J., Watson, Robert J.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2014
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4233354/
https://ncbi.nlm.nih.gov/pubmed/25408830
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml5002932
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