4UYE

BROMODOMAIN OF HUMAN BRPF1 WITH N-1,3-dimethyl-2-oxo-6-(piperidin-1- yl)-2,3-dihydro-1H-1,3-benzodiazol-5-yl-2-methoxybenzamide

Summary for 4UYE

• Entry DOI: 10.2210/pdb4uye/pdb
• Related: 4UYD 4UYF 4UYG 4UYH
• Descriptor: PEREGRIN, 1,2-ETHANEDIOL, N-[1,3-dimethyl-2-oxo-6-(piperidin-1-yl)-2,3-dihydro-1H-benzimidazol-5-yl]-2-methoxybenzamide, ... (4 entities in total)
• Functional Keywords: transcription, inhibitor, histone, epigenetic reader, antagonist
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Nucleus : P55201
• Total number of polymer chains: 2
• Total formula weight: 28702.84

Authors

Chung, C.,Bamborough, P.,Demont, E. (deposition date: 2014-08-30, release date: 2014-09-17, Last modification date: 2024-05-08)

Primary citation

Demont, E.H.,Bamborough, P.,Chung, C.W.,Craggs, P.D.,Fallon, D.,Gordon, L.J.,Grandi, P.,Hobbs, C.I.,Hussain, J.,Jones, E.J.,Le Gall, A.,Michon, A.M.,Mitchell, D.J.,Prinjha, R.K.,Roberts, A.D.,Sheppard, R.J.,Watson, R.J.
1,3-Dimethyl Benzimidazolones are Potent, Selective Inhibitors of the Brpf1 Bromodomain.
Acs Med.Chem.Lett., 5:1190-, 2014

PubMed Abstract: 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 of inhibitors of the BRPF1 bromodomain.

PubMed: 25408830
DOI: 10.1021/ML5002932

Experimental method

X-RAY DIFFRACTION (1.65 Å)