4UYD

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 1,3-dimethyl-2-oxo-2,3- dihydro-1H-1,3-benzodiazole-5-carboxamide

Summary for 4UYD

Entry DOI	10.2210/pdb4uyd/pdb
Related	4UYE 4UYF 4UYG 4UYH
Descriptor	BROMODOMAIN-CONTAINING PROTEIN 4, DIMETHYL SULFOXIDE, 1,2-ETHANEDIOL, ... (5 entities in total)
Functional Keywords	transcription, inhibitor, histone, epigenetic reader, antagonist
Biological source	HOMO SAPIENS (HUMAN)
Cellular location	Nucleus: O60885
Total number of polymer chains	1
Total formula weight	18307.00
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 Cited by 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 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.37 Å)

Structure validation