4MR4

Crystal Structure of the first bromodomain of human BRD4 in complex with a quinazolinone ligand (RVX-208)

Summary for 4MR4

Entry DOI	10.2210/pdb4mr4/pdb
Related	4MR3 4MR5 4MR6
Descriptor	Bromodomain-containing protein 4, 1,2-ETHANEDIOL, 2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxyquinazolin-4(3H)-one, ... (4 entities in total)
Functional Keywords	brd4, cap, hunk1, mcap, mitotic chromosome associated protein, brd, small molecule inhibitor, rvx-208, structural genomics consortium, sgc, transcription-transcription inhibitor complex, transcription/transcription inhibitor
Biological source	Homo sapiens (human)
Cellular location	Nucleus: O60885
Total number of polymer chains	1
Total formula weight	15655.98
Authors	Filippakopoulos, P.,Picaud, S.,Felletar, I.,Martin, S.,Fedorov, O.,von Delft, F.,Arrowsmith, C.H.,Edwards, A.M.,Weigelt, J.,Bountra, C.,Knapp, S.,Structural Genomics Consortium (SGC) (deposition date: 2013-09-17, release date: 2013-11-27, Last modification date: 2023-09-20)
Primary citation	Picaud, S.,Wells, C.,Felletar, I.,Brotherton, D.,Martin, S.,Savitsky, P.,Diez-Dacal, B.,Philpott, M.,Bountra, C.,Lingard, H.,Fedorov, O.,Muller, S.,Brennan, P.E.,Knapp, S.,Filippakopoulos, P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc.Natl.Acad.Sci.USA, 110:19754-19759, 2013 Cited by PubMed: 24248379 DOI: 10.1073/pnas.1310658110 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.66 Å)

Structure validation