4MR6
Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-208)
Summary for 4MR6
Entry DOI | 10.2210/pdb4mr6/pdb |
Descriptor | Bromodomain-containing protein 2, 1,2-ETHANEDIOL, DIMETHYL SULFOXIDE, ... (5 entities in total) |
Functional Keywords | brd2, ring3, small molecule inhibitor, rvx-208, inhibitor complex, structural genomics consortium, sgc, transcription-transcription inhibitor complex, transcription/transcription inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Nucleus (Probable): P25440 |
Total number of polymer chains | 1 |
Total formula weight | 14010.15 |
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: 24248379DOI: 10.1073/pnas.1310658110 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.67 Å) |
Structure validation
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