4E96
Crystal Structure of the first bromodomain of human BRD4 in complex with the inhibitor PFi-1
Summary for 4E96
Entry DOI | 10.2210/pdb4e96/pdb |
Related | 2OSS |
Descriptor | Bromodomain-containing protein 4, 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide, SODIUM ION, ... (6 entities in total) |
Functional Keywords | bromodomain, cap, hunk1, mcap, mitotic chromosome associated protein, jq1, betsoff1, structural genomics consortium, sgc, cell cycle, protein binding-inhibitor complex, protein binding/inhibitor |
Biological source | Homo sapiens (human) |
Cellular location | Nucleus (By similarity): O60885 |
Total number of polymer chains | 1 |
Total formula weight | 15609.96 |
Authors | Filippakopoulos, P.,Picaud, S.,Felletar, I.,Fedorov, O.,von Delft, F.,Arrowsmith, C.H.,Edwards, A.M.,Weigelt, J.,Fish, P.,Bunnage, M.,Owen, D.,Knapp, S.,Cook, A.,Structural Genomics Consortium (SGC) (deposition date: 2012-03-20, release date: 2012-04-18, Last modification date: 2023-09-13) |
Primary citation | Fish, P.V.,Filippakopoulos, P.,Bish, G.,Brennan, P.E.,Bunnage, M.E.,Cook, A.S.,Federov, O.,Gerstenberger, B.S.,Jones, H.,Knapp, S.,Marsden, B.,Nocka, K.,Owen, D.R.,Philpott, M.,Picaud, S.,Primiano, M.J.,Ralph, M.J.,Sciammetta, N.,Trzupek, J.D. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J.Med.Chem., 55:9831-9837, 2012 Cited by PubMed: 23095041DOI: 10.1021/jm3010515 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.92 Å) |
Structure validation
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