5EGU
FIRST DOMAIN OF HUMAN BROMODOMAIN BRD4 IN COMPLEX WITH INHIBITOR 3-Butyl-8-(6-butyl-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-ylsulfanylmethyl)-7-ethyl-3,7-dihydropurine-2,6-dione
Summary for 5EGU
Entry DOI | 10.2210/pdb5egu/pdb |
Descriptor | Bromodomain-containing protein 4, 3-butyl-8-[(6-butyl-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfanylmethyl]-7-ethyl-purine-2,6-dione, 1,2-ETHANEDIOL, ... (4 entities in total) |
Functional Keywords | inhibitor, histone, epigenetic reader, bromodomain, brd4, brd4_bd1, brd4_bd1 06-nov, transcription |
Biological source | Homo sapiens (Human) |
Cellular location | Nucleus: O60885 |
Total number of polymer chains | 4 |
Total formula weight | 62398.06 |
Authors | Raux, B.,Rebuffet, E.,Betzi, S.,Priet, S.,Morelli, X. (deposition date: 2015-10-27, release date: 2016-01-20, Last modification date: 2024-01-10) |
Primary citation | Raux, B.,Voitovich, Y.,Derviaux, C.,Lugari, A.,Rebuffet, E.,Milhas, S.,Priet, S.,Roux, T.,Trinquet, E.,Guillemot, J.C.,Knapp, S.,Brunel, J.M.,Fedorov, A.Y.,Collette, Y.,Roche, P.,Betzi, S.,Combes, S.,Morelli, X. Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins. J.Med.Chem., 59:1634-1641, 2016 Cited by PubMed: 26735842DOI: 10.1021/acs.jmedchem.5b01708 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.21 Å) |
Structure validation
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