3ZYU

Crystal Structure of the first bromodomain of human BRD4 in complex with I-BET151(GSK1210151A)

Summary for 3ZYU

• Entry DOI: 10.2210/pdb3zyu/pdb
• Descriptor: BROMODOMAIN-CONTAINING PROTEIN 4, 1,2-ETHANEDIOL, 7-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)-8-METHOXY-1-[(1R)-1-(PYRIDIN-2-YL)ETHYL]-1H,2H,3H-IMIDAZO[4,5-C]QUINOLIN-2-ONE, ... (4 entities in total)
• Functional Keywords: signaling protein, bromodomain, i-151, inhibitor, histone, epigenetic reader
• Biological source: HOMO SAPIENS (HUMAN)
• Cellular location: Nucleus (By similarity): O60885
• Total number of polymer chains: 2
• Total formula weight: 31464.13

Authors

Chung, C.W.,Mirguet, O. (deposition date: 2011-08-25, release date: 2011-11-02, Last modification date: 2023-12-20)

• Primary citation: Dawson, M.A.,Prinjha, R.K.,Dittman, A.,Giotopoulos, G.,Bantscheff, M.,Chan, W.I.,Robson, S.C.,Chung, C.W.,Hopf, C.,Savitski, M.M.,Huthmacher, C.,Gudgin, E.,Lugo, D.,Beinke, S.,Chapman, T.D.,Roberts, E.J.,Soden, P.E.,Auger, K.R.,Mirguet, O.,Doehner, K.,Delwel, R.,Burnett, A.K.,Jeffrey, P.,Drewes, G.,Lee, K.,Huntly, B.J.,Kouzarides, T.; Inhibition of Bet Recruitment to Chromatin as an Effective Treatment for Mll-Fusion Leukaemia.; Nature, 478:529-, 2011; PubMed: 21964340; DOI: 10.1038/NATURE10509

Experimental method

X-RAY DIFFRACTION (1.5 Å)