4UYF

N-Terminal bromodomain of Human BRD2 with I-BET726 (GSK1324726A)

Summary for 4UYF

• Entry DOI: 10.2210/pdb4uyf/pdb
• Related: 4UYD 4UYE 4UYG 4UYH
• Descriptor: BROMODOMAIN-CONTAINING PROTEIN 2, 1,2-ETHANEDIOL, 4-[(2S,4R)-1-acetyl-4-[(4-chlorophenyl)amino]-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl]benzoic acid, ... (6 entities in total)
• Functional Keywords: transcription, inhibitor, histone, epigenetic reader, bet, brd2, bromodomain
• Biological source: HOMO SAPIENS (HUMAN); More
• Total number of polymer chains: 3
• Total formula weight: 55490.24

Authors

Chung, C.,Bamborough, P.,Gosmini, R. (deposition date: 2014-08-31, release date: 2014-10-08, Last modification date: 2019-05-15)

• Primary citation: Gosmini, R.,Nguyen, V.L.,Toum, J.,Simon, C.,Brusq, J.M.,Krysa, G.,Mirguet, O.,Riou-Eymard, A.M.,Boursier, E.V.,Trottet, L.,Bamborough, P.,Clark, H.,Chung, C.W.,Cutler, L.,Demont, E.H.,Kaur, R.,Lewis, A.J.,Schilling, M.B.,Soden, P.E.,Taylor, S.,Walker, A.L.,Walker, M.D.,Prinjha, R.K.,Nicodeme, E.; The Discovery of I-Bet726 (Gsk1324726A), a Potent Tetrahydroquinoline Apoa1 Up-Regulator and Selective Bet Bromodomain Inhibitor.; J.Med.Chem., 57:8111-, 2014; PubMed: 25249180; DOI: 10.1021/JM5010539

Experimental method

X-RAY DIFFRACTION (1.6 Å)