5O3A

Human Brd2(BD2) mutant in complex with ET

Summary for 5O3A

• Entry DOI: 10.2210/pdb5o3a/pdb
• Descriptor: Bromodomain-containing protein 2, methyl (2R)-2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]butanoate (3 entities in total)
• Functional Keywords: the bromodomain and extra-terminal domain (bet) family chromatin binding protein, transcription
• Biological source: Homo sapiens (Human)
• Cellular location: Nucleus : P25440
• Total number of polymer chains: 1
• Total formula weight: 13800.29

Authors

Chan, K.-H.,Runcie, A.C.,Ciulli, A. (deposition date: 2017-05-23, release date: 2018-02-14, Last modification date: 2024-01-17)

• Primary citation: Runcie, A.C.,Zengerle, M.,Chan, K.H.,Testa, A.,van Beurden, L.,Baud, M.G.J.,Epemolu, O.,Ellis, L.C.J.,Read, K.D.,Coulthard, V.,Brien, A.,Ciulli, A.; Optimization of a "bump-and-hole" approach to allele-selective BET bromodomain inhibition.; Chem Sci, 9:2452-2468, 2018; PubMed: 29732121; DOI: 10.1039/c7sc02536j

Experimental method

X-RAY DIFFRACTION (2.4 Å)