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5O3H

Human Brd2(BD2) mutant in complex with 9-ME-Am1

Summary for 5O3H
Entry DOI10.2210/pdb5o3h/pdb
DescriptorBromodomain-containing protein 2, (2~{R})-2-[(4~{S})-6-(4-chlorophenyl)-9-methoxy-1-methyl-4~{H}-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-~{N}-ethyl-propanamide, CHLORIDE ION, ... (5 entities in total)
Functional Keywordsthe bromodomain and extra-terminal domain (bet) family chromatin binding protein, transcription
Biological sourceHomo sapiens (Human)
Cellular locationNucleus : P25440
Total number of polymer chains1
Total formula weight13968.93
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 citationRuncie, 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
Cited by
PubMed: 29732121
DOI: 10.1039/c7sc02536j
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.4 Å)
Structure validation

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