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5F60

Crystal structure of the first bromodomain of human BRD4 in complex with SG3-014

Summary for 5F60
Entry DOI10.2210/pdb5f60/pdb
Related5F5Z 5F61 5F62 5F63
DescriptorBromodomain-containing protein 4, ~{N}-[2-chloranyl-5-[[5-methyl-2-[[4-(4-methylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]amino]phenyl]-2-methyl-propane-2-sulfonamide, DI(HYDROXYETHYL)ETHER, ... (5 entities in total)
Functional Keywordsbromodomain, cap, hunk1, mcap, protein binding-inhibitor complex, mitotic chromosome associated protein, cell cycle, inhibitor, transcription-inhibitor complex, transcription-transcription inhibitor complex, transcription/transcription inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationNucleus: O60885
Total number of polymer chains1
Total formula weight15935.82
Authors
Ember, S.W.,Zhu, J.-Y.,Schonbrunn, E. (deposition date: 2015-12-04, release date: 2017-02-08, Last modification date: 2023-09-27)
Primary citationEmber, S.W.,Lambert, Q.T.,Berndt, N.,Gunawan, S.,Ayaz, M.,Tauro, M.,Zhu, J.Y.,Cranfill, P.J.,Greninger, P.,Lynch, C.C.,Benes, C.H.,Lawrence, H.R.,Reuther, G.W.,Lawrence, N.J.,Schonbrunn, E.
Potent Dual BET Bromodomain-Kinase Inhibitors as Value-Added Multitargeted Chemical Probes and Cancer Therapeutics.
Mol. Cancer Ther., 16:1054-1067, 2017
Cited by
PubMed: 28336808
DOI: 10.1158/1535-7163.MCT-16-0568-T
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.35 Å)
Structure validation

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