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5D3H

First bromodomain of BRD4 bound to inhibitor XD29

Summary for 5D3H
Entry DOI10.2210/pdb5d3h/pdb
DescriptorBromodomain-containing protein 4, N-[5-(diethylsulfamoyl)-2-hydroxyphenyl]-3-ethyl-4-(hydroxyacetyl)-5-methyl-1H-pyrrole-2-carboxamide (3 entities in total)
Functional Keywordsgene regulation, bromodomain, inhibitor, transcription
Biological sourceHomo sapiens (Human)
Cellular locationNucleus: O60885
Total number of polymer chains1
Total formula weight15449.81
Authors
Wohlwend, D.,Huegle, M.,Weitzel, G. (deposition date: 2015-08-06, release date: 2016-01-20, Last modification date: 2017-09-06)
Primary citationHugle, M.,Lucas, X.,Weitzel, G.,Ostrovskyi, D.,Breit, B.,Gerhardt, S.,Einsle, O.,Gunther, S.,Wohlwend, D.
4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).
J.Med.Chem., 59:1518-1530, 2016
Cited by
PubMed: 26731611
DOI: 10.1021/acs.jmedchem.5b01267
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.7 Å)
Structure validation

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