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5D25

First bromodomain of BRD4 bound to inhibitor XD27

Summary for 5D25
Entry DOI10.2210/pdb5d25/pdb
DescriptorBromodomain-containing protein 4, 4-acetyl-N-[5-(diethylsulfamoyl)-2-hydroxyphenyl]-3,5-dimethyl-1H-pyrrole-2-carboxamide, GLYCEROL, ... (5 entities in total)
Functional Keywordsgene regulation, inhibitor, bromodomain, transcription
Biological sourceHomo sapiens (Human)
Cellular locationNucleus: O60885
Total number of polymer chains1
Total formula weight15602.00
Authors
Wohlwend, D.,Huegle, M.,Gerhardt, S. (deposition date: 2015-08-05, 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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