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4F3I

Crystal structure of the first bromodomain of human BRD4 in complex with MS417 inhibitor

Summary for 4F3I
Entry DOI10.2210/pdb4f3i/pdb
DescriptorBromodomain-containing protein 4, 1,2-ETHANEDIOL, methyl [(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetate, ... (4 entities in total)
Functional Keywordsprotein-inhibitor complex, acetyl-lysine binding, nucleus, signaling protein-inhibitor complex, signaling protein/inhibitor
Biological sourceHomo sapiens (human)
Cellular locationNucleus: O60885
Total number of polymer chains1
Total formula weight15638.42
Authors
Joshua, J.,Zhou, M.-M.,Plotnikov, A.N. (deposition date: 2012-05-09, release date: 2012-09-12, Last modification date: 2023-09-13)
Primary citationZhang, G.,Liu, R.,Zhong, Y.,Plotnikov, A.N.,Zhang, W.,Zeng, L.,Rusinova, E.,Gerona-Nevarro, G.,Moshkina, N.,Joshua, J.,Chuang, P.Y.,Ohlmeyer, M.,He, J.C.,Zhou, M.M.
Down-regulation of NF-{kappa}B Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition.
J.Biol.Chem., 287:28840-28851, 2012
Cited by
PubMed: 22645123
DOI: 10.1074/jbc.M112.359505
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.4 Å)
Structure validation

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