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5mq1

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'''Unreleased structure'''
 
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The entry 5mq1 is ON HOLD until Paper Publication
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==Crystal structure of the BRD7 bromodomain in complex with BI-9564==
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<StructureSection load='5mq1' size='340' side='right'caption='[[5mq1]], [[Resolution|resolution]] 1.50&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5mq1]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5MQ1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5MQ1 FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.5&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5U6:4-[4-[(DIMETHYLAMINO)METHYL]-2,5-DIMETHOXY-PHENYL]-2-METHYL-2,7-NAPHTHYRIDIN-1-ONE'>5U6</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5mq1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mq1 OCA], [https://pdbe.org/5mq1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5mq1 RCSB], [https://www.ebi.ac.uk/pdbsum/5mq1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5mq1 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/BRD7_HUMAN BRD7_HUMAN] Acts both as coactivator and as corepressor. May play a role in chromatin remodeling. Activator of the Wnt signaling pathway in a DVL1-dependent manner by negatively regulating the GSK3B phosphotransferase activity. Induces dephosphorylation of GSK3B at 'Tyr-216'. Down-regulates TRIM24-mediated activation of transcriptional activation by AR (By similarity). Transcriptional corepressor that down-regulates the expression of target genes. Binds to target promoters, leading to increased histone H3 acetylation at 'Lys-9' (H3K9ac). Binds to the ESR1 promoter. Recruits BRCA1 and POU2F1 to the ESR1 promoter. Coactivator for TP53-mediated activation of transcription of a set of target genes. Required for TP53-mediated cell-cycle arrest in response to oncogene activation. Promotes acetylation of TP53 at 'Lys-382', and thereby promotes efficient recruitment of TP53 to target promoters. Inhibits cell cycle progression from G1 to S phase.<ref>PMID:16265664</ref> <ref>PMID:16475162</ref> <ref>PMID:20215511</ref> <ref>PMID:20228809</ref> <ref>PMID:20660729</ref>
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Authors: Diaz-Saez, L., Martin, L.J., Panagakou, I., Picaud, S., Krojer, T., von Delft, F., Knapp, S., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Huber, K., Structural Genomics Consortium
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==See Also==
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*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
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Description: Crystal structure of the BRD7 bromodomain in complex with BI-9564
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== References ==
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[[Category: Unreleased Structures]]
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<references/>
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[[Category: Huber, K]]
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__TOC__
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[[Category: Arrowsmith, C.H]]
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</StructureSection>
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[[Category: Panagakou, I]]
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[[Category: Homo sapiens]]
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[[Category: Von Delft, F]]
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[[Category: Large Structures]]
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[[Category: Picaud, S]]
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[[Category: Arrowsmith CH]]
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[[Category: Knapp, S]]
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[[Category: Bountra C]]
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[[Category: Edwards, A.M]]
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[[Category: Diaz-Saez L]]
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[[Category: Structural Genomics Consortium]]
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[[Category: Edwards AM]]
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[[Category: Krojer, T]]
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[[Category: Huber K]]
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[[Category: Martin, L.J]]
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[[Category: Knapp S]]
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[[Category: Diaz-Saez, L]]
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[[Category: Krojer T]]
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[[Category: Bountra, C]]
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[[Category: Martin LJ]]
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[[Category: Panagakou I]]
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[[Category: Picaud S]]
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[[Category: Von Delft F]]

Current revision

Crystal structure of the BRD7 bromodomain in complex with BI-9564

PDB ID 5mq1

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