5mq1
From Proteopedia
(Difference between revisions)
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of the BRD7 bromodomain in complex with BI-9564== | |
| - | + | <StructureSection load='5mq1' size='340' side='right' caption='[[5mq1]], [[Resolution|resolution]] 1.50Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[5mq1]] is a 1 chain structure. 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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5MQ1 FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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> | |
| - | [[Category: | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5mq1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mq1 OCA], [http://pdbe.org/5mq1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5mq1 RCSB], [http://www.ebi.ac.uk/pdbsum/5mq1 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5mq1 ProSAT]</span></td></tr> |
| + | </table> | ||
| + | == Function == | ||
| + | [[http://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> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Arrowsmith, C H]] | ||
| + | [[Category: Bountra, C]] | ||
| + | [[Category: Delft, F von]] | ||
| + | [[Category: Diaz-Saez, L]] | ||
| + | [[Category: Edwards, A M]] | ||
[[Category: Huber, K]] | [[Category: Huber, K]] | ||
| - | [[Category: | + | [[Category: Knapp, S]] |
| + | [[Category: Krojer, T]] | ||
| + | [[Category: Martin, L J]] | ||
[[Category: Panagakou, I]] | [[Category: Panagakou, I]] | ||
| - | [[Category: Von Delft, F]] | ||
[[Category: Picaud, S]] | [[Category: Picaud, S]] | ||
| - | + | [[Category: Structural genomic]] | |
| - | + | [[Category: Bromodomain]] | |
| - | [[Category: Structural | + | [[Category: Transcription]] |
| - | + | ||
| - | + | ||
| - | [[Category: | + | |
| - | [[Category: | + | |
Revision as of 06:47, 17 January 2018
Crystal structure of the BRD7 bromodomain in complex with BI-9564
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