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==Crystal structure of the BRD7 bromodomain in complex with BI-9564==
==Crystal structure of the BRD7 bromodomain in complex with BI-9564==
<StructureSection load='5mq1' size='340' side='right' caption='[[5mq1]], [[Resolution|resolution]] 1.50&Aring;' scene=''>
<StructureSection load='5mq1' size='340' side='right'caption='[[5mq1]], [[Resolution|resolution]] 1.50&Aring;' scene=''>
== Structural highlights ==
== 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>
<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://proteopedia.org/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>
</td></tr><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>
<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>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/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>
</table>
== Function ==
== 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>   
[[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>   
==See Also==
*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Arrowsmith, C H]]
[[Category: Arrowsmith, C H]]
[[Category: Bountra, C]]
[[Category: Bountra, C]]

Revision as of 10:25, 19 August 2020

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

Structural highlights

5mq1 is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:, , , ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[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.[1] [2] [3] [4] [5]

See Also

References

  1. ↑ Peng C, Zhou J, Liu HY, Zhou M, Wang LL, Zhang QH, Yang YX, Xiong W, Shen SR, Li XL, Li GY. The transcriptional regulation role of BRD7 by binding to acetylated histone through bromodomain. J Cell Biochem. 2006 Mar 1;97(4):882-92. PMID:16265664 doi:http://dx.doi.org/10.1002/jcb.20645
  2. ↑ Zhou M, Liu H, Xu X, Zhou H, Li X, Peng C, Shen S, Xiong W, Ma J, Zeng Z, Fang S, Nie X, Yang Y, Zhou J, Xiang J, Cao L, Peng S, Li S, Li G. Identification of nuclear localization signal that governs nuclear import of BRD7 and its essential roles in inhibiting cell cycle progression. J Cell Biochem. 2006 Jul 1;98(4):920-30. PMID:16475162 doi:http://dx.doi.org/10.1002/jcb.20788
  3. ↑ Harte MT, O'Brien GJ, Ryan NM, Gorski JJ, Savage KI, Crawford NT, Mullan PB, Harkin DP. BRD7, a subunit of SWI/SNF complexes, binds directly to BRCA1 and regulates BRCA1-dependent transcription. Cancer Res. 2010 Mar 15;70(6):2538-47. doi: 10.1158/0008-5472.CAN-09-2089. Epub, 2010 Mar 9. PMID:20215511 doi:http://dx.doi.org/10.1158/0008-5472.CAN-09-2089
  4. ↑ Drost J, Mantovani F, Tocco F, Elkon R, Comel A, Holstege H, Kerkhoven R, Jonkers J, Voorhoeve PM, Agami R, Del Sal G. BRD7 is a candidate tumour suppressor gene required for p53 function. Nat Cell Biol. 2010 Apr;12(4):380-9. doi: 10.1038/ncb2038. Epub 2010 Mar 14. PMID:20228809 doi:http://dx.doi.org/10.1038/ncb2038
  5. ↑ Burrows AE, Smogorzewska A, Elledge SJ. Polybromo-associated BRG1-associated factor components BRD7 and BAF180 are critical regulators of p53 required for induction of replicative senescence. Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14280-5. doi:, 10.1073/pnas.1009559107. Epub 2010 Jul 26. PMID:20660729 doi:http://dx.doi.org/10.1073/pnas.1009559107

5mq1, resolution 1.50Å

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