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5a81

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==Crystal structure of human ATAD2 bromodomain in complex with 8-(3R,4R) -3-(cyclohexylmethoxy)piperidin-4-yl-amino-3-methyl-1,2-dihydro-1,7- naphthyridin-2-one==
==Crystal structure of human ATAD2 bromodomain in complex with 8-(3R,4R) -3-(cyclohexylmethoxy)piperidin-4-yl-amino-3-methyl-1,2-dihydro-1,7- naphthyridin-2-one==
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<StructureSection load='5a81' size='340' side='right' caption='[[5a81]], [[Resolution|resolution]] 2.03&Aring;' scene=''>
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<StructureSection load='5a81' size='340' side='right'caption='[[5a81]], [[Resolution|resolution]] 2.03&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5a81]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5A81 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5A81 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5a81]] 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=5A81 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5A81 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=78J:(3R,4R)-3-(CYCLOHEXYLMETHOXY)PIPERIDIN-4-YL]AMINO}-3-METHYL-1,2-DIHYDRO-1,7-NAPHTHYRIDIN-2-ONE'>78J</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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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]] 2.03&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5a82|5a82]], [[5a83|5a83]], [[5a85|5a85]]</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=78J:(3R,4R)-3-(CYCLOHEXYLMETHOXY)PIPERIDIN-4-YL]AMINO}-3-METHYL-1,2-DIHYDRO-1,7-NAPHTHYRIDIN-2-ONE'>78J</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Adenosinetriphosphatase Adenosinetriphosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.6.1.3 3.6.1.3] </span></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=5a81 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5a81 OCA], [https://pdbe.org/5a81 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5a81 RCSB], [https://www.ebi.ac.uk/pdbsum/5a81 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5a81 ProSAT]</span></td></tr>
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<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=5a81 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5a81 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=5a81 RCSB], [http://www.ebi.ac.uk/pdbsum/5a81 PDBsum]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/ATAD2_HUMAN ATAD2_HUMAN]] May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1. May play a role in the recruitment or occupancy of CREBBP at some ESR1 target gene promoters. May be required for histone hyperacetylation. Involved in the estrogen-induced cell proliferation and cell cycle progression of breast cancer cells.<ref>PMID:17998543</ref>
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[https://www.uniprot.org/uniprot/ATAD2_HUMAN ATAD2_HUMAN] May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1. May play a role in the recruitment or occupancy of CREBBP at some ESR1 target gene promoters. May be required for histone hyperacetylation. Involved in the estrogen-induced cell proliferation and cell cycle progression of breast cancer cells.<ref>PMID:17998543</ref>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
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<div class="pdbe-citations 5a81" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[ATPase family AAA domain-containing protein|ATPase family AAA domain-containing protein]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Adenosinetriphosphatase]]
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[[Category: Homo sapiens]]
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[[Category: Bamborough, P]]
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[[Category: Large Structures]]
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[[Category: Chung, C]]
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[[Category: Bamborough P]]
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[[Category: Demont, E]]
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[[Category: Chung C]]
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[[Category: Atad2]]
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[[Category: Demont E]]
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[[Category: Atpase family aaa domain-containing protein 2]]
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[[Category: Bromodomain]]
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[[Category: Epigenetic]]
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[[Category: Hydrolase]]
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[[Category: Inhibitor]]
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Current revision

Crystal structure of human ATAD2 bromodomain in complex with 8-(3R,4R) -3-(cyclohexylmethoxy)piperidin-4-yl-amino-3-methyl-1,2-dihydro-1,7- naphthyridin-2-one

PDB ID 5a81

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