4zqd

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==Crystal Structure of the Heterodimeric HIF-2a:ARNT Complex with the Benzoxadiazole Antagonist 0X3==
==Crystal Structure of the Heterodimeric HIF-2a:ARNT Complex with the Benzoxadiazole Antagonist 0X3==
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<StructureSection load='4zqd' size='340' side='right' caption='[[4zqd]], [[Resolution|resolution]] 2.87&Aring;' scene=''>
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<StructureSection load='4zqd' size='340' side='right'caption='[[4zqd]], [[Resolution|resolution]] 2.87&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4zqd]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZQD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZQD FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4zqd]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZQD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ZQD 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=0X3:N-(3-CHLORO-5-FLUOROPHENYL)-4-NITRO-2,1,3-BENZOXADIAZOL-5-AMINE'>0X3</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]] 2.87&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4zp4|4zp4]], [[4zph|4zph]], [[4zpk|4zpk]], [[4zpr|4zpr]]</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=0X3:N-(3-CHLORO-5-FLUOROPHENYL)-4-NITRO-2,1,3-BENZOXADIAZOL-5-AMINE'>0X3</scene></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=4zqd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zqd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4zqd RCSB], [http://www.ebi.ac.uk/pdbsum/4zqd PDBsum]</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=4zqd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zqd OCA], [https://pdbe.org/4zqd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4zqd RCSB], [https://www.ebi.ac.uk/pdbsum/4zqd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4zqd ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/ARNT_MOUSE ARNT_MOUSE]] Required for activity of the Ah (dioxin) receptor. This protein is required for the ligand-binding subunit to translocate from the cytosol to the nucleus after ligand binding. The complex then initiates transcription of genes involved in the activation of PAH procarcinogens. The heterodimer with HIF1A or EPAS1/HIF2A functions as a transcriptional regulator of the adaptive response to hypoxia (By similarity). [[http://www.uniprot.org/uniprot/EPAS1_MOUSE EPAS1_MOUSE]] Transcription factor involved in the induction of oxygen regulated genes. Binds to core DNA sequence 5'-[AG]CGTG-3' within the hypoxia response element (HRE) of target gene promoters. Regulates the vascular endothelial growth factor (VEGF) expression and seems to be implicated in the development of blood vessels and the tubular system of lung. May also play a role in the formation of the endothelium that gives rise to the blood brain barrier. Potent activator of the Tie-2 tyrosine kinase expression. Activation requires recruitment of transcriptional coactivators such as CREBPB and probably EP300. Interaction with redox regulatory protein APEX seems to activate CTAD (By similarity).
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[https://www.uniprot.org/uniprot/ARNT_MOUSE ARNT_MOUSE] Required for activity of the Ah (dioxin) receptor. This protein is required for the ligand-binding subunit to translocate from the cytosol to the nucleus after ligand binding. The complex then initiates transcription of genes involved in the activation of PAH procarcinogens. The heterodimer with HIF1A or EPAS1/HIF2A functions as a transcriptional regulator of the adaptive response to hypoxia (By similarity).
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== 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>
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</div>
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<div class="pdbe-citations 4zqd" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[3D structures of hypoxia-inducible factor|3D structures of hypoxia-inducible factor]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Kim, Y]]
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[[Category: Large Structures]]
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[[Category: Lu, J]]
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[[Category: Mus musculus]]
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[[Category: Potluri, N]]
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[[Category: Kim Y]]
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[[Category: Rastinejad, F]]
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[[Category: Lu J]]
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[[Category: Wu, D]]
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[[Category: Potluri N]]
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[[Category: Arnt]]
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[[Category: Rastinejad F]]
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[[Category: Bhlh-pa]]
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[[Category: Wu D]]
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[[Category: Hif-2a]]
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[[Category: Protein transport-transcription complex]]
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Current revision

Crystal Structure of the Heterodimeric HIF-2a:ARNT Complex with the Benzoxadiazole Antagonist 0X3

PDB ID 4zqd

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