6d09

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'''Unreleased structure'''
 
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The entry 6d09 is ON HOLD until Paper Publication
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==Crystal structure of PT2440 bound to HIF2a-B*:ARNT-B* complex==
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<StructureSection load='6d09' size='340' side='right' caption='[[6d09]], [[Resolution|resolution]] 1.85&Aring;' scene=''>
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Authors: Du, X.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6d09]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D09 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D09 FirstGlance]. <br>
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Description: Crystal structure of PT2440 bound to HIF2a-B*:ARNT-B* complex
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FOJ:3-{[(3R)-4-(difluoromethyl)-2,2-difluoro-3-hydroxy-1,1-dioxo-2,3-dihydro-1H-1-benzothiophen-5-yl]oxy}-5-fluorobenzonitrile'>FOJ</scene></td></tr>
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[[Category: Unreleased Structures]]
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6czw|6czw]]</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=6d09 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d09 OCA], [http://pdbe.org/6d09 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d09 RCSB], [http://www.ebi.ac.uk/pdbsum/6d09 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d09 ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[[http://www.uniprot.org/uniprot/EPAS1_HUMAN EPAS1_HUMAN]] Defects in EPAS1 are the cause of familial erythrocytosis type 4 (ECYT4) [MIM:[http://omim.org/entry/611783 611783]]. ECYT4 is an autosomal dominant disorder characterized by increased serum red blood cell mass, elevated hemoglobin concentration and hematocrit, and normal platelet and leukocyte counts.<ref>PMID:19208626</ref> <ref>PMID:18378852</ref> <ref>PMID:18184961</ref> <ref>PMID:22367913</ref>
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== Function ==
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[[http://www.uniprot.org/uniprot/EPAS1_HUMAN EPAS1_HUMAN]] 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 seems to require recruitment of transcriptional coactivators such as CREBPB and probably EP300. Interaction with redox regulatory protein APEX seems to activate CTAD. [[http://www.uniprot.org/uniprot/ARNT_HUMAN ARNT_HUMAN]] 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.
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== References ==
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<references/>
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__TOC__
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</StructureSection>
[[Category: Du, X]]
[[Category: Du, X]]
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[[Category: Arnt]]
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[[Category: Epas1]]
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[[Category: Hif2a]]
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[[Category: Hypoxia inducible factor]]
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[[Category: Pas b domain]]
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[[Category: Transcription]]

Revision as of 06:49, 31 October 2018

Crystal structure of PT2440 bound to HIF2a-B*:ARNT-B* complex

6d09, resolution 1.85Å

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