5ufp
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of PT2399 bound to HIF2a-B*:ARNT-B* complex== | |
| + | <StructureSection load='5ufp' size='340' side='right'caption='[[5ufp]], [[Resolution|resolution]] 1.90Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5ufp]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5t0t 5t0t]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5UFP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5UFP FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.9Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=86D:3-({(1S)-7-[(DIFLUOROMETHYL)SULFONYL]-2,2-DIFLUORO-1-HYDROXY-2,3-DIHYDRO-1H-INDEN-4-YL}OXY)-5-FLUOROBENZONITRILE'>86D</scene></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5ufp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ufp OCA], [https://pdbe.org/5ufp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ufp RCSB], [https://www.ebi.ac.uk/pdbsum/5ufp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ufp ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Disease == | ||
| + | [https://www.uniprot.org/uniprot/EPAS1_HUMAN EPAS1_HUMAN] Defects in EPAS1 are the cause of familial erythrocytosis type 4 (ECYT4) [MIM:[https://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> | ||
| + | == Function == | ||
| + | [https://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. | ||
| - | + | ==See Also== | |
| - | + | *[[3D structures of hypoxia-inducible factor|3D structures of hypoxia-inducible factor]] | |
| - | + | == References == | |
| - | [[Category: | + | <references/> |
| - | [[Category: Du | + | __TOC__ |
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Du X]] | ||
Current revision
Crystal structure of PT2399 bound to HIF2a-B*:ARNT-B* complex
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