4h6j
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Identification of Cys 255 in HIF-1 as a novel site for development of covalent inhibitors of HIF-1 /ARNT PasB domain protein-protein interaction.== | |
| + | <StructureSection load='4h6j' size='340' side='right'caption='[[4h6j]], [[Resolution|resolution]] 1.52Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4h6j]] is a 2 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=4H6J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4H6J 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]] 1.52Å</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=4h6j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4h6j OCA], [https://pdbe.org/4h6j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4h6j RCSB], [https://www.ebi.ac.uk/pdbsum/4h6j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4h6j ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/HIF1A_HUMAN HIF1A_HUMAN] Functions as a master transcriptional regulator of the adaptive response to hypoxia. Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transporters, glycolytic enzymes, vascular endothelial growth factor, HILPDA, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia. Plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease. Binds to core DNA sequence 5'-[AG]CGTG-3' within the hypoxia response element (HRE) of target gene promoters. Activation requires recruitment of transcriptional coactivators such as CREBPB and EP300. Activity is enhanced by interaction with both, NCOA1 or NCOA2. Interaction with redox regulatory protein APEX seems to activate CTAD and potentiates activation by NCOA1 and CREBBP. Involved in the axonal distribution and transport of mitochondria in neurons during hypoxia.<ref>PMID:9887100</ref> <ref>PMID:11566883</ref> <ref>PMID:11292861</ref> <ref>PMID:15465032</ref> <ref>PMID:16543236</ref> <ref>PMID:16973622</ref> <ref>PMID:17610843</ref> <ref>PMID:19528298</ref> <ref>PMID:20624928</ref> | ||
| - | + | ==See Also== | |
| - | + | *[[Factor inhibiting HIF|Factor inhibiting HIF]] | |
| - | + | *[[3D structures of hypoxia-inducible factor|3D structures of hypoxia-inducible factor]] | |
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Bergqvist S]] | ||
| + | [[Category: Brooun A]] | ||
| + | [[Category: Cardoso R]] | ||
| + | [[Category: Chen P]] | ||
| + | [[Category: Deng Y-L]] | ||
| + | [[Category: Dyson HJ]] | ||
| + | [[Category: Greig MJ]] | ||
| + | [[Category: Liu K]] | ||
| + | [[Category: Love RA]] | ||
| + | [[Category: Nilsson C]] | ||
| + | [[Category: Nowlin D]] | ||
| + | [[Category: Yan J]] | ||
| + | [[Category: Zhu J]] | ||
Current revision
Identification of Cys 255 in HIF-1 as a novel site for development of covalent inhibitors of HIF-1 /ARNT PasB domain protein-protein interaction.
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Categories: Homo sapiens | Large Structures | Bergqvist S | Brooun A | Cardoso R | Chen P | Deng Y-L | Dyson HJ | Greig MJ | Liu K | Love RA | Nilsson C | Nowlin D | Yan J | Zhu J
