4ai8

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[[Image:4ai8.jpg|left|200px]]
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==FACTOR INHIBITING HIF-1 ALPHA IN COMPLEX WITH DAMINOZIDE==
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<StructureSection load='4ai8' size='340' side='right' caption='[[4ai8]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4ai8]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AI8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AI8 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=DZA:DAMINOZIDE'>DZA</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2wa4|2wa4]], [[2y0i|2y0i]], [[2w0x|2w0x]], [[2cgn|2cgn]], [[2wa3|2wa3]], [[2cgo|2cgo]], [[2yde|2yde]], [[1iz3|1iz3]], [[1h2m|1h2m]], [[1mze|1mze]], [[1mzf|1mzf]], [[2yc0|2yc0]], [[1yci|1yci]], [[1h2n|1h2n]], [[1h2k|1h2k]], [[2xum|2xum]], [[1h2l|1h2l]]</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/Peptide-aspartate_beta-dioxygenase Peptide-aspartate beta-dioxygenase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.11.16 1.14.11.16] </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=4ai8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ai8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ai8 RCSB], [http://www.ebi.ac.uk/pdbsum/4ai8 PDBsum]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/HIF1N_HUMAN HIF1N_HUMAN]] Hydroxylates HIF-1 alpha at 'Asp-803' in the C-terminal transactivation domain (CAD). Functions as an oxygen sensor and, under normoxic conditions, the hydroxylation prevents interaction of HIF-1 with transcriptional coactivators including Cbp/p300-interacting transactivator. Involved in transcriptional repression through interaction with HIF1A, VHL and histone deacetylases. Hydroxylates specific Asn residues within ankyrin repeat domains (ARD) of NFKB1, NFKBIA, NOTCH1, ASB4, PPP1R12A and several other ARD-containing proteins. Also hydroxylates Asp and His residues within ARDs of ANK1 and TNKS2, respectively. Negatively regulates NOTCH1 activity, accelerating myogenic differentiation. Positively regulates ASB4 activity, promoting vascular differentiation.<ref>PMID:12080085</ref> <ref>PMID:12042299</ref> <ref>PMID:17003112</ref> <ref>PMID:18299578</ref> <ref>PMID:19245366</ref> <ref>PMID:17573339</ref> <ref>PMID:21251231</ref> <ref>PMID:21177872</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The JmjC oxygenases catalyze the N-demethylation of N(epsilon)-methyl lysine residues in histones and are current therapeutic targets. A set of human 2-oxoglutarate analogues were screened using a unified assay platform for JmjC demethylases and related oxygenases. Results led to the finding that daminozide (N-(dimethylamino)succinamic acid, 160 Da), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily. Kinetic and crystallographic studies reveal that daminozide chelates the active site metal via its hydrazide carbonyl and dimethylamino groups.
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{{STRUCTURE_4ai8| PDB=4ai8 | SCENE= }}
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Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.,Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A J Med Chem. 2012 Jul 26;55(14):6639-43. Epub 2012 Jul 11. PMID:22724510<ref>PMID:22724510</ref>
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===FACTOR INHIBITING HIF-1 ALPHA IN COMPLEX WITH DAMINOZIDE===
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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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{{ABSTRACT_PUBMED_22724510}}
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==See Also==
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*[[Factor inhibiting HIF|Factor inhibiting HIF]]
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==About this Structure==
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== References ==
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[[4ai8]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AI8 OCA].
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<references/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Peptide-aspartate beta-dioxygenase]]
[[Category: Peptide-aspartate beta-dioxygenase]]
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[[Category: Chowdhury, R.]]
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[[Category: Chowdhury, R]]
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[[Category: Clifton, I J.]]
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[[Category: Clifton, I J]]
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[[Category: Kawamura, A.]]
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[[Category: Kawamura, A]]
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[[Category: King, O N.F.]]
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[[Category: King, O N.F]]
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[[Category: Mcdonough, M A.]]
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[[Category: Mcdonough, M A]]
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[[Category: Rose, N R.]]
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[[Category: Rose, N R]]
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[[Category: Schofield, C J.]]
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[[Category: Schofield, C J]]
[[Category: Ankyrin repeat domain]]
[[Category: Ankyrin repeat domain]]
[[Category: Beta-hydroxylation]]
[[Category: Beta-hydroxylation]]

Revision as of 18:23, 25 December 2014

FACTOR INHIBITING HIF-1 ALPHA IN COMPLEX WITH DAMINOZIDE

4ai8, resolution 2.40Å

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