2q8g

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[[Image:2q8g.png|left|200px]]
 
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{{STRUCTURE_2q8g| PDB=2q8g | SCENE= }}
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==Structure of pyruvate dehydrogenase kinase isoform 1 in complex with glucose-lowering drug AZD7545==
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<StructureSection load='2q8g' size='340' side='right'caption='[[2q8g]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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===Structure of pyruvate dehydrogenase kinase isoform 1 in complex with glucose-lowering drug AZD7545===
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2q8g]] is a 1 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=2Q8G OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Q8G FirstGlance]. <br>
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{{ABSTRACT_PUBMED_17683942}}
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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]] 1.9&#8491;</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=AZX:4-[(3-CHLORO-4-{[(2R)-3,3,3-TRIFLUORO-2-HYDROXY-2-METHYLPROPANOYL]AMINO}PHENYL)SULFONYL]-N,N-DIMETHYLBENZAMIDE'>AZX</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene></td></tr>
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==About this Structure==
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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=2q8g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q8g OCA], [https://pdbe.org/2q8g PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2q8g RCSB], [https://www.ebi.ac.uk/pdbsum/2q8g PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2q8g ProSAT]</span></td></tr>
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[[2q8g]] 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=2Q8G OCA].
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PDK1_HUMAN PDK1_HUMAN] Serine/threonine kinase that plays a key role in regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Plays an important role in cellular responses to hypoxia and is important for cell proliferation under hypoxia. Protects cells against apoptosis in response to hypoxia and oxidative stress.<ref>PMID:7499431</ref> <ref>PMID:18541534</ref> <ref>PMID:22195962</ref> <ref>PMID:17683942</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/q8/2q8g_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2q8g ConSurf].
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<div style="clear:both"></div>
==See Also==
==See Also==
*[[Pyruvate dehydrogenase kinase|Pyruvate dehydrogenase kinase]]
*[[Pyruvate dehydrogenase kinase|Pyruvate dehydrogenase kinase]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:017683942</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Chuang, D T.]]
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[[Category: Large Structures]]
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[[Category: Chuang, J L.]]
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[[Category: Chuang DT]]
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[[Category: Kato, M.]]
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[[Category: Chuang JL]]
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[[Category: Li, J.]]
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[[Category: Kato M]]
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[[Category: Ghkl atpase/kinase family]]
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[[Category: Li J]]
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[[Category: Glucose-lowering drug azd7545]]
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[[Category: Mitochondrial kinase]]
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[[Category: Pyruvate dehydrogenase complex]]
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[[Category: Transferase]]
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Current revision

Structure of pyruvate dehydrogenase kinase isoform 1 in complex with glucose-lowering drug AZD7545

PDB ID 2q8g

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