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==Crystal structure of pyruvate dehydrogenase kinase isoform 2 in complex with inhibitor PS35==
==Crystal structure of pyruvate dehydrogenase kinase isoform 2 in complex with inhibitor PS35==
<StructureSection load='5j71' size='340' side='right' caption='[[5j71]], [[Resolution|resolution]] 1.65&Aring;' scene=''>
<StructureSection load='5j71' size='340' side='right'caption='[[5j71]], [[Resolution|resolution]] 1.65&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[5j71]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5J71 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5J71 FirstGlance]. <br>
<table><tr><td colspan='2'>[[5j71]] 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=5J71 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5J71 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=P35:4-({5-[(PIPERIDIN-4-YL)AMINO]-1,3-DIHYDRO-2H-ISOINDOL-2-YL}SULFONYL)BENZENE-1,3-DIOL'>P35</scene>, <scene name='pdbligand=TLA:L(+)-TARTARIC+ACID'>TLA</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.65&#8491;</td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4mp2|4mp2]], [[4mp7|4mp7]], [[4mpe|4mpe]], [[4mpc|4mpc]], [[4mpn|4mpn]], [[5j6a|5j6a]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=P35:4-({5-[(PIPERIDIN-4-YL)AMINO]-1,3-DIHYDRO-2H-ISOINDOL-2-YL}SULFONYL)BENZENE-1,3-DIOL'>P35</scene>, <scene name='pdbligand=TLA:L(+)-TARTARIC+ACID'>TLA</scene></td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/[Pyruvate_dehydrogenase_(acetyl-transferring)]_kinase [Pyruvate dehydrogenase (acetyl-transferring)] kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.2 2.7.11.2] </span></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=5j71 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j71 OCA], [https://pdbe.org/5j71 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5j71 RCSB], [https://www.ebi.ac.uk/pdbsum/5j71 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5j71 ProSAT]</span></td></tr>
<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=5j71 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j71 OCA], [http://pdbe.org/5j71 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5j71 RCSB], [http://www.ebi.ac.uk/pdbsum/5j71 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5j71 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://www.uniprot.org/uniprot/PDK2_HUMAN PDK2_HUMAN]] Serine/threonine kinase that plays a key role in the 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. Inhibition of pyruvate dehydrogenase decreases glucose utilization and increases fat metabolism. Mediates cellular responses to insulin. Plays an important role in maintaining normal blood glucose levels and in metabolic adaptation to nutrient availability. Via its regulation of pyruvate dehydrogenase activity, plays an important role in maintaining normal blood pH and in preventing the accumulation of ketone bodies under starvation. Plays a role in the regulation of cell proliferation and in resistance to apoptosis under oxidative stress. Plays a role in p53/TP53-mediated apoptosis.<ref>PMID:7499431</ref> <ref>PMID:9787110</ref> <ref>PMID:17222789</ref> <ref>PMID:19833728</ref> <ref>PMID:21283817</ref> <ref>PMID:22123926</ref>
[https://www.uniprot.org/uniprot/PDK2_HUMAN PDK2_HUMAN] Serine/threonine kinase that plays a key role in the 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. Inhibition of pyruvate dehydrogenase decreases glucose utilization and increases fat metabolism. Mediates cellular responses to insulin. Plays an important role in maintaining normal blood glucose levels and in metabolic adaptation to nutrient availability. Via its regulation of pyruvate dehydrogenase activity, plays an important role in maintaining normal blood pH and in preventing the accumulation of ketone bodies under starvation. Plays a role in the regulation of cell proliferation and in resistance to apoptosis under oxidative stress. Plays a role in p53/TP53-mediated apoptosis.<ref>PMID:7499431</ref> <ref>PMID:9787110</ref> <ref>PMID:17222789</ref> <ref>PMID:19833728</ref> <ref>PMID:21283817</ref> <ref>PMID:22123926</ref>  
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 5j71" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 5j71" style="background-color:#fffaf0;"></div>
==See Also==
*[[Pyruvate dehydrogenase kinase|Pyruvate dehydrogenase kinase]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Chuang, D T]]
[[Category: Homo sapiens]]
[[Category: Chuang, J L]]
[[Category: Large Structures]]
[[Category: Gui, W J]]
[[Category: Chuang DT]]
[[Category: Qi, X]]
[[Category: Chuang JL]]
[[Category: Tso, S C]]
[[Category: Gui WJ]]
[[Category: Wu, C Y]]
[[Category: Qi X]]
[[Category: Wynn, R M]]
[[Category: Tso SC]]
[[Category: Bergerat nucleotide-binding fold]]
[[Category: Wu CY]]
[[Category: Cancer]]
[[Category: Wynn RM]]
[[Category: Ghkl protein kinase]]
[[Category: Hepatic steatosis]]
[[Category: Impaired glucose oxidation]]
[[Category: Mitochondrial protein kinase]]
[[Category: Protein kinase]]
[[Category: Pyruvate dehydrogenase complex]]
[[Category: Transferase-transferase inhibitor complex]]
[[Category: Type 2 diabetes]]
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