4jpg

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{{STRUCTURE_4jpg| PDB=4jpg | SCENE= }}
 
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===2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as Novel PKM2 Activators===
 
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{{ABSTRACT_PUBMED_23622982}}
 
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==Function==
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==2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as Novel PKM2 Activators==
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[[http://www.uniprot.org/uniprot/KPYM_HUMAN KPYM_HUMAN]] Glycolytic enzyme that catalyzes the transfer of a phosphoryl group from phosphoenolpyruvate (PEP) to ADP, generating ATP. Stimulates POU5F1-mediated transcriptional activation. Plays a general role in caspase independent cell death of tumor cells. The ratio betwween the highly active tetrameric form and nearly inactive dimeric form determines whether glucose carbons are channeled to biosynthetic processes or used for glycolytic ATP production. The transition between the 2 forms contributes to the control of glycolysis and is important for tumor cell proliferation and survival.<ref>PMID:17308100</ref> <ref>PMID:18191611</ref> <ref>PMID:21620138</ref>
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<StructureSection load='4jpg' size='340' side='right'caption='[[4jpg]], [[Resolution|resolution]] 2.33&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4jpg]] is a 4 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=4JPG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4JPG FirstGlance]. <br>
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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]] 2.33&#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=1OX:2-(1H-BENZIMIDAZOL-1-YLMETHYL)-4H-PYRIDO[1,2-A]PYRIMIDIN-4-ONE'>1OX</scene>, <scene name='pdbligand=FBP:BETA-FRUCTOSE-1,6-DIPHOSPHATE'>FBP</scene></td></tr>
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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=4jpg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4jpg OCA], [https://pdbe.org/4jpg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4jpg RCSB], [https://www.ebi.ac.uk/pdbsum/4jpg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4jpg ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/KPYM_HUMAN KPYM_HUMAN] Glycolytic enzyme that catalyzes the transfer of a phosphoryl group from phosphoenolpyruvate (PEP) to ADP, generating ATP. Stimulates POU5F1-mediated transcriptional activation. Plays a general role in caspase independent cell death of tumor cells. The ratio betwween the highly active tetrameric form and nearly inactive dimeric form determines whether glucose carbons are channeled to biosynthetic processes or used for glycolytic ATP production. The transition between the 2 forms contributes to the control of glycolysis and is important for tumor cell proliferation and survival.<ref>PMID:17308100</ref> <ref>PMID:18191611</ref> <ref>PMID:21620138</ref>
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==About this Structure==
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==See Also==
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[[4jpg]] is a 4 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=4JPG OCA].
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*[[Pyruvate kinase 3D structures|Pyruvate kinase 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:023622982</ref><references group="xtra"/><references/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Pyruvate kinase]]
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[[Category: Large Structures]]
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[[Category: Cronin, C.]]
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[[Category: Cronin C]]
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[[Category: Greasley, S E.]]
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[[Category: Greasley SE]]
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[[Category: Hickey, M.]]
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[[Category: Hickey M]]
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[[Category: Phonephaly, H.]]
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[[Category: Phonephaly H]]
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[[Category: Pyruvate kinase]]
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[[Category: Transferase-transferase activator complex]]
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2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as Novel PKM2 Activators

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