3sp6

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==Structural basis for iloprost as a dual PPARalpha/delta agonist==
==Structural basis for iloprost as a dual PPARalpha/delta agonist==
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<StructureSection load='3sp6' size='340' side='right' caption='[[3sp6]], [[Resolution|resolution]] 2.21&Aring;' scene=''>
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<StructureSection load='3sp6' size='340' side='right'caption='[[3sp6]], [[Resolution|resolution]] 2.21&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3sp6]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3SP6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3SP6 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3sp6]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3SP6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3SP6 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=IL2:(5E)-5-[(3AS,4R,5R,6AS)-5-HYDROXY-4-[(1E,3S,4R)-3-HYDROXY-4-METHYLOCT-1-EN-6-YN-1-YL]HEXAHYDROPENTALEN-2(1H)-YLIDENE]PENTANOIC+ACID'>IL2</scene></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=IL2:(5E)-5-[(3AS,4R,5R,6AS)-5-HYDROXY-4-[(1E,3S,4R)-3-HYDROXY-4-METHYLOCT-1-EN-6-YN-1-YL]HEXAHYDROPENTALEN-2(1H)-YLIDENE]PENTANOIC+ACID'>IL2</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3sp9|3sp9]]</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3sp9|3sp9]]</div></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PPARA, NR1C1, PPAR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PPARA, NR1C1, PPAR ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3sp6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3sp6 OCA], [http://pdbe.org/3sp6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3sp6 RCSB], [http://www.ebi.ac.uk/pdbsum/3sp6 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3sp6 ProSAT]</span></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=3sp6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3sp6 OCA], [https://pdbe.org/3sp6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3sp6 RCSB], [https://www.ebi.ac.uk/pdbsum/3sp6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3sp6 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/PPARA_HUMAN PPARA_HUMAN]] Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety (By similarity). Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2.<ref>PMID:7684926</ref> <ref>PMID:7629123</ref> <ref>PMID:9556573</ref> <ref>PMID:10195690</ref> [[http://www.uniprot.org/uniprot/PRGC2_HUMAN PRGC2_HUMAN]] Plays a role of stimulator of transcription factors and nuclear receptors activities. Activates transcritional activity of estrogen receptor alpha, nuclear respiratory factor 1 (NRF1) and glucocorticoid receptor in the presence of glucocorticoids. May play a role in constitutive non-adrenergic-mediated mitochondrial biogenesis as suggested by increased basal oxygen consumption and mitochondrial number when overexpressed. May be involved in fat oxidation and non-oxidative glucose metabolism and in the regulation of energy expenditure. Induces the expression of PERM1 in the skeletal muscle in an ESRRA-dependent manner.<ref>PMID:11854298</ref> <ref>PMID:12678921</ref> <ref>PMID:15546003</ref> <ref>PMID:23836911</ref>
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[[https://www.uniprot.org/uniprot/PPARA_HUMAN PPARA_HUMAN]] Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety (By similarity). Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2.<ref>PMID:7684926</ref> <ref>PMID:7629123</ref> <ref>PMID:9556573</ref> <ref>PMID:10195690</ref> [[https://www.uniprot.org/uniprot/PRGC2_HUMAN PRGC2_HUMAN]] Plays a role of stimulator of transcription factors and nuclear receptors activities. Activates transcritional activity of estrogen receptor alpha, nuclear respiratory factor 1 (NRF1) and glucocorticoid receptor in the presence of glucocorticoids. May play a role in constitutive non-adrenergic-mediated mitochondrial biogenesis as suggested by increased basal oxygen consumption and mitochondrial number when overexpressed. May be involved in fat oxidation and non-oxidative glucose metabolism and in the regulation of energy expenditure. Induces the expression of PERM1 in the skeletal muscle in an ESRRA-dependent manner.<ref>PMID:11854298</ref> <ref>PMID:12678921</ref> <ref>PMID:15546003</ref> <ref>PMID:23836911</ref>
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<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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==See Also==
==See Also==
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*[[Peroxisome Proliferator-Activated Receptors|Peroxisome Proliferator-Activated Receptors]]
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*[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Human]]
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[[Category: Large Structures]]
[[Category: Li, Y]]
[[Category: Li, Y]]
[[Category: Rong, H]]
[[Category: Rong, H]]

Revision as of 08:04, 29 June 2022

Structural basis for iloprost as a dual PPARalpha/delta agonist

PDB ID 3sp6

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