4bcr - Revision history

OCA at 10:59, 9 May 2024

OCA — Thu, 09 May 2024 10:59:17 GMT

←Older revision		Revision as of 10:59, 9 May 2024
Line 3:		Line 3:
	<StructureSection load='4bcr' size='340' side='right'caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>		<StructureSection load='4bcr' size='340' side='right'caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4bcr]] 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4BCR FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4bcr]] is a 2 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4BCR FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=EDO:1,2~~-~~ETHANEDIOL'>EDO</scene>~~, ~~<scene name='pdbligand=WY1:2-({4-CHLORO-6-~~[~~(2,3-DIMETHYLPHENYL)AMINO~~]~~PYRIMIDIN-~~2~~-YL}SULFANYL)ACETIC+ACID'>WY1</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]] 2.497Å</td></tr>
-	<tr id='~~related~~'><td class="sblockLbl"><b>[[~~Related_structure~~\|~~Related~~:]]</b></td><td class="sblockDat"><~~div style~~='~~overflow~~: ~~auto; max~~-~~height: 3em;~~'>~~[[1i7g\|1i7g]], [[1k7l\|1k7l]], [[1kkq\|1kkq]]~~</~~div~~><~~/td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=WY1:2-({4-CHLORO-6-[(2,3-DIMETHYLPHENYL)AMINO]PYRIMIDIN-2-YL}SULFANYL)ACETIC+ACID'>WY1</scene></td></tr>
-	~~<tr id~~='~~activity'><td class~~=~~"sblockLbl"><b>Activity~~:~~</b></td><td class="sblockDat"><span class='plainlinks'>~~[~~https://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase]~~, ~~with EC number [https://www.brenda~~-~~enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48~~] </~~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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [https://pdbe.org/4bcr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [https://www.ebi.ac.uk/pdbsum/4bcr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4bcr ProSAT]</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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [https://pdbe.org/4bcr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [https://www.ebi.ac.uk/pdbsum/4bcr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4bcr ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[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/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>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 27:		Line 26:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Histone acetyltransferase]]~~	+	[[Category: Homo sapiens]]
-	~~[[Category: Human~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Bernardes, A]]	+	[[Category: Bernardes A]]
-	[[Category: Muniz~~, J R.C~~]]	+	[[Category: Muniz JRC]]
-	[[Category: Polikarpov, I]]	+	[[Category: Polikarpov I]]
-	~~[[Category: Fibrate]]~~	+
-	~~[[Category: Nuclear receptor]]~~	+
-	~~[[Category: Ppar]]~~	+
-	~~[[Category: Transcription~~]]	+

OCA at 07:08, 31 August 2022

OCA — Wed, 31 Aug 2022 07:08:26 GMT

←Older revision		Revision as of 07:08, 31 August 2022
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	<StructureSection load='4bcr' size='340' side='right'caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>		<StructureSection load='4bcr' size='340' side='right'caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4bcr]] 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4BCR FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4bcr]] 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4BCR FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=WY1:2-({4-CHLORO-6-[(2,3-DIMETHYLPHENYL)AMINO]PYRIMIDIN-2-YL}SULFANYL)ACETIC+ACID'>WY1</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=WY1:2-({4-CHLORO-6-[(2,3-DIMETHYLPHENYL)AMINO]PYRIMIDIN-2-YL}SULFANYL)ACETIC+ACID'>WY1</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1i7g\|1i7g]], [[1k7l\|1k7l]], [[1kkq\|1kkq]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1i7g\|1i7g]], [[1k7l\|1k7l]], [[1kkq\|1kkq]]</div></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [~~http~~://pdbe.org/4bcr PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4bcr PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4bcr ProSAT]</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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [https://pdbe.org/4bcr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [https://www.ebi.ac.uk/pdbsum/4bcr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4bcr ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~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>	+	[[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>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 22:		Line 22:

	==See Also==		==See Also==
-	*[[Peroxisome ~~Proliferator~~-~~Activated Receptors~~\|Peroxisome ~~Proliferator~~-~~Activated Receptors~~]]	+	*[[Peroxisome proliferator-activated receptor 3D structures\|Peroxisome proliferator-activated receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 13:01, 13 March 2019

OCA — Wed, 13 Mar 2019 13:01:46 GMT

←Older revision		Revision as of 13:01, 13 March 2019
Line 1:		Line 1:

	==Structure of PPARalpha in complex with WY14643==		==Structure of PPARalpha in complex with WY14643==
-	<StructureSection load='4bcr' size='340' side='right' caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>	+	<StructureSection load='4bcr' size='340' side='right'caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4bcr]] 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BCR FirstGlance]. <br>		<table><tr><td colspan='2'>[[4bcr]] 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BCR FirstGlance]. <br>
Line 29:		Line 29:
	[[Category: Histone acetyltransferase]]		[[Category: Histone acetyltransferase]]
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Bernardes, A]]		[[Category: Bernardes, A]]
	[[Category: Muniz, J R.C]]		[[Category: Muniz, J R.C]]

OCA at 12:10, 4 August 2016

OCA — Thu, 04 Aug 2016 12:10:48 GMT

←Older revision		Revision as of 12:10, 4 August 2016
Line 1:		Line 1:
		+
	==Structure of PPARalpha in complex with WY14643==		==Structure of PPARalpha in complex with WY14643==
	<StructureSection load='4bcr' size='340' side='right' caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>		<StructureSection load='4bcr' size='340' side='right' caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4bcr]] is a 2 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BCR FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4bcr]] 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BCR FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=WY1:2-({4-CHLORO-6-[(2,3-DIMETHYLPHENYL)AMINO]PYRIMIDIN-2-YL}SULFANYL)ACETIC+ACID'>WY1</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=WY1:2-({4-CHLORO-6-[(2,3-DIMETHYLPHENYL)AMINO]PYRIMIDIN-2-YL}SULFANYL)ACETIC+ACID'>WY1</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1i7g\|1i7g]], [[1k7l\|1k7l]], [[1kkq\|1kkq]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1i7g\|1i7g]], [[1k7l\|1k7l]], [[1kkq\|1kkq]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [http://www.ebi.ac.uk/pdbsum/4bcr PDBsum]</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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [http://pdbe.org/4bcr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [http://www.ebi.ac.uk/pdbsum/4bcr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4bcr ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 18:		Line 19:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 4bcr" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 26:		Line 28:
	</StructureSection>		</StructureSection>
	[[Category: Histone acetyltransferase]]		[[Category: Histone acetyltransferase]]
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Bernardes, A]]		[[Category: Bernardes, A]]
	[[Category: Muniz, J R.C]]		[[Category: Muniz, J R.C]]

OCA at 14:20, 24 December 2014

OCA — Wed, 24 Dec 2014 14:20:14 GMT

←Older revision		Revision as of 14:20, 24 December 2014
Line 8:		Line 8:
	<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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [http://www.ebi.ac.uk/pdbsum/4bcr PDBsum]</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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [http://www.ebi.ac.uk/pdbsum/4bcr PDBsum]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[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>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==

OCA at 08:53, 21 December 2014

OCA — Sun, 21 Dec 2014 08:53:10 GMT

←Older revision		Revision as of 08:53, 21 December 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_4bcr~~\| ~~PDB~~=4bcr \| ~~SCENE~~= }}	+	==Structure of PPARalpha in complex with WY14643==
-	===~~Structure~~ of PPARalpha in complex with WY14643~~===~~	+	<StructureSection load='4bcr' size='340' side='right' caption='[[4bcr]], [[Resolution\|resolution]] 2.50Å' scene=''>
-	~~{{ABSTRACT_PUBMED_23707408}}~~	+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[4bcr]] is a 2 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=4BCR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BCR FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=WY1:2-({4-CHLORO-6-[(2,3-DIMETHYLPHENYL)AMINO]PYRIMIDIN-2-YL}SULFANYL)ACETIC+ACID'>WY1</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1i7g\|1i7g]], [[1k7l\|1k7l]], [[1kkq\|1kkq]]</td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </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=4bcr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bcr OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bcr RCSB], [http://www.ebi.ac.uk/pdbsum/4bcr PDBsum]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Peroxisome proliferator-activated receptors (PPARs) are members of a superfamily of nuclear transcription factors. They are involved in mediating numerous physiological effects in humans, including glucose and lipid metabolism. PPARalpha ligands effectively treat dyslipidemia and have significant antiinflammatory and anti-atherosclerotic activities. These effects and their ligand-dependent activity make nuclear receptors obvious targets for drug design. Here, we present the structure of the human PPARalpha in complex with WY14643, a member of fibrate class of drug, and a widely used PPAR activator. The crystal structure of this complex suggests that WY14643 induces activation of PPARalpha in an unusual bipartite mechanism involving conventional direct helix 12 stabilization and an alternative mode that involves a second ligand in the pocket. We present structural observations, molecular dynamics and activity assays that support the importance of the second site in WY14643 action. The unique binding mode of WY14643 reveals a new pattern of nuclear receptor ligand recognition and suggests a novel basis for ligand design, offering clues for improving the binding affinity and selectivity of ligand. We show that binding of WY14643 to PPARalpha was associated with antiinflammatory disease in a human corneal cell model, suggesting possible applications for PPARalpha ligands.

-	~~==Function==~~	+	Molecular Mechanism of Peroxisome Proliferator-Activated Receptor alpha Activation by WY14643: a New Mode of Ligand Recognition and Receptor Stabilization.,Bernardes A, Souza PC, Muniz JR, Ricci CG, Ayers SD, Parekh NM, Godoy AS, Trivella DB, Reinach P, Webb P, Skaf MS, Polikarpov I J Mol Biol. 2013 May 21. pii: S0022-2836(13)00309-4. doi:, 10.1016/j.jmb.2013.05.010. PMID:23707408<ref>PMID:23707408</ref>
-	~~[[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>	+

-	~~==About this Structure==~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[4bcr]] is~~ a ~~2 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=4BCR OCA].~~	+	</div>

-	==~~Reference~~==	+	==See Also==
-	~~<ref group~~=~~"xtra">PMID:023707408</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	*[[Peroxisome Proliferator-Activated Receptors\|Peroxisome Proliferator-Activated Receptors]]
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
	[[Category: Histone acetyltransferase]]		[[Category: Histone acetyltransferase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Bernardes, A.]]	+	[[Category: Bernardes, A]]
-	[[Category: Muniz, J R.C.]]	+	[[Category: Muniz, J R.C]]
-	[[Category: Polikarpov, I.]]	+	[[Category: Polikarpov, I]]
	[[Category: Fibrate]]		[[Category: Fibrate]]
	[[Category: Nuclear receptor]]		[[Category: Nuclear receptor]]
	[[Category: Ppar]]		[[Category: Ppar]]
	[[Category: Transcription]]		[[Category: Transcription]]

OCA at 13:27, 19 June 2013

OCA — Wed, 19 Jun 2013 13:27:05 GMT

←Older revision		Revision as of 13:27, 19 June 2013
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	{{STRUCTURE_4bcr\| PDB=4bcr \| SCENE= }}
		+	===Structure of PPARalpha in complex with WY14643===
		+	{{ABSTRACT_PUBMED_23707408}}

-	~~The entry 4bcr~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	==Function==
		+	[[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>

-	~~Authors~~: ~~Bernardes, A~~.~~, Muniz, J~~.R.C.~~, Polikarpov, I~~.	+	==About this Structure==
		+	[[4bcr]] is a 2 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=4BCR OCA].

-	~~Description~~: ~~Structure of PPARalpha in complex with WY14643~~	+	==Reference==
		+	<ref group="xtra">PMID:023707408</ref><references group="xtra"/><references/>
		+	[[Category: Histone acetyltransferase]]
		+	[[Category: Homo sapiens]]
		+	[[Category: Bernardes, A.]]
		+	[[Category: Muniz, J R.C.]]
		+	[[Category: Polikarpov, I.]]
		+	[[Category: Fibrate]]
		+	[[Category: Nuclear receptor]]
		+	[[Category: Ppar]]
		+	[[Category: Transcription]]

OCA: Protected "4bcr" [edit=sysop:move=sysop]

OCA — Wed, 10 Oct 2012 06:44:30 GMT

Protected "4bcr" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:44, 10 October 2012

OCA: New page: '''Unreleased structure''' The entry 4bcr is ON HOLD until Paper Publication Authors: Bernardes, A., Muniz, J.R.C., Polikarpov, I. Description: Structure of PPARalpha in complex with W...

OCA — Wed, 10 Oct 2012 06:44:29 GMT

New page: '''Unreleased structure''' The entry 4bcr is ON HOLD until Paper Publication Authors: Bernardes, A., Muniz, J.R.C., Polikarpov, I. Description: Structure of PPARalpha in complex with W...

New page

'''Unreleased structure'''

The entry 4bcr is ON HOLD until Paper Publication

Authors: Bernardes, A., Muniz, J.R.C., Polikarpov, I.

Description: Structure of PPARalpha in complex with WY14643