OCA at 15:25, 29 November 2023

OCA — Wed, 29 Nov 2023 15:25:23 GMT

←Older revision		Revision as of 15:25, 29 November 2023
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-	====	+	==X-ray structure of human PPARalpha ligand binding domain-GW7647-SRC1 coactivator peptide co-crystals obtained by delipidation and co-crystallization==
-	<StructureSection load='7bq3' size='340' side='right'caption='[[7bq3]]' scene=''>	+	<StructureSection load='7bq3' size='340' side='right'caption='[[7bq3]], [[Resolution\|resolution]] 1.98Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id= OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol= FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7bq3]] 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=7BQ3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7BQ3 FirstGlance]. <br>
-	</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://proteopedia.org/fgij/fg.htm?mol=7bq3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7bq3 OCA], [~~http~~://pdbe.org/7bq3 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=7bq3 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/7bq3 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=7bq3 ProSAT]</span></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]] 1.98Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=2VN:2-[(4-{2-[(4-cyclohexylbutyl)(cyclohexylcarbamoyl)amino]ethyl}phenyl)sulfanyl]-2-methylpropanoic+acid'>2VN</scene></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=7bq3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7bq3 OCA], [https://pdbe.org/7bq3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7bq3 RCSB], [https://www.ebi.ac.uk/pdbsum/7bq3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7bq3 ProSAT]</span></td></tr>
	</table>		</table>
		+	== 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>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Most triacylglycerol-lowering fibrates have been developed in the 1960s-1980s before their molecular target, peroxisome proliferator-activated receptor alpha (PPARalpha), was identified. Twenty-one ligand-bound PPARalpha structures have been deposited in the Protein Data Bank since 2001; however, binding modes of fibrates and physiological ligands remain unknown. Here we show thirty-four X-ray crystallographic structures of the PPARalpha ligand-binding domain, which are composed of a "Center" and four "Arm" regions, in complexes with five endogenous fatty acids, six fibrates in clinical use, and six synthetic PPARalpha agonists. High-resolution structural analyses, in combination with coactivator recruitment and thermostability assays, demonstrate that stearic and palmitic acids are presumably physiological ligands; coordination to Arm III is important for high PPARalpha potency/selectivity of pemafibrate and GW7647; and agonistic activities of four fibrates are enhanced by the partial agonist GW9662. These results renew our understanding of PPARalpha ligand recognition and contribute to the molecular design of next-generation PPAR-targeted drugs.
		+
		+	PPARalpha Ligand-Binding Domain Structures with Endogenous Fatty Acids and Fibrates.,Kamata S, Oyama T, Saito K, Honda A, Yamamoto Y, Suda K, Ishikawa R, Itoh T, Watanabe Y, Shibata T, Uchida K, Suematsu M, Ishii I iScience. 2020 Oct 23;23(11):101727. doi: 10.1016/j.isci.2020.101727. eCollection, 2020 Nov 20. PMID:33205029<ref>PMID:33205029</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7bq3" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Peroxisome proliferator-activated receptor 3D structures\|Peroxisome proliferator-activated receptor 3D structures]]
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Z-disk~~]]	+	[[Category: Akahane M]]
		+	[[Category: Ishii I]]
		+	[[Category: Ishikawa R]]
		+	[[Category: Kamata S]]
		+	[[Category: Oyama T]]

OCA at 08:02, 11 November 2020

OCA — Wed, 11 Nov 2020 08:02:25 GMT

←Older revision		Revision as of 08:02, 11 November 2020
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-	'''Unreleased structure'''

-	~~The entry~~ 7bq3 ~~is ON HOLD until Paper Publication~~	+	====
-		+	<StructureSection load='7bq3' size='340' side='right'caption='[[7bq3]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id= OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol= FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=7bq3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7bq3 OCA], [http://pdbe.org/7bq3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=7bq3 RCSB], [http://www.ebi.ac.uk/pdbsum/7bq3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=7bq3 ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Z-disk]]

OCA at 05:39, 15 April 2020

OCA — Wed, 15 Apr 2020 05:39:54 GMT

←Older revision		Revision as of 05:39, 15 April 2020
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7bq3 is ON HOLD	+	The entry 7bq3 is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "7bq3" [edit=sysop:move=sysop]

OCA — Wed, 01 Apr 2020 07:53:38 GMT

Protected "7bq3" [edit=sysop:move=sysop]

←Older revision

Revision as of 07:53, 1 April 2020

OCA: New page: '''Unreleased structure''' The entry 7bq3 is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 01 Apr 2020 07:53:37 GMT

New page: '''Unreleased structure''' The entry 7bq3 is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7bq3 is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]

7bq3 - Revision history

OCA at 15:25, 29 November 2023

OCA at 08:02, 11 November 2020

OCA at 05:39, 15 April 2020

OCA: Protected "7bq3" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 7bq3 is ON HOLD Authors: Description: Category: Unreleased Structures