5wr1 - Revision history

OCA at 07:35, 13 December 2017

OCA — Wed, 13 Dec 2017 07:35:41 GMT

←Older revision		Revision as of 07:35, 13 December 2017
Line 3:		Line 3:
	<StructureSection load='5wr1' size='340' side='right' caption='[[5wr1]], [[Resolution\|resolution]] 2.34Å' scene=''>		<StructureSection load='5wr1' size='340' side='right' caption='[[5wr1]], [[Resolution\|resolution]] 2.34Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5wr1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5WR1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5WR1 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5wr1]] 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=5WR1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5WR1 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8XO:2-[E-(E-16-azido-2-oxidanylidene-hexadec-3-enylidene)amino]ethanoic+acid'>8XO</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8XO:2-[E-(E-16-azido-2-oxidanylidene-hexadec-3-enylidene)amino]ethanoic+acid'>8XO</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PPARG, NR1C3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=5wr1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5wr1 OCA], [http://pdbe.org/5wr1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5wr1 RCSB], [http://www.ebi.ac.uk/pdbsum/5wr1 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5wr1 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=5wr1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5wr1 OCA], [http://pdbe.org/5wr1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5wr1 RCSB], [http://www.ebi.ac.uk/pdbsum/5wr1 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5wr1 ProSAT]</span></td></tr>
	</table>		</table>
Line 24:		Line 25:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Itoh, T]]		[[Category: Itoh, T]]
	[[Category: Kojima, H]]		[[Category: Kojima, H]]

OCA at 07:45, 22 November 2017

OCA — Wed, 22 Nov 2017 07:45:11 GMT

←Older revision		Revision as of 07:45, 22 November 2017
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5wr1 is ~~ON HOLD~~	+	==Covalent bond formation of bifunctional ligand with hPPARg-LBD==
		+	<StructureSection load='5wr1' size='340' side='right' caption='[[5wr1]], [[Resolution\|resolution]] 2.34Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5wr1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5WR1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5WR1 FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=8XO:2-[E-(E-16-azido-2-oxidanylidene-hexadec-3-enylidene)amino]ethanoic+acid'>8XO</scene></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=5wr1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5wr1 OCA], [http://pdbe.org/5wr1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5wr1 RCSB], [http://www.ebi.ac.uk/pdbsum/5wr1 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5wr1 ProSAT]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/PPARG_HUMAN PPARG_HUMAN]] Note=Defects in PPARG can lead to type 2 insulin-resistant diabetes and hyptertension. PPARG mutations may be associated with colon cancer. Defects in PPARG may be associated with susceptibility to obesity (OBESITY) [MIM:[http://omim.org/entry/601665 601665]]. It is a condition characterized by an increase of body weight beyond the limitation of skeletal and physical requirements, as the result of excessive accumulation of body fat.<ref>PMID:9753710</ref> Defects in PPARG are the cause of familial partial lipodystrophy type 3 (FPLD3) [MIM:[http://omim.org/entry/604367 604367]]. Familial partial lipodystrophies (FPLD) are a heterogeneous group of genetic disorders characterized by marked loss of subcutaneous (sc) fat from the extremities. Affected individuals show an increased preponderance of insulin resistance, diabetes mellitus and dyslipidemia.<ref>PMID:12453919</ref> <ref>PMID:11788685</ref> Genetic variations in PPARG can be associated with susceptibility to glioma type 1 (GLM1) [MIM:[http://omim.org/entry/137800 137800]]. Gliomas are central nervous system neoplasms derived from glial cells and comprise astrocytomas, glioblastoma multiforme, oligodendrogliomas, and ependymomas. Note=Polymorphic PPARG alleles have been found to be significantly over-represented among a cohort of American patients with sporadic glioblastoma multiforme suggesting a possible contribution to disease susceptibility.
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/PPARG_HUMAN PPARG_HUMAN]] Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated proinflammatory responses.<ref>PMID:9065481</ref> <ref>PMID:16150867</ref> <ref>PMID:20829347</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Site-specific labeling is an important methodology to elucidate the biological function of a target protein. Here, we report a strategy for site-specific chemical labeling, termed the "on-site reaction". We designed and readily synthesized a bifunctional ligand possessing two reaction sites, an enone and an azide moiety. This strategy involves an on-site conjugate addition reaction with protein followed by a Huisgen cycloaddition reaction. We demonstrate this strategy by using fluorescein as a probe and peroxisome proliferator activated receptor gamma (PPARgamma) as a target protein. The reactions were evaluated by ESI-mass analysis and the binding site and modes of binding were revealed by X-ray crystallization analysis. The proposed methodology can easily convert a covalent ligand into chemical tool for protein functional analysis and the identification of drug targets.

-	~~Authors: Kojima~~, H., Itoh, T., Yamamoto, K.	+	On-site reaction for PPARgamma modification using a specific bifunctional ligand.,Kojima H, Itoh T, Yamamoto K Bioorg Med Chem. 2017 Oct 23. pii: S0968-0896(17)31943-0. doi:, 10.1016/j.bmc.2017.10.024. PMID:29097031<ref>PMID:29097031</ref>

-	~~Description: Covalent bond formation~~ of ~~bifunctional ligand with hPPARg-LBD~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[Category: Unreleased Structures]]~~	+	</div>
-	~~[[Category~~: ~~Yamamoto, K]]~~	+	<div class="pdbe-citations 5wr1" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
	[[Category: Itoh, T]]		[[Category: Itoh, T]]
	[[Category: Kojima, H]]		[[Category: Kojima, H]]
		+	[[Category: Yamamoto, K]]
		+	[[Category: Receptor]]
		+	[[Category: Transcription]]

OCA: Protected "5wr1" [edit=sysop:move=sysop]

OCA — Fri, 09 Dec 2016 18:18:46 GMT

Protected "5wr1" [edit=sysop:move=sysop]

←Older revision

Revision as of 18:18, 9 December 2016

OCA: New page: '''Unreleased structure''' The entry 5wr1 is ON HOLD Authors: Kojima, H., Itoh, T., Yamamoto, K. Description: Covalent bond formation of bifunctional ligand with hPPARg-LBD [[Category:...

OCA — Fri, 09 Dec 2016 18:18:45 GMT

New page: '''Unreleased structure''' The entry 5wr1 is ON HOLD Authors: Kojima, H., Itoh, T., Yamamoto, K. Description: Covalent bond formation of bifunctional ligand with hPPARg-LBD [[Category:...

New page

'''Unreleased structure'''

The entry 5wr1 is ON HOLD

Authors: Kojima, H., Itoh, T., Yamamoto, K.

Description: Covalent bond formation of bifunctional ligand with hPPARg-LBD
[[Category: Unreleased Structures]]
[[Category: Yamamoto, K]]
[[Category: Itoh, T]]
[[Category: Kojima, H]]