5ywy - Revision history

OCA at 08:46, 19 December 2018

OCA — Wed, 19 Dec 2018 08:46:12 GMT

←Older revision		Revision as of 08:46, 19 December 2018
Line 10:		Line 10:
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/PE2R4_HUMAN PE2R4_HUMAN]] Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. Has a relaxing effect on smooth muscle. May play an important role in regulating renal hemodynamics, intestinal epithelial transport, adrenal aldosterone secretion, and uterine function.		[[http://www.uniprot.org/uniprot/PE2R4_HUMAN PE2R4_HUMAN]] Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. Has a relaxing effect on smooth muscle. May play an important role in regulating renal hemodynamics, intestinal epithelial transport, adrenal aldosterone secretion, and uterine function.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Prostaglandin E receptor EP4, a G-protein-coupled receptor, is involved in disorders such as cancer and autoimmune disease. Here, we report the crystal structure of human EP4 in complex with its antagonist ONO-AE3-208 and an inhibitory antibody at 3.2 A resolution. The structure reveals that the extracellular surface is occluded by the extracellular loops and that the antagonist lies at the interface with the lipid bilayer, proximal to the highly conserved Arg316 residue in the seventh transmembrane domain. Functional and docking studies demonstrate that the natural agonist PGE2 binds in a similar manner. This structural information also provides insight into the ligand entry pathway from the membrane bilayer to the EP4 binding pocket. Furthermore, the structure reveals that the antibody allosterically affects the ligand binding of EP4. These results should facilitate the design of new therapeutic drugs targeting both orthosteric and allosteric sites in this receptor family.
		+
		+	Ligand binding to human prostaglandin E receptor EP4 at the lipid-bilayer interface.,Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K, Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T Nat Chem Biol. 2019 Jan;15(1):18-26. doi: 10.1038/s41589-018-0131-3. Epub 2018, Dec 3. PMID:30510193<ref>PMID:30510193</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 5ywy" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>

OCA at 07:06, 12 December 2018

OCA — Wed, 12 Dec 2018 07:06:25 GMT

←Older revision		Revision as of 07:06, 12 December 2018
Line 1:		Line 1:

-	==Crystal structure of the ~~clinically important GPCR~~ in complex with ~~functional antibody.~~==	+	==Crystal structure of the human prostaglandin E receptor EP4 in complex with Fab and ONO-AE3-208==
	<StructureSection load='5ywy' size='340' side='right' caption='[[5ywy]], [[Resolution\|resolution]] 3.20Å' scene=''>		<StructureSection load='5ywy' size='340' side='right' caption='[[5ywy]], [[Resolution\|resolution]] 3.20Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5ywy]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YWY OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5YWY FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5ywy]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human] and [http://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YWY OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5YWY FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7UR:4-[4-cyano-2-[[(2R)-2-(4-fluoranylnaphthalen-1-yl)propanoyl]amino]phenyl]butanoic+acid'>7UR</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7UR:4-[4-cyano-2-[[(2R)-2-(4-fluoranylnaphthalen-1-yl)propanoyl]amino]phenyl]butanoic+acid'>7UR</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PTGER4, PTGER2 ([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=5ywy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ywy OCA], [http://pdbe.org/5ywy PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ywy RCSB], [http://www.ebi.ac.uk/pdbsum/5ywy PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ywy 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=5ywy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ywy OCA], [http://pdbe.org/5ywy PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ywy RCSB], [http://www.ebi.ac.uk/pdbsum/5ywy PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ywy ProSAT]</span></td></tr>
	</table>		</table>
Line 11:		Line 12:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Lk3 transgenic mice]]
	[[Category: Horita, S]]		[[Category: Horita, S]]
	[[Category: Iwata, S]]		[[Category: Iwata, S]]

OCA at 06:29, 5 December 2018

OCA — Wed, 05 Dec 2018 06:29:59 GMT

←Older revision		Revision as of 06:29, 5 December 2018
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5ywy is ~~ON HOLD until Paper Publication~~	+	==Crystal structure of the clinically important GPCR in complex with functional antibody.==
-		+	<StructureSection load='5ywy' size='340' side='right' caption='[[5ywy]], [[Resolution\|resolution]] 3.20Å' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[5ywy]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YWY OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5YWY FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7UR:4-[4-cyano-2-[[(2R)-2-(4-fluoranylnaphthalen-1-yl)propanoyl]amino]phenyl]butanoic+acid'>7UR</scene></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	<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=5ywy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ywy OCA], [http://pdbe.org/5ywy PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ywy RCSB], [http://www.ebi.ac.uk/pdbsum/5ywy PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ywy ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/PE2R4_HUMAN PE2R4_HUMAN]] Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. Has a relaxing effect on smooth muscle. May play an important role in regulating renal hemodynamics, intestinal epithelial transport, adrenal aldosterone secretion, and uterine function.
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Horita, S]]
		+	[[Category: Iwata, S]]
		+	[[Category: Kobayashi, T]]
		+	[[Category: Morimoto, K]]
		+	[[Category: Suno, R]]
		+	[[Category: Toyoda, Y]]
		+	[[Category: Functional antibody]]
		+	[[Category: G-protein coupled receptor]]
		+	[[Category: Lipid mediator]]
		+	[[Category: Membrane protein]]
		+	[[Category: Signaling protein-immune system]]
		+	[[Category: Signaling protein-immune system complex]]

OCA at 07:11, 27 December 2017

OCA — Wed, 27 Dec 2017 07:11:22 GMT

←Older revision		Revision as of 07:11, 27 December 2017
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 5ywy is ON HOLD	+	The entry 5ywy is ON HOLD until Paper Publication

	Authors:		Authors:

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

OCA — Wed, 06 Dec 2017 06:01:40 GMT

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

←Older revision

Revision as of 06:01, 6 December 2017

OCA: New page: '''Unreleased structure''' The entry 5ywy is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 06 Dec 2017 06:01:38 GMT

New page: '''Unreleased structure''' The entry 5ywy is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 5ywy is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]