4ea3 - Revision history

OCA at 02:49, 21 November 2024

2024-11-21T02:49:24Z

← Older revision		Revision as of 02:49, 21 November 2024
Line 9:		Line 9:
	</table>		</table>
	== Function ==		== Function ==
	[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.[https://www.uniprot.org/uniprot/OPRX_HUMAN OPRX_HUMAN] G-protein coupled opioid receptor that functions as receptor for the endogenous neuropeptide nociceptin. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling via G proteins mediates inhibition of adenylate cyclase activity and calcium channel activity. Arrestins modulate signaling via G proteins and mediate the activation of alternative signaling pathways that lead to the activation of MAP kinases. Plays a role in modulating nociception and the perception of pain. Plays a role in the regulation of locomotor activity by the neuropeptide nociceptin.<ref>PMID:11238602</ref> <ref>PMID:12568343</ref> <ref>PMID:22596163</ref> <ref>PMID:23086955</ref> <ref>PMID:8137918</ref>		[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.[https://www.uniprot.org/uniprot/OPRX_HUMAN OPRX_HUMAN] G-protein coupled opioid receptor that functions as a receptor for the endogenous neuropeptide nociceptin. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling via G proteins mediates inhibition of adenylate cyclase activity and calcium channel activity. Arrestins modulate signaling via G proteins and mediate the activation of alternative signaling pathways that lead to the activation of MAP kinases. Plays a role in modulating nociception and the perception of pain. Plays a role in the regulation of locomotor activity by the neuropeptide nociceptin.<ref>PMID:11238602</ref> <ref>PMID:12568343</ref> <ref>PMID:22596163</ref> <ref>PMID:23086955</ref> <ref>PMID:8137918</ref>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			Members of the opioid receptor family of G-protein-coupled receptors (GPCRs) are found throughout the peripheral and central nervous system, where they have key roles in nociception and analgesia. Unlike the 'classical' opioid receptors, delta, kappa and mu (delta-OR, kappa-OR and mu-OR), which were delineated by pharmacological criteria in the 1970s and 1980s, the nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP, also known as ORL-1) was discovered relatively recently by molecular cloning and characterization of an orphan GPCR. Although it shares high sequence similarity with classical opioid GPCR subtypes ( approximately 60%), NOP has a markedly distinct pharmacology, featuring activation by the endogenous peptide N/OFQ, and unique selectivity for exogenous ligands. Here we report the crystal structure of human NOP, solved in complex with the peptide mimetic antagonist compound-24 (C-24) (ref. 4), revealing atomic details of ligand-receptor recognition and selectivity. Compound-24 mimics the first four amino-terminal residues of the NOP-selective peptide antagonist UFP-101, a close derivative of N/OFQ, and provides important clues to the binding of these peptides. The X-ray structure also shows substantial conformational differences in the pocket regions between NOP and the classical opioid receptors kappa (ref. 5) and mu (ref. 6), and these are probably due to a small number of residues that vary between these receptors. The NOP-compound-24 structure explains the divergent selectivity profile of NOP and provides a new structural template for the design of NOP ligands.

			Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic.,Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V, Stevens RC Nature. 2012 May 16;485(7398):395-9. doi: 10.1038/nature11085. PMID:22596163<ref>PMID:22596163</ref>

			From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
			<div class="pdbe-citations 4ea3" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==

OCA at 14:56, 14 March 2024

2024-03-14T14:56:24Z

← Older revision		Revision as of 14:56, 14 March 2024
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4ea3]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4EA3 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ea3]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4EA3 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0NN:1-BENZYL-N-[3-(1H,3H-SPIRO[2-BENZOFURAN-1,4-PIPERIDIN]-1-YL)PROPYL]-D-PROLINAMIDE'>0NN</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</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]] 3.013Å</td></tr>
			<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0NN:1-BENZYL-N-[3-(1H,3H-SPIRO[2-BENZOFURAN-1,4-PIPERIDIN]-1-YL)PROPYL]-D-PROLINAMIDE'>0NN</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</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=4ea3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ea3 OCA], [https://pdbe.org/4ea3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ea3 RCSB], [https://www.ebi.ac.uk/pdbsum/4ea3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ea3 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=4ea3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ea3 OCA], [https://pdbe.org/4ea3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ea3 RCSB], [https://www.ebi.ac.uk/pdbsum/4ea3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ea3 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function.[[https://www.uniprot.org/uniprot/OPRX_HUMAN OPRX_HUMAN]] G-protein coupled opioid receptor that functions as receptor for the endogenous neuropeptide nociceptin. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling via G proteins mediates inhibition of adenylate cyclase activity and calcium channel activity. Arrestins modulate signaling via G proteins and mediate the activation of alternative signaling pathways that lead to the activation of MAP kinases. Plays a role in modulating nociception and the perception of pain. Plays a role in the regulation of locomotor activity by the neuropeptide nociceptin.<ref>PMID:11238602</ref> <ref>PMID:12568343</ref> <ref>PMID:22596163</ref> <ref>PMID:23086955</ref> <ref>PMID:8137918</ref>		[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.[https://www.uniprot.org/uniprot/OPRX_HUMAN OPRX_HUMAN] G-protein coupled opioid receptor that functions as receptor for the endogenous neuropeptide nociceptin. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling via G proteins mediates inhibition of adenylate cyclase activity and calcium channel activity. Arrestins modulate signaling via G proteins and mediate the activation of alternative signaling pathways that lead to the activation of MAP kinases. Plays a role in modulating nociception and the perception of pain. Plays a role in the regulation of locomotor activity by the neuropeptide nociceptin.<ref>PMID:11238602</ref> <ref>PMID:12568343</ref> <ref>PMID:22596163</ref> <ref>PMID:23086955</ref> <ref>PMID:8137918</ref>
	~~<div style="background-color:#fffaf0;">~~
	~~== Publication Abstract from PubMed ==~~
	Members of the opioid receptor family of G-protein-coupled receptors (GPCRs) are found throughout the peripheral and central nervous system, where they have key roles in nociception and analgesia. Unlike the 'classical' opioid receptors, delta, kappa and mu (delta-OR, kappa-OR and mu-OR), which were delineated by pharmacological criteria in the 1970s and 1980s, the nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP, also known as ORL-1) was discovered relatively recently by molecular cloning and characterization of an orphan GPCR. Although it shares high sequence similarity with classical opioid GPCR subtypes ( approximately 60%), NOP has a markedly distinct pharmacology, featuring activation by the endogenous peptide N/OFQ, and unique selectivity for exogenous ligands. Here we report the crystal structure of human NOP, solved in complex with the peptide mimetic antagonist compound-24 (C-24) (ref. 4), revealing atomic details of ligand-receptor recognition and selectivity. Compound-24 mimics the first four amino-terminal residues of the NOP-selective peptide antagonist UFP-101, a close derivative of N/OFQ, and provides important clues to the binding of these peptides. The X-ray structure also shows substantial conformational differences in the pocket regions between NOP and the classical opioid receptors kappa (ref. 5) and mu (ref. 6), and these are probably due to a small number of residues that vary between these receptors. The NOP-compound-24 structure explains the divergent selectivity profile of NOP and provides a new structural template for the design of NOP ligands.

	Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic.,Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V, Stevens RC Nature. 2012 May 16;485(7398):395-9. doi: 10.1038/nature11085. PMID:22596163<ref>PMID:22596163</ref>

	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~
	~~</div>~~
	~~<div class="pdbe-citations 4ea3" style="background-color:#fffaf0;"></div~~>

	==See Also==		==See Also==

OCA at 06:59, 28 September 2022

2022-09-28T06:59:35Z

← Older revision		Revision as of 06:59, 28 September 2022
Line 1:		Line 1:

	==Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic==		==Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic==
	<StructureSection load='4ea3' size='340' side='right' caption='[[4ea3]], [[Resolution\|resolution]] 3.01Å' scene=''>		<StructureSection load='4ea3' size='340' side='right'caption='[[4ea3]], [[Resolution\|resolution]] 3.01Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4ea3]] is a 2 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~"bacillus_coli"_migula_1895 "bacillus~~ coli~~" migula 1895~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4EA3 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ea3]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4EA3 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0NN:1-BENZYL-N-[3-(1H,3H-SPIRO[2-BENZOFURAN-1,4-PIPERIDIN]-1-YL)PROPYL]-D-PROLINAMIDE'>0NN</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>~~</td></tr>~~		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0NN:1-BENZYL-N-[3-(1H,3H-SPIRO[2-BENZOFURAN-1,4-PIPERIDIN]-1-YL)PROPYL]-D-PROLINAMIDE'>0NN</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">OOR, OPRL1, ORL1, cybC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</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=4ea3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ea3 OCA], [https://pdbe.org/4ea3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ea3 RCSB], [https://www.ebi.ac.uk/pdbsum/4ea3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ea3 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=4ea3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ea3 OCA], [~~http~~://pdbe.org/4ea3 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4ea3 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4ea3 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4ea3 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[~~http~~://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function.		[[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function.[[https://www.uniprot.org/uniprot/OPRX_HUMAN OPRX_HUMAN]] G-protein coupled opioid receptor that functions as receptor for the endogenous neuropeptide nociceptin. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling via G proteins mediates inhibition of adenylate cyclase activity and calcium channel activity. Arrestins modulate signaling via G proteins and mediate the activation of alternative signaling pathways that lead to the activation of MAP kinases. Plays a role in modulating nociception and the perception of pain. Plays a role in the regulation of locomotor activity by the neuropeptide nociceptin.<ref>PMID:11238602</ref> <ref>PMID:12568343</ref> <ref>PMID:22596163</ref> <ref>PMID:23086955</ref> <ref>PMID:8137918</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 19:		Line 18:
	</div>		</div>
	<div class="pdbe-citations 4ea3" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 4ea3" style="background-color:#fffaf0;"></div>

			==See Also==
			*[[Opioid receptor\|Opioid receptor]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Bacillus~~ coli ~~migula 1895~~]]		[[Category: Escherichia coli]]
	[[Category: ~~Calo, G~~]]		[[Category: Homo sapiens]]
	[[Category: ~~Cherezov, V~~]]		[[Category: Large Structures]]
	[[Category: ~~Chun, E~~]]		[[Category: Calo G]]
	[[Category: ~~GPCR, GPCR Network~~]]		[[Category: Cherezov V]]
	[[Category: Guerrini, R]]		[[Category: Chun E]]
	[[Category: Huang~~, X P~~]]		[[Category: Guerrini R]]
	[[Category: Katritch, V]]		[[Category: Huang XP]]
	[[Category: Liu, W]]		[[Category: Katritch V]]
	[[Category: Roth~~, B L~~]]		[[Category: Liu W]]
	[[Category: Stevens~~, R C~~]]		[[Category: Roth BL]]
	[[Category: Thompson~~, A A~~]]		[[Category: Stevens RC]]
	[[Category: Trapella, C]]		[[Category: Thompson AA]]
	[[Category: Vardy, E]]		[[Category: Trapella C]]
	[[Category: Wu, H]]		[[Category: Vardy E]]
	~~[[Category: Fusion]]~~		[[Category: Wu H]]
	~~[[Category: Gpcr membrane protein 7tm nop orl1 cytochrome b562]]~~
	~~[[Category: Membrane transmembrane]]~~
	~~[[Category: Nociceptin orphanin fq compound 24 opioid]]~~
	~~[[Category: Psi-biology gpcr network]]~~
	~~[[Category: Receptor]]~~
	~~[[Category: Signaling protein]]~~
	~~[[Category: Structural genomic~~]]

OCA at 08:00, 15 November 2017

2017-11-15T08:00:48Z

← Older revision		Revision as of 08:00, 15 November 2017
Line 19:		Line 19:
	</div>		</div>
	<div class="pdbe-citations 4ea3" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 4ea3" style="background-color:#fffaf0;"></div>

	~~==See Also==~~
	*[[G protein-coupled receptor\|G protein-coupled receptor]]
	*[[Opioid receptor\|Opioid receptor]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 16:28, 4 August 2016

2016-08-04T16:28:40Z

← Older revision		Revision as of 16:28, 4 August 2016
Line 1:		Line 1:

	==Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic==		==Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic==
	<StructureSection load='4ea3' size='340' side='right' caption='[[4ea3]], [[Resolution\|resolution]] 3.01Å' scene=''>		<StructureSection load='4ea3' size='340' side='right' caption='[[4ea3]], [[Resolution\|resolution]] 3.01Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4ea3]] 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=4EA3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4EA3 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ea3]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/"bacillus_coli"_migula_1895 "bacillus coli" migula 1895]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4EA3 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0NN:1-BENZYL-N-[3-(1H,3H-SPIRO[2-BENZOFURAN-1,4-PIPERIDIN]-1-YL)PROPYL]-D-PROLINAMIDE'>0NN</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0NN:1-BENZYL-N-[3-(1H,3H-SPIRO[2-BENZOFURAN-1,4-PIPERIDIN]-1-YL)PROPYL]-D-PROLINAMIDE'>0NN</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">OOR, OPRL1, ORL1, cybC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=~~9606 Homo sapiens~~])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">OOR, OPRL1, ORL1, cybC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</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=4ea3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ea3 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ea3 RCSB], [http://www.ebi.ac.uk/pdbsum/4ea3 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=4ea3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ea3 OCA], [http://pdbe.org/4ea3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ea3 RCSB], [http://www.ebi.ac.uk/pdbsum/4ea3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ea3 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 17:		Line 18:
	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 4ea3" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 25:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Homo sapiens~~]]		[[Category: Bacillus coli migula 1895]]
	[[Category: Calo, G]]		[[Category: Calo, G]]
	[[Category: Cherezov, V]]		[[Category: Cherezov, V]]

OCA at 17:01, 24 December 2014

2014-12-24T17:01:01Z

← Older revision		Revision as of 17:01, 24 December 2014
Line 1:		Line 1:
	[[~~Image~~:~~4ea3~~.~~png~~\|~~left~~\|~~200px~~]]		==Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic==
			<StructureSection load='4ea3' size='340' side='right' caption='[[4ea3]], [[Resolution\|resolution]] 3.01Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[4ea3]] 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=4EA3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4EA3 FirstGlance]. <br>
			</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0NN:1-BENZYL-N-[3-(1H,3H-SPIRO[2-BENZOFURAN-1,4-PIPERIDIN]-1-YL)PROPYL]-D-PROLINAMIDE'>0NN</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></td></tr>
			<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">OOR, OPRL1, ORL1, cybC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=4ea3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ea3 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ea3 RCSB], [http://www.ebi.ac.uk/pdbsum/4ea3 PDBsum]</span></td></tr>
			</table>
			== Function ==
			[[http://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function.
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			Members of the opioid receptor family of G-protein-coupled receptors (GPCRs) are found throughout the peripheral and central nervous system, where they have key roles in nociception and analgesia. Unlike the 'classical' opioid receptors, delta, kappa and mu (delta-OR, kappa-OR and mu-OR), which were delineated by pharmacological criteria in the 1970s and 1980s, the nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP, also known as ORL-1) was discovered relatively recently by molecular cloning and characterization of an orphan GPCR. Although it shares high sequence similarity with classical opioid GPCR subtypes ( approximately 60%), NOP has a markedly distinct pharmacology, featuring activation by the endogenous peptide N/OFQ, and unique selectivity for exogenous ligands. Here we report the crystal structure of human NOP, solved in complex with the peptide mimetic antagonist compound-24 (C-24) (ref. 4), revealing atomic details of ligand-receptor recognition and selectivity. Compound-24 mimics the first four amino-terminal residues of the NOP-selective peptide antagonist UFP-101, a close derivative of N/OFQ, and provides important clues to the binding of these peptides. The X-ray structure also shows substantial conformational differences in the pocket regions between NOP and the classical opioid receptors kappa (ref. 5) and mu (ref. 6), and these are probably due to a small number of residues that vary between these receptors. The NOP-compound-24 structure explains the divergent selectivity profile of NOP and provides a new structural template for the design of NOP ligands.

	~~{{STRUCTURE_4ea3\| PDB=4ea3 \| SCENE= }}~~		Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic.,Thompson AA, Liu W, Chun E, Katritch V, Wu H, Vardy E, Huang XP, Trapella C, Guerrini R, Calo G, Roth BL, Cherezov V, Stevens RC Nature. 2012 May 16;485(7398):395-9. doi: 10.1038/nature11085. PMID:22596163<ref>PMID:22596163</ref>

	~~===Structure~~ of the ~~N/OFQ Opioid Receptor in Complex with a Peptide Mimetic===~~		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
	~~{{ABSTRACT_PUBMED_22596163}}~~

	~~==About this Structure==~~
	~~[[4ea3]] 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=4EA3 OCA].~~

	==See Also==		==See Also==
	*[[G protein-coupled receptor\|G protein-coupled receptor]]		*[[G protein-coupled receptor\|G protein-coupled receptor]]
			*[[Opioid receptor\|Opioid receptor]]
	==~~Reference~~==		== References ==
	<~~ref group="xtra">PMID:022596163<~~/~~ref~~><~~references group="xtra"~~/>		<references/>
			__TOC__
			</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Calo, G.]]		[[Category: Calo, G]]
	[[Category: Cherezov, V.]]		[[Category: Cherezov, V]]
	[[Category: Chun, E.]]		[[Category: Chun, E]]
	[[Category: GPCR, GPCR Network.]]		[[Category: GPCR, GPCR Network]]
	[[Category: Guerrini, R.]]		[[Category: Guerrini, R]]
	[[Category: Huang, X P.]]		[[Category: Huang, X P]]
	[[Category: Katritch, V.]]		[[Category: Katritch, V]]
	[[Category: Liu, W.]]		[[Category: Liu, W]]
	[[Category: Roth, B L.]]		[[Category: Roth, B L]]
	[[Category: Stevens, R C.]]		[[Category: Stevens, R C]]
	[[Category: Thompson, A A.]]		[[Category: Thompson, A A]]
	[[Category: Trapella, C.]]		[[Category: Trapella, C]]
	[[Category: Vardy, E.]]		[[Category: Vardy, E]]
	[[Category: Wu, H.]]		[[Category: Wu, H]]
	[[Category: Fusion]]		[[Category: Fusion]]
	[[Category: Gpcr membrane protein 7tm nop orl1 cytochrome b562]]		[[Category: Gpcr membrane protein 7tm nop orl1 cytochrome b562]]

OCA at 07:21, 20 October 2012

2012-10-20T07:21:49Z

← Older revision		Revision as of 07:21, 20 October 2012
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	[[Image:4ea3.png\|left\|200px]]		[[Image:4ea3.png\|left\|200px]]

	~~<!--~~
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	{{STRUCTURE_4ea3\| PDB=4ea3 \| SCENE= }}		{{STRUCTURE_4ea3\| PDB=4ea3 \| SCENE= }}

	===Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic===		===Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic===


	~~<!--~~
	~~The line below this paragraph, {{ABSTRACT_PUBMED_22596163}}, adds the Publication Abstract to the page~~
	~~(as it appears on PubMed at http://www.pubmed.gov), where 22596163 is the PubMed ID number.~~
	~~-->~~
	{{ABSTRACT_PUBMED_22596163}}		{{ABSTRACT_PUBMED_22596163}}

	==About this Structure==		==About this Structure==
	[[4ea3]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens~~,_escherichia_coli~~ Homo sapiens~~, escherichia coli~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA].		[[4ea3]] 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=4EA3 OCA].

			==See Also==
			*[[G protein-coupled receptor\|G protein-coupled receptor]]

	==Reference==		==Reference==
	<ref group="xtra">PMID:022596163</ref><references group="xtra"/>		<ref group="xtra">PMID:022596163</ref><references group="xtra"/>
	[[Category: Homo sapiens~~, escherichia coli~~]]		[[Category: Homo sapiens]]
	[[Category: Calo, G.]]		[[Category: Calo, G.]]
	[[Category: Cherezov, V.]]		[[Category: Cherezov, V.]]

OCA at 05:07, 30 May 2012

2012-05-30T05:07:55Z

← Older revision		Revision as of 05:07, 30 May 2012
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	[[Image:4ea3.~~jpg~~\|left\|200px]]		[[Image:4ea3.png\|left\|200px]]

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	===Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic===		===Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic===


			<!--
			The line below this paragraph, {{ABSTRACT_PUBMED_22596163}}, adds the Publication Abstract to the page
			(as it appears on PubMed at http://www.pubmed.gov), where 22596163 is the PubMed ID number.
			-->
			{{ABSTRACT_PUBMED_22596163}}

	==About this Structure==		==About this Structure==
	[[4ea3]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens,_escherichia_coli Homo sapiens, escherichia coli]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA].		[[4ea3]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens,_escherichia_coli Homo sapiens, escherichia coli]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EA3 OCA].

			==Reference==
			<ref group="xtra">PMID:022596163</ref><references group="xtra"/>
	[[Category: Homo sapiens, escherichia coli]]		[[Category: Homo sapiens, escherichia coli]]
	[[Category: Calo, G.]]		[[Category: Calo, G.]]

OCA at 09:28, 25 April 2012

2012-04-25T09:28:55Z

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+[[Image:4ea3.jpg|left|200px]]
-The entry 4ea3 is ON HOLD  until Paper Publication
+<!--
-Authors: Thompson, A.A., Liu, W., Chun, E., Katritch, V., Wu, H., Vardy, E., Huang, X.P., Trapella, C., Guerrini, R., Calo, G., Roth, B.L., Cherezov, V., Stevens, R.C., GPCR Network (GPCR)
+===Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic===
-Description: Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic

OCA at 05:46, 4 April 2012

2012-04-04T05:46:38Z

← Older revision		Revision as of 05:46, 4 April 2012
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	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 4ea3 is ON HOLD		The entry 4ea3 is ON HOLD until Paper Publication

	Authors: Thompson, A.A., Liu, W., Chun, E., Katritch, V., Wu, H., Vardy, E., Huang, X.P., Trapella, C., Guerrini, R., Calo, G., Roth, B.L., Cherezov, V., Stevens, R.C., GPCR Network (GPCR)		Authors: Thompson, A.A., Liu, W., Chun, E., Katritch, V., Wu, H., Vardy, E., Huang, X.P., Trapella, C., Guerrini, R., Calo, G., Roth, B.L., Cherezov, V., Stevens, R.C., GPCR Network (GPCR)

	Description: Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic		Description: Structure of the N/OFQ Opioid Receptor in Complex with a Peptide Mimetic