5dhh

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==The crystal structure of nociceptin/orphanin FQ peptide receptor (NOP) in complex with SB-612111 (PSI Community Target)==
==The crystal structure of nociceptin/orphanin FQ peptide receptor (NOP) in complex with SB-612111 (PSI Community Target)==
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<StructureSection load='5dhh' size='340' side='right' caption='[[5dhh]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
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<StructureSection load='5dhh' size='340' side='right'caption='[[5dhh]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5dhh]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DHH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DHH FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5dhh]] 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=5DHH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5DHH FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DGW:(5S,7S)-7-{[4-(2,6-DICHLOROPHENYL)PIPERIDIN-1-YL]METHYL}-1-METHYL-6,7,8,9-TETRAHYDRO-5H-BENZO[7]ANNULEN-5-OL'>DGW</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.004&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4ea3|4ea3]]</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DGW:(5S,7S)-7-{[4-(2,6-DICHLOROPHENYL)PIPERIDIN-1-YL]METHYL}-1-METHYL-6,7,8,9-TETRAHYDRO-5H-BENZO[7]ANNULEN-5-OL'>DGW</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></td></tr>
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<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=5dhh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dhh OCA], [http://pdbe.org/5dhh PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5dhh RCSB], [http://www.ebi.ac.uk/pdbsum/5dhh PDBsum]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5dhh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5dhh OCA], [https://pdbe.org/5dhh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5dhh RCSB], [https://www.ebi.ac.uk/pdbsum/5dhh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5dhh ProSAT]</span></td></tr>
</table>
</table>
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== Function ==
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[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Understanding the mechanism by which ligands affect receptor conformational equilibria is key in accelerating membrane protein structural biology. In the case of G protein-coupled receptors (GPCRs), we currently pursue a brute-force approach for identifying ligands that stabilize receptors and facilitate crystallogenesis. The nociceptin/orphanin FQ peptide receptor (NOP) is a member of the opioid receptor subfamily of GPCRs for which many structurally diverse ligands are available for screening. We observed that antagonist potency is correlated with a ligand's ability to induce receptor stability (Tm) and crystallogenesis. Using this screening strategy, we solved two structures of NOP in complex with top candidate ligands SB-612111 and C-35. Docking studies indicate that while potent, stabilizing antagonists strongly favor a single binding orientation, less potent ligands can adopt multiple binding modes, contributing to their low Tm values. These results suggest a mechanism for ligand-aided crystallogenesis whereby potent antagonists stabilize a single ligand-receptor conformational pair.
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The Importance of Ligand-Receptor Conformational Pairs in Stabilization: Spotlight on the N/OFQ G Protein-Coupled Receptor.,Miller RL, Thompson AA, Trapella C, Guerrini R, Malfacini D, Patel N, Han GW, Cherezov V, Calo G, Katritch V, Stevens RC Structure. 2015 Oct 24. pii: S0969-2126(15)00407-4. doi:, 10.1016/j.str.2015.07.024. PMID:26526853<ref>PMID:26526853</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 5dhh" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Calo, G]]
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[[Category: Escherichia coli]]
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[[Category: Cherezov, V]]
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[[Category: Homo sapiens]]
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[[Category: GPCR, GPCR Network]]
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[[Category: Large Structures]]
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[[Category: Guerrini, R]]
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[[Category: Calo G]]
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[[Category: Han, G W]]
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[[Category: Cherezov V]]
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[[Category: Katritch, V]]
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[[Category: Guerrini R]]
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[[Category: Malfacini, D]]
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[[Category: Han GW]]
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[[Category: Miller, R L]]
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[[Category: Katritch V]]
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[[Category: Patel, N]]
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[[Category: Malfacini D]]
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[[Category: Stevens, R C]]
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[[Category: Miller RL]]
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[[Category: Thompson, A A]]
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[[Category: Patel N]]
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[[Category: Trapella, C]]
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[[Category: Stevens RC]]
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[[Category: Bret]]
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[[Category: Thompson AA]]
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[[Category: G protein-coupled receptor]]
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[[Category: Trapella C]]
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[[Category: Gpcr]]
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[[Category: Gpcr network]]
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[[Category: Lipidic cubic phase]]
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[[Category: Membrane protein]]
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[[Category: N/ofq]]
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[[Category: Nociceptin/orphanin fq peptide receptor]]
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[[Category: Nop]]
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[[Category: Opioid receptor]]
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[[Category: Orl-1]]
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[[Category: Psi-biology]]
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[[Category: Psicnt-127]]
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[[Category: Receptor-ligand conformational pair]]
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[[Category: Signaling protein]]
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[[Category: Structural genomic]]
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Current revision

The crystal structure of nociceptin/orphanin FQ peptide receptor (NOP) in complex with SB-612111 (PSI Community Target)

PDB ID 5dhh

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