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4n6h

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{{STRUCTURE_4n6h| PDB=4n6h | SCENE= }}
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==1.8 A Structure of the human delta opioid 7TM receptor (PSI Community Target)==
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===1.8 A Structure of the human delta opioid 7TM receptor===
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<StructureSection load='4n6h' size='340' side='right' caption='[[4n6h]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4n6h]] is a 1 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=4N6H OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4N6H FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EJ4:(4BS,8R,8AS,14BR)-7-(CYCLOPROPYLMETHYL)-5,6,7,8,14,14B-HEXAHYDRO-4,8-METHANO[1]BENZOFURO[2,3-A]PYRIDO[4,3-B]CARBAZOLE-1,8A(9H)-DIOL'>EJ4</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=PGE:TRIETHYLENE+GLYCOL'>PGE</scene>, <scene name='pdbligand=TLA:L(+)-TARTARIC+ACID'>TLA</scene><br>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4ej4|4ej4]]</td></tr>
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<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">OPRD, OPRD1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4n6h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4n6h OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4n6h RCSB], [http://www.ebi.ac.uk/pdbsum/4n6h PDBsum]</span></td></tr>
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<table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Opioids represent widely prescribed and abused medications, although their signal transduction mechanisms are not well understood. Here we present the 1.8 A high-resolution crystal structure of the human delta-opioid receptor (delta-OR), revealing the presence and fundamental role of a sodium ion in mediating allosteric control of receptor functional selectivity and constitutive activity. The distinctive delta-OR sodium ion site architecture is centrally located in a polar interaction network in the seven-transmembrane bundle core, with the sodium ion stabilizing a reduced agonist affinity state, and thereby modulating signal transduction. Site-directed mutagenesis and functional studies reveal that changing the allosteric sodium site residue Asn 131 to an alanine or a valine augments constitutive beta-arrestin-mediated signalling. Asp95Ala, Asn310Ala and Asn314Ala mutations transform classical delta-opioid antagonists such as naltrindole into potent beta-arrestin-biased agonists. The data establish the molecular basis for allosteric sodium ion control in opioid signalling, revealing that sodium-coordinating residues act as 'efficacy switches' at a prototypic G-protein-coupled receptor.
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==Function==
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Molecular control of delta-opioid receptor signalling.,Fenalti G, Giguere PM, Katritch V, Huang XP, Thompson AA, Cherezov V, Roth BL, Stevens RC Nature. 2014 Feb 13;506(7487):191-6. doi: 10.1038/nature12944. Epub 2014 Jan 12. PMID:24413399<ref>PMID:24413399</ref>
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[[http://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function.
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==About this Structure==
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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[[4n6h]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4N6H OCA].
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</div>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Bacillus coli migula 1895]]
[[Category: Cherezov, V.]]
[[Category: Cherezov, V.]]
[[Category: Fenalti, G.]]
[[Category: Fenalti, G.]]
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[[Category: Membrane]]
[[Category: Membrane]]
[[Category: Membrane protein]]
[[Category: Membrane protein]]
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[[Category: Psi:biology]]
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[[Category: Psi-biology]]
[[Category: Signaling protein]]
[[Category: Signaling protein]]
[[Category: Sodium regulation]]
[[Category: Sodium regulation]]
[[Category: Structural genomic]]
[[Category: Structural genomic]]

Revision as of 13:37, 18 May 2014

1.8 A Structure of the human delta opioid 7TM receptor (PSI Community Target)

4n6h, resolution 1.80Å

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