8f7s

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'''Unreleased structure'''
 
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The entry 8f7s is ON HOLD
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==Gi bound delta-opioid receptor in complex with deltorphin==
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<StructureSection load='8f7s' size='340' side='right'caption='[[8f7s]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[8f7s]] is a 8 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens], [https://en.wikipedia.org/wiki/Phyllomedusa Phyllomedusa] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8F7S OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8F7S FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3&#8491;</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=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=DAL:D-ALANINE'>DAL</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene>, <scene name='pdbligand=PLM:PALMITIC+ACID'>PLM</scene></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=8f7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8f7s OCA], [https://pdbe.org/8f7s PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8f7s RCSB], [https://www.ebi.ac.uk/pdbsum/8f7s PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8f7s ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/OPRD_HUMAN OPRD_HUMAN] G-protein coupled receptor that functions as a receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine.<ref>PMID:22184124</ref> <ref>PMID:7808419</ref> <ref>PMID:8201839</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Opioids are effective analgesics, but their use is beset by serious side effects, including addiction and respiratory depression, which contribute to the ongoing opioid crisis. The human opioid system contains four opioid receptors (muOR, deltaOR, kappaOR, and NOPR) and a set of related endogenous opioid peptides (EOPs), which show distinct selectivity toward their respective opioid receptors (ORs). Despite being key to the development of safer analgesics, the mechanisms of molecular recognition and selectivity of EOPs to ORs remain unclear. Here, we systematically characterize the binding of EOPs to ORs and present five structures of EOP-OR-G(i) complexes, including beta-endorphin- and endomorphin-bound muOR, deltorphin-bound deltaOR, dynorphin-bound kappaOR, and nociceptin-bound NOPR. These structures, supported by biochemical results, uncover the specific recognition and selectivity of opioid peptides and the conserved mechanism of opioid receptor activation. These results provide a structural framework to facilitate rational design of safer opioid drugs for pain relief.
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Authors: Wang, Y., Zhuang, Y., DiBerto, J.F., Zhou, X.E., Schmitz, G.P., Yuan, Q., Jain, M.K., Liu, W., Melcher, K., Jiang, Y., Roth, B.L., Xu, H.E.
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, PMID:36638794<ref>PMID:36638794</ref>
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Description: Gi bound delta-opioid receptor in complex with deltorphin
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Zhou, X.E]]
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<div class="pdbe-citations 8f7s" style="background-color:#fffaf0;"></div>
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[[Category: Xu, H.E]]
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[[Category: Jain, M.K]]
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==See Also==
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[[Category: Melcher, K]]
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*[[Opioid receptor|Opioid receptor]]
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[[Category: Liu, W]]
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*[[Transducin 3D structures|Transducin 3D structures]]
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[[Category: Diberto, J.F]]
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== References ==
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[[Category: Jiang, Y]]
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<references/>
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[[Category: Wang, Y]]
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__TOC__
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[[Category: Zhuang, Y]]
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</StructureSection>
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[[Category: Roth, B.L]]
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[[Category: Bos taurus]]
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[[Category: Yuan, Q]]
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[[Category: Homo sapiens]]
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[[Category: Schmitz, G.P]]
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[[Category: Large Structures]]
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[[Category: Phyllomedusa]]
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[[Category: Rattus norvegicus]]
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[[Category: DiBerto JF]]
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[[Category: Jain MK]]
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[[Category: Jiang Y]]
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[[Category: Liu W]]
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[[Category: Melcher K]]
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[[Category: Roth BL]]
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[[Category: Schmitz GP]]
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[[Category: Wang Y]]
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[[Category: Xu HE]]
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[[Category: Yuan Q]]
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[[Category: Zhou XE]]
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[[Category: Zhuang Y]]

Current revision

Gi bound delta-opioid receptor in complex with deltorphin

PDB ID 8f7s

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