4dkl
From Proteopedia
(Difference between revisions)
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| - | + | ==Crystal structure of the mu-opioid receptor bound to a morphinan antagonist== | |
| - | + | <StructureSection load='4dkl' size='340' side='right' caption='[[4dkl]], [[Resolution|resolution]] 2.80Å' scene=''> | |
| - | { | + | == Structural highlights == |
| + | <table><tr><td colspan='2'>[[4dkl]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Enterobacteria_phage_t4 Enterobacteria phage t4]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4DKL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4DKL FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=BF0:METHYL+4-{[(5BETA,6ALPHA)-17-(CYCLOPROPYLMETHYL)-3,14-DIHYDROXY-4,5-EPOXYMORPHINAN-6-YL]AMINO}-4-OXOBUTANOATE'>BF0</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=MPG:1-MONOOLEOYL-RAC-GLYCEROL'>MPG</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Mor, Oprm, Oprm1, E ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10665 Enterobacteria phage T4])</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </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=4dkl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4dkl OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4dkl RCSB], [http://www.ebi.ac.uk/pdbsum/4dkl PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Opium is one of the world's oldest drugs, and its derivatives morphine and codeine are among the most used clinical drugs to relieve severe pain. These prototypical opioids produce analgesia as well as many undesirable side effects (sedation, apnoea and dependence) by binding to and activating the G-protein-coupled micro-opioid receptor (micro-OR) in the central nervous system. Here we describe the 2.8 A crystal structure of the mouse micro-OR in complex with an irreversible morphinan antagonist. Compared to the buried binding pocket observed in most G-protein-coupled receptors published so far, the morphinan ligand binds deeply within a large solvent-exposed pocket. Of particular interest, the micro-OR crystallizes as a two-fold symmetrical dimer through a four-helix bundle motif formed by transmembrane segments 5 and 6. These high-resolution insights into opioid receptor structure will enable the application of structure-based approaches to develop better drugs for the management of pain and addiction. | ||
| - | + | Crystal structure of the micro-opioid receptor bound to a morphinan antagonist.,Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S Nature. 2012 Mar 21. doi: 10.1038/nature10954. PMID:22437502<ref>PMID:22437502</ref> | |
| - | + | ||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
==See Also== | ==See Also== | ||
*[[G protein-coupled receptor|G protein-coupled receptor]] | *[[G protein-coupled receptor|G protein-coupled receptor]] | ||
| + | *[[Lysozyme 3D structures|Lysozyme 3D structures]] | ||
*[[Mu Opioid Receptor Bound to a Morphinan Antagonist|Mu Opioid Receptor Bound to a Morphinan Antagonist]] | *[[Mu Opioid Receptor Bound to a Morphinan Antagonist|Mu Opioid Receptor Bound to a Morphinan Antagonist]] | ||
| - | + | *[[Opioid receptor|Opioid receptor]] | |
| - | == | + | == References == |
| - | < | + | <references/> |
| + | __TOC__ | ||
| + | </StructureSection> | ||
[[Category: Enterobacteria phage t4]] | [[Category: Enterobacteria phage t4]] | ||
[[Category: Lysozyme]] | [[Category: Lysozyme]] | ||
| - | [[Category: Granier, S | + | [[Category: Granier, S]] |
| - | [[Category: Kobilka, B K | + | [[Category: Kobilka, B K]] |
| - | [[Category: Kobilka, T S | + | [[Category: Kobilka, T S]] |
| - | [[Category: Kruse, A C | + | [[Category: Kruse, A C]] |
| - | [[Category: Manglik, A | + | [[Category: Manglik, A]] |
| - | [[Category: Mathiesen, J M | + | [[Category: Mathiesen, J M]] |
| - | [[Category: Pardo, L | + | [[Category: Pardo, L]] |
| - | [[Category: Sunahara, R K | + | [[Category: Sunahara, R K]] |
| - | [[Category: Thian, F S | + | [[Category: Thian, F S]] |
| - | [[Category: Weis, W I | + | [[Category: Weis, W I]] |
| - | [[Category: | + | [[Category: Transmembrane receptor]] |
[[Category: G-protein coupled receptor]] | [[Category: G-protein coupled receptor]] | ||
[[Category: Signaling protein-antagonist complex]] | [[Category: Signaling protein-antagonist complex]] | ||
Revision as of 13:04, 5 January 2015
Crystal structure of the mu-opioid receptor bound to a morphinan antagonist
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