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| | ==Human cannabinoid receptor-2 helix 6== | | ==Human cannabinoid receptor-2 helix 6== |
| - | <StructureSection load='2ki9' size='340' side='right'caption='[[2ki9]], [[NMR_Ensembles_of_Models | 15 NMR models]]' scene=''> | + | <StructureSection load='2ki9' size='340' side='right'caption='[[2ki9]]' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[2ki9]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2KI9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2KI9 FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[2ki9]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2KI9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2KI9 FirstGlance]. <br> |
| - | </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=2ki9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ki9 OCA], [https://pdbe.org/2ki9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2ki9 RCSB], [https://www.ebi.ac.uk/pdbsum/2ki9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2ki9 ProSAT]</span></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</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=2ki9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ki9 OCA], [https://pdbe.org/2ki9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2ki9 RCSB], [https://www.ebi.ac.uk/pdbsum/2ki9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2ki9 ProSAT]</span></td></tr> |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[https://www.uniprot.org/uniprot/CNR2_HUMAN CNR2_HUMAN]] Heterotrimeric G protein-coupled receptor for endocannabinoid 2-arachidonoylglycerol mediating inhibition of adenylate cyclase. May function in inflammatory response, nociceptive transmission and bone homeostasis.<ref>PMID:10051546</ref> <ref>PMID:12663043</ref> <ref>PMID:12711605</ref> <ref>PMID:18692962</ref>
| + | [https://www.uniprot.org/uniprot/CNR2_HUMAN CNR2_HUMAN] Heterotrimeric G protein-coupled receptor for endocannabinoid 2-arachidonoylglycerol mediating inhibition of adenylate cyclase. May function in inflammatory response, nociceptive transmission and bone homeostasis.<ref>PMID:10051546</ref> <ref>PMID:12663043</ref> <ref>PMID:12711605</ref> <ref>PMID:18692962</ref> |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| | + | [[Category: Homo sapiens]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Deshmukh, L]] | + | [[Category: Deshmukh L]] |
| - | [[Category: Janero, D R]] | + | [[Category: Janero DR]] |
| - | [[Category: Makriyannis, A]] | + | [[Category: Makriyannis A]] |
| - | [[Category: Tiburu, E K]] | + | [[Category: Tiburu EK]] |
| - | [[Category: Tyukhtenko, S]] | + | [[Category: Tyukhtenko S]] |
| - | [[Category: Vinogradova, O]] | + | [[Category: Vinogradova O]] |
| - | [[Category: G-protein coupled receptor]]
| + | |
| - | [[Category: Gpcr]]
| + | |
| - | [[Category: Human cannabinoid receptor-2]]
| + | |
| - | [[Category: Membrane protein]]
| + | |
| Structural highlights
Function
CNR2_HUMAN Heterotrimeric G protein-coupled receptor for endocannabinoid 2-arachidonoylglycerol mediating inhibition of adenylate cyclase. May function in inflammatory response, nociceptive transmission and bone homeostasis.[1] [2] [3] [4]
Publication Abstract from PubMed
We detail the structure and dynamics of a synthetic peptide corresponding to transmembrane helix 6 (TMH6) of human cannabinoid receptor-2 (hCB2) in biomembrane-mimetic environments. The peptide's NMR structural biology is characterized by two alpha-helical domains bridged by a flexible, nonhelical hinge region containing a highly-conserved CWFP motif with an environmentally sensitive, Pro-based conformational switch. Buried within the peptide's flexible region, W(258) may hydrogen-bond with L(255) to help stabilize the Pro-kinked hCB2 TMH6 structure and position C(257) advantageously for interaction with agonist ligands. These characteristics of hCB2 TMH6 are potential structural features of ligand-induced hCB2 activation in vivo.
Structural biology of human cannabinoid receptor-2 helix 6 in membrane-mimetic environments.,Tiburu EK, Tyukhtenko S, Deshmukh L, Vinogradova O, Janero DR, Makriyannis A Biochem Biophys Res Commun. 2009 Jun 26;384(2):243-8. Epub 2009 May 3. PMID:19397896[5]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Tao Q, McAllister SD, Andreassi J, Nowell KW, Cabral GA, Hurst DP, Bachtel K, Ekman MC, Reggio PH, Abood ME. Role of a conserved lysine residue in the peripheral cannabinoid receptor (CB2): evidence for subtype specificity. Mol Pharmacol. 1999 Mar;55(3):605-13. PMID:10051546
- ↑ Feng W, Song ZH. Effects of D3.49A, R3.50A, and A6.34E mutations on ligand binding and activation of the cannabinoid-2 (CB2) receptor. Biochem Pharmacol. 2003 Apr 1;65(7):1077-85. PMID:12663043
- ↑ Kishimoto S, Gokoh M, Oka S, Muramatsu M, Kajiwara T, Waku K, Sugiura T. 2-arachidonoylglycerol induces the migration of HL-60 cells differentiated into macrophage-like cells and human peripheral blood monocytes through the cannabinoid CB2 receptor-dependent mechanism. J Biol Chem. 2003 Jul 4;278(27):24469-75. Epub 2003 Apr 23. PMID:12711605 doi:http://dx.doi.org/10.1074/jbc.M301359200
- ↑ Anand U, Otto WR, Sanchez-Herrera D, Facer P, Yiangou Y, Korchev Y, Birch R, Benham C, Bountra C, Chessell IP, Anand P. Cannabinoid receptor CB2 localisation and agonist-mediated inhibition of capsaicin responses in human sensory neurons. Pain. 2008 Sep 15;138(3):667-80. doi: 10.1016/j.pain.2008.06.007. Epub 2008 Aug, 9. PMID:18692962 doi:http://dx.doi.org/10.1016/j.pain.2008.06.007
- ↑ Tiburu EK, Tyukhtenko S, Deshmukh L, Vinogradova O, Janero DR, Makriyannis A. Structural biology of human cannabinoid receptor-2 helix 6 in membrane-mimetic environments. Biochem Biophys Res Commun. 2009 Jun 26;384(2):243-8. Epub 2009 May 3. PMID:19397896 doi:10.1016/j.bbrc.2009.04.099
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