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| | ==Human cannabinoid receptor 1 - helix 7/8 peptide== | | ==Human cannabinoid receptor 1 - helix 7/8 peptide== |
| - | <StructureSection load='2koe' size='340' side='right' caption='[[2koe]], [[NMR_Ensembles_of_Models | 18 NMR models]]' scene=''> | + | <StructureSection load='2koe' size='340' side='right'caption='[[2koe]]' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[2koe]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2KOE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2KOE FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[2koe]] 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=2KOE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2KOE FirstGlance]. <br> |
| - | </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=2koe FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2koe OCA], [http://pdbe.org/2koe PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2koe RCSB], [http://www.ebi.ac.uk/pdbsum/2koe PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2koe 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=2koe FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2koe OCA], [https://pdbe.org/2koe PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2koe RCSB], [https://www.ebi.ac.uk/pdbsum/2koe PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2koe ProSAT]</span></td></tr> |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://www.uniprot.org/uniprot/CNR1_HUMAN CNR1_HUMAN]] Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.<ref>PMID:15620723</ref> | + | [https://www.uniprot.org/uniprot/CNR1_HUMAN CNR1_HUMAN] Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.<ref>PMID:15620723</ref> |
| | == Evolutionary Conservation == | | == Evolutionary Conservation == |
| | [[Image:Consurf_key_small.gif|200px|right]] | | [[Image:Consurf_key_small.gif|200px|right]] |
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| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Deshmukh, L]] | + | [[Category: Homo sapiens]] |
| - | [[Category: Janero, D]] | + | [[Category: Large Structures]] |
| - | [[Category: Makriyannis, A]] | + | [[Category: Deshmukh L]] |
| - | [[Category: Tiburu, E]] | + | [[Category: Janero D]] |
| - | [[Category: Tyukhtenko, S]] | + | [[Category: Makriyannis A]] |
| - | [[Category: Vinogradova, O]] | + | [[Category: Tiburu E]] |
| - | [[Category: Gpcr]] | + | [[Category: Tyukhtenko S]] |
| - | [[Category: Hcb1]] | + | [[Category: Vinogradova O]] |
| - | [[Category: Membrane protein]]
| + | |
| - | [[Category: Signaling protein]]
| + | |
| Structural highlights
Function
CNR1_HUMAN Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.[1]
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
We report the NMR solution structure of a synthetic 40-mer (T(377)-E(416)) that encompasses human cannabinoid receptor-1 (hCB1) transmembrane helix 7 (TMH7) and helix 8 (H8) [hCB1(TMH7/H8)] in 30% trifluoroethanol/H(2)O. Structural features include, from the peptide's amino terminus, a hydrophobic alpha-helix (TMH7); a loop-like, 11 residue segment featuring a pronounced Pro-kink within the conserved NPxxY motif; a short amphipathic alpha-helix (H8) orthogonal to TMH7 with cationic and hydrophobic amino-acid clusters; and an unstructured C-terminal end. The hCB1(TMH7/H8) NMR solution structure suggests multiple electrostatic amino-acid interactions, including an intrahelical H8 salt bridge and a hydrogen-bond network involving the peptide's loop-like region. Potential cation-pi and cation-phenolic OH interactions between Y(397) in the TMH7 NPxxY motif and R(405) in H8 are identified as candidate structural forces promoting interhelical microdomain formation. This microdomain may function as a flexible molecular hinge during ligand-induced hCB1 conformer transitions.
NMR solution structure of human cannabinoid receptor-1 helix 7/8 peptide: candidate electrostatic interactions and microdomain formation.,Tyukhtenko S, Tiburu EK, Deshmukh L, Vinogradova O, Janero DR, Makriyannis A Biochem Biophys Res Commun. 2009 Dec 18;390(3):441-6. Epub 2009 Sep 18. PMID:19766594[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Ryberg E, Vu HK, Larsson N, Groblewski T, Hjorth S, Elebring T, Sjogren S, Greasley PJ. Identification and characterisation of a novel splice variant of the human CB1 receptor. FEBS Lett. 2005 Jan 3;579(1):259-64. PMID:15620723 doi:http://dx.doi.org/10.1016/j.febslet.2004.11.085
- ↑ Tyukhtenko S, Tiburu EK, Deshmukh L, Vinogradova O, Janero DR, Makriyannis A. NMR solution structure of human cannabinoid receptor-1 helix 7/8 peptide: candidate electrostatic interactions and microdomain formation. Biochem Biophys Res Commun. 2009 Dec 18;390(3):441-6. Epub 2009 Sep 18. PMID:19766594 doi:10.1016/j.bbrc.2009.09.053
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