4or2: Difference between revisions
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==Human class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulator== | ==Human class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulator== | ||
<StructureSection load='4or2' size='340' side='right' caption='[[4or2]], [[Resolution|resolution]] 2.80Å' scene=''> | <StructureSection load='4or2' size='340' side='right' caption='[[4or2]], [[Resolution|resolution]] 2.80Å' scene=''> | ||
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=FM9:4-FLUORO-N-METHYL-N-{4-[6-(PROPAN-2-YLAMINO)PYRIMIDIN-4-YL]-1,3-THIAZOL-2-YL}BENZAMIDE'>FM9</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=PO4:PHOSPHATE+ION'>PO4</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=FM9:4-FLUORO-N-METHYL-N-{4-[6-(PROPAN-2-YLAMINO)PYRIMIDIN-4-YL]-1,3-THIAZOL-2-YL}BENZAMIDE'>FM9</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=PO4:PHOSPHATE+ION'>PO4</scene></td></tr> | ||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">cybC, GRM1_HUMAN, GPRC1A, GRM1, MGLUR1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</td></tr> | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">cybC, GRM1_HUMAN, GPRC1A, GRM1, MGLUR1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</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=4or2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4or2 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4or2 RCSB], [http://www.ebi.ac.uk/pdbsum/4or2 PDBsum]</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=4or2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4or2 OCA], [http://pdbe.org/4or2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4or2 RCSB], [http://www.ebi.ac.uk/pdbsum/4or2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4or2 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 4or2" style="background-color:#fffaf0;"></div> | |||
==See Also== | ==See Also== | ||
Revision as of 20:06, 2 January 2017
Human class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulatorHuman class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulator
Structural highlights
Function[C562_ECOLX] Electron-transport protein of unknown function. Publication Abstract from PubMedThe excitatory neurotransmitter glutamate induces modulatory actions via the metabotropic glutamate receptors (mGlus), which are class C G protein-coupled receptors (GPCRs). We determined the structure of the human mGlu1 receptor seven-transmembrane (7TM) domain bound to a negative allosteric modulator, FITM, at a resolution of 2.8 angstroms. The modulator binding site partially overlaps with the orthosteric binding sites of class A GPCRs but is more restricted than most other GPCRs. We observed a parallel 7TM dimer mediated by cholesterols, which suggests that signaling initiated by glutamate's interaction with the extracellular domain might be mediated via 7TM interactions within the full-length receptor dimer. A combination of crystallography, structure-activity relationships, mutagenesis, and full-length dimer modeling provides insights about the allosteric modulation and activation mechanism of class C GPCRs. Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator.,Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y, Niswender CM, Katritch V, Meiler J, Cherezov V, Conn PJ, Stevens RC Science. 2014 Apr 4;344(6179):58-64. doi: 10.1126/science.1249489. Epub 2014 Mar , 6. PMID:24603153[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Bacillus coli migula 1895
- Cherezov, V
- Cho, H P
- Conn, P J
- GPCR, GPCR Network
- Gregory, K J
- Han, G W
- Katritch, V
- Niswender, C M
- Stevens, R C
- Wang, C
- Wu, H
- Xia, Y
- Allosteric modulator
- Gpcr
- Gpcr network
- Human metabotropic glutamate receptor 1
- Membrane
- Membrane protein
- Novel protein engineering
- Psi-biology
- Signaling protein
- Structural genomic