From Proteopedia

spinqualitylabelsall models mGlu5 Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image metabotropic Glutamate Receptor 5 Homo sapiens Introduction G-coupled protein receptors GPCR are trans-membrane proteins that are integral to cell signaling. The human genome encodes for approximately 750 GPCRS, 350 of which are known to respond to extracellular ligands.[1]. GPCRs are divided into four major classes based on sequence similarity and transduction mechanism; Class A,B,C, and F.[2]. Metabotropic Glutamate Receptor 5 (mGlu5) is a class C GPCR that is involved in the Gq pathway [3]. mGlu5is highly expressed in neuronal and glial cells in the central nervous system, where glutamate serves as the major neurotransmitter. When glutamate binds to the extracellular domain of mGlu5, consisting of the Venus Fly Trap [4], a conformational change through the tram-membrane domains activates the coupled G-protein. This G-protein disassociates and the alpha subunit activates Phospholipase C which has the final outcome of increased neuronal activity[2]. spinqualitylabelsall models Caption for this structure Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image Contents 1 Introduction 1.1 Biological Background 1.2 Importance 2 Function 3 Structure 3.1 Domain highlights 4 Disease 5 Relevance 6 Structural highlights Introduction Biological Background G protein-coupled receptors (GPCRs) can be broken up into four classes: A, B, C, and F. [5]. Metabotropic glutamate receptor 5 (mGLu5) is a Class C GPCR that couples with the Gq pathway [6]. Importance Function Structure Hydrophobic Pocket Surrounding Mavoglurant Image:Mav HB 1.1.png Hydrogen Bonding interactions between protein and Mavoglurant Further Hydrogen Bonding between protein and Mavoglurant Domain highlights Disease Relevance Structural highlights

References

1. ↑ Vassilatis DK, Hohmann JG, Zeng H, Li F, Ranchalis JE, Mortrud MT, Brown A, Rodriguez SS, Weller JR, Wright AC, Bergmann JE, Gaitanaris GA. The G protein-coupled receptor repertoires of human and mouse. Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4903-8. Epub 2003 Apr 4. PMID:12679517 doi:http://dx.doi.org/10.1073/pnas.0230374100
2. ↑ ^{2.0 2.1} Venkatakrishnan AJ, Deupi X, Lebon G, Tate CG, Schertler GF, Babu MM. Molecular signatures of G-protein-coupled receptors. Nature. 2013 Feb 14;494(7436):185-94. doi: 10.1038/nature11896. PMID:23407534 doi:http://dx.doi.org/10.1038/nature11896
3. ↑ Pin JP, Galvez T, Prezeau L. Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors. Pharmacol Ther. 2003 Jun;98(3):325-54. PMID:12782243
4. ↑ Dore AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH. Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain. Nature. 2014 Jul 31;511(7511):557-62. doi: 10.1038/nature13396. Epub 2014 Jul 6. PMID:25042998 doi:http://dx.doi.org/10.1038/nature13396
5. ↑ Venkatakrishnan AJ, Deupi X, Lebon G, Tate CG, Schertler GF, Babu MM. Molecular signatures of G-protein-coupled receptors. Nature. 2013 Feb 14;494(7436):185-94. doi: 10.1038/nature11896. PMID:23407534 doi:http://dx.doi.org/10.1038/nature11896
6. ↑ Pin JP, Galvez T, Prezeau L. Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors. Pharmacol Ther. 2003 Jun;98(3):325-54. PMID:12782243