Sandbox Reserved 1162: Difference between revisions
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= metabotropic Glutamate Receptor 5 = | = metabotropic Glutamate Receptor 5 = | ||
== Introduction == | == Introduction == | ||
G-coupled protein receptors [https://en.wikipedia.org/wiki/G_protein–coupled_receptor (GPCR's)] are helical trans-membrane proteins that bind to an extracellular signal and activate a cellular response. The human genome encodes for approximately 750 GPCR's, 350 of which are known to respond to extracellular ligands.<ref name="GPCRRep">PMID: 12679517 </ref> GPCR's are divided into four major classes based on sequence similarity and transduction mechanism: | G-coupled protein receptors [https://en.wikipedia.org/wiki/G_protein–coupled_receptor (GPCR's)] are helical trans-membrane proteins that bind to an extracellular signal and activate a cellular response. The human genome encodes for approximately 750 GPCR's, 350 of which are known to respond to extracellular ligands.<ref name="GPCRRep">PMID: 12679517 </ref> GPCR's are divided into four major classes based on sequence similarity and transduction mechanism: Classes A, B, C, and F.<ref name="MSGPCR">PMID:23407534</ref> Metabotropic Glutamate Receptor 5 (<scene name='72/726409/Overview/6'>mGlu<sub>5</sub></scene>) is a class C GPCR that is involved in the G<sub>q</sub> pathway.<ref name="CCGPCR">PMID:12782243</ref> In this pathway, glutamate binds to the extracellular domain of mGlu<sub>5</sub>, and the trans-membrane domain then undergoes a conformational change that activates the coupled [http://proteopedia.org/wiki/index.php/GTP-binding_protein G-protein] on the intracellular side of the membrane.<ref name="Primary">PMID: 25042998 </ref> The activated G-protein disassociates, and the alpha subunit activates [https://en.wikipedia.org/wiki/Phospholipase_C Phospholipase C]. Phospholipase C in turn cleaves [https://en.wikipedia.org/wiki/Phosphatidylinositol_4,5-bisphosphate PIP2] to [https://en.wikipedia.org/wiki/Diglyceride DAG] and [https://en.wikipedia.org/wiki/Inositol_trisphosphate IP<sub>3</sub>]. IP<sub>3</sub> then binds to calcium channels on the [https://en.wikipedia.org/wiki/Endoplasmic_reticulum Endoplasmic reticulum], creating an increased cellular concentration of calcium. Increased calcium concentrations thus lead to increased neuronal activity.<ref name="MSGPCR">PMID:23407534</ref> Due to its involvement in neuronal activity, mGlu<sub>5</sub> is highly expressed in neuronal and glial cells in the central nervous system, where glutamate serves as the major neurotransmitter. | ||
== Structure == | == Structure == | ||