Sandbox Reserved 1160: Difference between revisions
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=== Binding Pocket === | === Binding Pocket === | ||
[[Image: Organic with clipped surface.png|200 px|left|thumb|Cross section view of mavoglurant in the binding pocket]] | [[Image: Organic with clipped surface.png|200 px|left|thumb|Cross section view of mavoglurant in the binding pocket]] | ||
The binding pocket represents an interesting source of regulatory control of receptor activity. The binding pocket is only accessible by a relatively narrow (7 angstrom) <scene name='72/721531/Protien_sur/4'>entrance</scene><ref name="Dore" />. This small entrance severely restricts the access of both positive and negative allosteric regulators. | The binding pocket represents an interesting source of regulatory control of receptor activity. The binding pocket is only accessible by a relatively narrow (7 angstrom) <scene name='72/721531/Protien_sur/4'>entrance</scene><ref name="Dore" />. This small entrance severely restricts the access of both positive and negative allosteric regulators. | ||
Important Amino Acids<ref name="Dore" />: | Important Amino Acids<ref name="Dore" />: | ||
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== Function and Pathway == | == Function and Pathway == | ||
It all begins with glutamate binding to the venus fly trap domain. The signal transduction goes across the cystine-rich domain to the TMD. Next the dimerization of the TMD occurs. This activates the Gq/11 pathway, which activates phspholipase Cβ. The active phospholipase Cβ performs hydrolysis on phosphotinositides and generates inositol 1,4,5-trisphosphate and diacyl-glycerol. This results in calcium mobilization and activation of protein kinase C<ref name="Niswender" />. | It all begins with glutamate binding to the venus fly trap domain. The signal transduction goes across the cystine-rich domain to the TMD. Next the dimerization of the TMD occurs. This activates the Gq/11 pathway, which activates phspholipase Cβ<ref name="Niswender" />. The active phospholipase Cβ performs hydrolysis on phosphotinositides and generates inositol 1,4,5-trisphosphate and diacyl-glycerol<ref name="Woodcock" />. This results in calcium mobilization and activation of protein kinase C<ref name="Niswender" />. | ||
== Disease == | == Disease == | ||
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<ref name="Niswender">PMID: 20055706</ref> | <ref name="Niswender">PMID: 20055706</ref> | ||
<ref name="Feng">PMID: 25762450</ref> | <ref name="Feng">PMID: 25762450</ref> | ||
<ref name="Bailey">PMID: 26855682</ref> | <ref name="Bailey">PMID: 26855682</ref> | ||
<ref name="Woodcock">PMID: 18940816</ref> | |||
<references/> | <references/> | ||
== External Resources == | == External Resources == | ||
[http://www.fraxa.org/novartis-discontinues-development-mavoglurant-afq056-fragile-x-syndrome/ Novartis Fragile X trials] | [http://www.fraxa.org/novartis-discontinues-development-mavoglurant-afq056-fragile-x-syndrome/ Novartis Fragile X trials] | ||
