Sandbox Reserved 1160: Difference between revisions
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== Human metabotropic glutamate receptor 5 transmembrane domain == | == Human metabotropic glutamate receptor 5 transmembrane domain == | ||
<StructureSection load='4oo9' size='300' frame='true' side='right' caption='Human metabotropic glutamate receptor 5 transmembrane domain' scene='72/721531/Protien_clean_sce/1'> | <StructureSection load='4oo9' size='300' frame='true' side='right' caption='Human metabotropic glutamate receptor 5 transmembrane domain' scene='72/721531/Protien_clean_sce/1'> | ||
Receiving and responding to extracellular messages is critical to the proper function of the nervous system. Glutamate is the major excitory neurotransmitter of the CNS, and metabotropic glutamate receptor 5 will play a major role in glutamate signaling. Metabotropic glutamate receptor 5 transmembrane domain is a homodimeric GPCR that resides in the cellular membrane <ref name="Dore" />. This domain is a member of the Class C GPCR family and can further be categorized into the Group I subgroup. The transmembrane domain will signal through a Gq/11 pathway. mGlu5 will bind glutamate to the extracellular Venus flytrap domain and the signal will be transduced across the membrane to a heterotrimeric G protein, which will ultimately lead to calcium release and activation of PKC. This will elicit a excitory post-synaptic repose and modulate long term potentiation. Human metabotropic glutamate receptor 5 is found throughout the central nervous system. Areas containing high concentrations of this protein are often involved involved in emotions and higher cognition<ref name=" | Receiving and responding to extracellular messages is critical to the proper function of the nervous system. Glutamate is the major excitory neurotransmitter of the CNS, and metabotropic glutamate receptor 5 will play a major role in glutamate signaling. Metabotropic glutamate receptor 5 transmembrane domain is a homodimeric GPCR that resides in the cellular membrane <ref name="Dore" />. This domain is a member of the Class C GPCR family and can further be categorized into the Group I subgroup. The transmembrane domain will signal through a Gq/11 pathway. mGlu5 will bind glutamate to the extracellular Venus flytrap domain and the signal will be transduced across the membrane to a heterotrimeric G protein, which will ultimately lead to calcium release and activation of PKC. This will elicit a excitory post-synaptic repose and modulate long term potentiation. Human metabotropic glutamate receptor 5 is found throughout the central nervous system. Areas containing high concentrations of this protein are often involved involved in emotions and higher cognition<ref name="Niswender" />. The localization of mGlu5 in the CNS and the presence of multiple domains makes mGlu5 a possible target for treating schizophrenia, Fragile X, depression, anxiety,and Alzheimer's disease<ref name="Wu" />. | ||
== Discovery == | == Discovery == | ||
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=== Fragile X === | === Fragile X === | ||
One positive characteristic of ligands that target the TMD is they tend to be more specific, thus interacting less with brain proteins<ref name="Feng" />. | |||
However, modulators of mGlu5 TMD continue to be studied in treating Parkinson's, Alzheimer's disease, and various addictions<ref name="Niswender" />. | |||
=== Parkinsons === | === Parkinsons === | ||
== Relevance == | == Relevance == | ||
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<ref name="Dore">PMID: 25042998</ref> | <ref name="Dore">PMID: 25042998</ref> | ||
<ref name="Wu">PMID: 24603153</ref> | <ref name="Wu">PMID: 24603153</ref> | ||
<ref name="Niswender">PMID: 20055706</ref> | |||
<ref name="Feng">PMID: 4406965</ref> | |||
<ref name="Dore">PMID: 25042998</ref> | |||
<references/> | <references/> | ||
== External Resources == | == External Resources == | ||
