Target type: molecularfunction
Binding to a type 2 metabotropic glutamate receptor. [GOC:mah, GOC:nln]
Type 2 metabotropic glutamate receptors (mGluR2) are members of the G protein-coupled receptor (GPCR) superfamily, specifically the class C GPCRs. They are responsible for mediating the effects of glutamate, the primary excitatory neurotransmitter in the central nervous system. Binding of glutamate to mGluR2 initiates a signaling cascade that ultimately leads to a decrease in neuronal activity.
mGluR2 is a dimeric receptor, meaning it is composed of two identical subunits. The binding of glutamate to the extracellular domain of the receptor causes a conformational change in the transmembrane domain, leading to the activation of the intracellular G protein. Specifically, mGluR2 is coupled to the Gi/o protein, which inhibits adenylyl cyclase, the enzyme that produces cyclic adenosine monophosphate (cAMP). Reduced cAMP levels then lead to a decrease in the activity of protein kinase A (PKA), a key enzyme involved in neuronal signaling.
The activation of mGluR2 also leads to the activation of other intracellular signaling pathways, including the phosphoinositide pathway and the mitogen-activated protein kinase (MAPK) pathway. These pathways contribute to the overall inhibitory effect of mGluR2 on neuronal activity.
Overall, the molecular function of mGluR2 binding can be summarized as follows:
1. **Glutamate binding:** Glutamate binds to the extracellular domain of the mGluR2 receptor.
2. **Conformational change:** Glutamate binding triggers a conformational change in the transmembrane domain of the receptor.
3. **G protein activation:** The conformational change activates the Gi/o protein.
4. **Inhibition of adenylyl cyclase:** Activated Gi/o protein inhibits adenylyl cyclase, reducing cAMP levels.
5. **Decrease in PKA activity:** Reduced cAMP levels lead to a decrease in PKA activity.
6. **Activation of other signaling pathways:** mGluR2 also activates other intracellular pathways, including the phosphoinositide pathway and the MAPK pathway.
7. **Inhibition of neuronal activity:** All these signaling events ultimately lead to a decrease in neuronal activity.'
"
Protein | Definition | Taxonomy |
---|---|---|
Na(+)/H(+) exchange regulatory cofactor NHE-RF1 | A Na(+)/H(+) exchange regulatory cofactor NHE-RF1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:O14745] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
---|---|---|---|
fh535 | FH535: inhibits Wnt signaling | sulfonamide |