Metabotropic glutamate receptor 4 is a protein that in humans is encoded by the GRM4 gene. [5] [6] [7]Together with GRM6, GRM7 and GRM8 it belongs to group III of the metabotropic glutamate receptor family. Group III receptors are linked to the inhibition of the cyclic AMP cascade. [7] Activation of GRM4 has potential therapeutic benefits in the treatment of parkinson's disease.

The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect metabotropic process. They are members of the group C family of G-protein-coupled receptors, or GPCRs. [1] . Like all glutamate receptors, mGluRs bind with glutamate, an amino acid that functions as an excitatory neurotransmitter.

mGluR8 is expressed at lower levels than mGluR4 and mGluR7 but is widely distributed in the brain. As for mGluR4, mGluR8 has been localized predominantly presynaptically but has been identified in some postsynaptic locations and in the periphery (reviewed in 128).

2020年4月16日 · G protein–coupled receptors (GPCRs) play a fundamental role in the modulation of synaptic transmission. A pivotal example is provided by the metabotropic glutamate receptor type 4 (mGluR4), which inhibits glutamate release at presynaptic active zones (AZs).

The metabotropic glutamate receptor 4 (mGluR4) is a Gαi-coupled receptor that modulates glutamatergic neurotransmission. As mGluR4 expression and activation have been implicated in a number of pathological conditions and because the internalization ...

In this article, we briefly review Parkinson's disease and then recent work in the mGluR area, with a focus on the efforts being made toward finding and optimizing novel mGluR4 positive allosteric modulators (PAMs).

2021年6月16日 · Here we report two cryo-electron microscopy structures of human mGlu2 and mGlu4 bound to heterotrimeric G i protein. The structures reveal a G-protein-binding site formed by three intracellular...

2023年12月1日 · Group III mGluRs activation modulates glutamate release in neurodegeneration. Many ligands have been synthesized with various potency and efficacy. Ligands are either specific or non-specific to a group III mGluR subtype. Group III mGluR ligands have been extensively studied for Parkinson’s disease.

2012年6月6日 · Schematic structure of mGluR4 and representation of peptides used for affinity chromatography. The receptor hmGluR4 is a G-protein-coupled receptor with a large N-terminal domain, seven transmembrane domains, and several cytoplasmic areas: three intracellular loops and a short C-terminal tail.

Here, we report that mGluR4 and mGluR8 are the primary group III mGluRs mediating the L-AP4-induced reduction of synaptic transmission at the LOT-PC synapse. Using novel ligands, we have established a role for both mGluR4 and mGluR8 to reduce synaptic transmission.