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Metabotropic glutamate receptor 1

Function of Metabotropic Glutamate Receptor 1: – L-glutamate is the major excitatory neurotransmitter in the central nervous system. – Glutamatergic neurotransmission is involved in most […]

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Function of Metabotropic Glutamate Receptor 1:
– L-glutamate is the major excitatory neurotransmitter in the central nervous system.
– Glutamatergic neurotransmission is involved in most aspects of normal brain function.
– Metabotropic glutamate receptors are a family of G protein-coupled receptors divided into 3 groups.
– Group I receptors activate phospholipase C.
– Group II and III receptors inhibit the cyclic AMP cascade.

Effects of Knockout of Metabotropic Glutamate Receptor 1:
– Mice lacking functional glutamate receptor 1 had impaired cerebellar long-term depression.
– Impaired motor functions, balance, and learning abilities were observed in knockout mice.
– No basic anatomical changes in the brain were noted.
– Impaired hippocampal long-term potentiation was observed.

Clinical Significance:
– Mutations in the GRM1 gene may contribute to melanoma susceptibility.
– Antibodies against mGluR1 receptors can cause cerebellar ataxia.
– Antibodies against mGluR1 receptors impair long-term depression in the cerebellum.

Ligands and Binding Sites:
– At least two distinct allosteric binding sites exist on the mGluR1.
– Several potent and specific allosteric ligands, mainly antagonists/inhibitors, have been developed.
– No orthosteric subtype-selective ligands for mGluR1 have been discovered yet.
– Allosteric ligands interact with mGluR1 at sites distinct from negative allosteric modulators.

Protein Function and Signaling Pathways:
– Homer regulates association of mGluRs with synaptic proteins.
– Protein kinase C and protein kinase A influence mGluR signaling.
– Desensitization of inositol trisphosphate/Ca2+ pathway by phosphorylation.
– Metabotropic glutamate receptor signaling modulation by phosphorylation.
– Dimerization of mGluRs using N-terminal truncation of mGluR1alpha.

Metabotropic glutamate receptor 1 (Wikipedia)

The glutamate receptor, metabotropic 1, also known as GRM1, is a human gene which encodes the metabotropic glutamate receptor 1 (mGluR1) protein.

GRM1
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesGRM1, GPRC1A, MGLU1, MGLUR1, PPP1R85, SCAR13, glutamate metabotropic receptor 1, SCA44
External IDsOMIM: 604473 MGI: 1351338 HomoloGene: 649 GeneCards: GRM1
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001114333
NM_016976

RefSeq (protein)

NP_001264993
NP_001264994
NP_001264995
NP_001264996

NP_001107805
NP_058672

Location (UCSC)Chr 6: 146.03 – 146.44 MbChr 10: 10.56 – 10.96 Mb
PubMed search
Wikidata
View/Edit HumanView/Edit Mouse
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