Target intelligence / Profile preview

Glutamate receptor, metabotropic 1 (mGluR1)

Target
mGluR1
Molecular classification
G protein-coupled receptor, Receptor, Glutamate receptor, Protein phosphatase 1 regulatory subunit
01

Overview

Glutamate receptor, metabotropic 1 (mGluR1, encoded by the GRM1 gene), is a member of the group I metabotropic glutamate receptors, belonging to the class C G protein-coupled receptor family[1][5]. mGluR1 is predominantly expressed in the central nervous system, especially in neurons, where it mediates excitatory neurotransmission by activating phospholipase C through Gq/G11 proteins, resulting in calcium signaling and activation of downstream effectors such as protein kinase C[1][5]. It plays essential roles in synaptic plasticity, neuronal excitability, and brain development. Aberrant expression of GRM1 has been linked to neuropsychiatric disorders (such as schizophrenia and depression), neurodegenerative diseases, and several cancer types, including melanoma and triple negative breast cancer, where it can act as an oncogene[2][3][4]. mGluR1 is a validated drug target for various CNS disorders and is under investigation for anti-cancer therapy with antagonist compounds[3].

Other names
Metabotropic glutamate receptor 1GRM1GPRC1AMGLUR1mGluR1mGlu1MGLU1PPP1R85SCA44SCAR13glutamate metabotropic receptor 1protein phosphatase 1 regulatory subunit 85
02

Mechanism of action

mGluR1 antagonists block the activation of the phosphatidylinositol-calcium second messenger system and downstream signaling pathways Allosteric modulation alters glutamate binding and receptor activity

03

Biological functions

Signal transductionSynaptic transmissionRegulation of neuronal excitabilityModulation of synaptic plasticity
04

Disease associations

Cancer (including melanoma and breast cancer)Neuropsychiatric disorders (e.g., schizophrenia, bipolar disorder, depression)Neurodegenerative disease
05

Safety considerations

Central nervous system side effects (since GRM1/mGluR1 is widely expressed in the brain)Risk of neuropsychiatric symptoms or reduced cognitive function with systemic antagonismPotential on-target effects impacting normal synaptic signaling and plasticity
06

Interacting drugs

Riluzole (modulates glutamatergic neurotransmission)

4 more in the full profile.

07

Biomarkers

Expression of GRM1 in tumor tissue (melanoma, breast cancer)Levels of GRM1/mGluR1 mRNA or protein as a marker for disease progression or prognosis

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