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