Gene Symbol: GRM1
Description: glutamate metabotropic receptor 1
Alias: GPRC1A, MGLU1, MGLUR1, PPP1R85, SCA44, SCAR13, metabotropic glutamate receptor 1, glutamate receptor, metabotropic 1, protein phosphatase 1, regulatory subunit 85
Species: human
Products:     GRM1

Top Publications

  1. Ayoub M, Angelicheva D, Vile D, Chandler D, Morar B, Cavanaugh J, et al. Deleterious GRM1 mutations in schizophrenia. PLoS ONE. 2012;7:e32849 pubmed publisher
    ..GRM1 encodes the metabotropic glutamate receptor 1 (mGluR1), whose documented role as a modulator of neuronal signalling and synaptic plasticity makes ..
  2. Wangari Talbot J, Wall B, Goydos J, Chen S. Functional effects of GRM1 suppression in human melanoma cells. Mol Cancer Res. 2012;10:1440-50 pubmed publisher
    Ectopic expression of a neuronal receptor, metabotropic glutamate receptor 1 (Grm1), in melanocytes has been implicated in melanoma development in mouse models...
  3. Pacheco R, Ciruela F, Casado V, Mallol J, Gallart T, Lluis C, et al. Group I metabotropic glutamate receptors mediate a dual role of glutamate in T cell activation. J Biol Chem. 2004;279:33352-8 pubmed
    ..This is a novel non-inhibitory action mechanism for glutamate in lymphocyte activation. mGlu1R and mGlu5R thus mediate opposite glutamate effects in human lymphocytes. ..
  4. Frank R, McRae A, Pocklington A, van de Lagemaat L, Navarro P, Croning M, et al. Clustered coding variants in the glutamate receptor complexes of individuals with schizophrenia and bipolar disorder. PLoS ONE. 2011;6:e19011 pubmed publisher
    ..cluster analysis of nsSNPs identified two exons encoding the cysteine-rich domain and first transmembrane helix of GRM1 as a risk locus with five mutations highly enriched within these domains...
  5. Ortiz P, Vanaclocha F, López Bran E, Esquivias J, López Estebaranz J, Martin Gonzalez M, et al. Genetic analysis of the GRM1 gene in human melanoma susceptibility. Eur J Hum Genet. 2007;15:1176-82 pubmed
    Data obtained from a mouse model indicated that the ectopic expression of the Grm1 gene is sufficient for transforming melanocytes and causing malignant melanoma in vivo...
  6. Wu H, Wang C, Gregory K, Han G, Cho H, Xia Y, et al. Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science. 2014;344:58-64 pubmed publisher
    ..We determined the structure of the human mGlu1 receptor seven-transmembrane (7TM) domain bound to a negative allosteric modulator, FITM, at a resolution of 2...
  7. Mehta M, Dolfi S, Bronfenbrener R, Bilal E, Chen C, Moore D, et al. Metabotropic glutamate receptor 1 expression and its polymorphic variants associate with breast cancer phenotypes. PLoS ONE. 2013;8:e69851 pubmed publisher
    Several epidemiological studies have suggested a link between melanoma and breast cancer. Metabotropic glutamate receptor 1 (GRM1), which is involved in many cellular processes including proliferation and differentiation, has been ..
  8. Crepaldi L, Lackner C, Corti C, Ferraguti F. Transcriptional activators and repressors for the neuron-specific expression of a metabotropic glutamate receptor. J Biol Chem. 2007;282:17877-89 pubmed
    b>Metabotropic glutamate receptor 1 (mGlu1) has a discrete distribution in the central nervous system restricted to neurons...
  9. Pollock P, Cohen Solal K, Sood R, Namkoong J, Martino J, Koganti A, et al. Melanoma mouse model implicates metabotropic glutamate signaling in melanocytic neoplasia. Nat Genet. 2003;34:108-12 pubmed
    ..mapping identified multiple tandem insertions of the transgene into intron 3 of Grm1 (encoding metabotropic glutamate receptor 1) with concomitant deletion of 70 kb of intronic sequence...

More Information


  1. Hermans E, Challiss R. Structural, signalling and regulatory properties of the group I metabotropic glutamate receptors: prototypic family C G-protein-coupled receptors. Biochem J. 2001;359:465-84 pubmed
    ..This review will focus on the group I mGlu receptors (mGlu1 and mGlu5)...
  2. Esseltine J, Ribeiro F, Ferguson S. Rab8 modulates metabotropic glutamate receptor subtype 1 intracellular trafficking and signaling in a protein kinase C-dependent manner. J Neurosci. 2012;32:16933-42a pubmed publisher
    ..Group 1 mGluRs (mGluR1 and mGluR5) are primarily coupled to G?(q/11) leading to the activation of phospholipase C and the formation of ..
  3. Anborgh P, Godin C, Pampillo M, Dhami G, Dale L, Cregan S, et al. Inhibition of metabotropic glutamate receptor signaling by the huntingtin-binding protein optineurin. J Biol Chem. 2005;280:34840-8 pubmed
    ..Taken together, these studies identify a novel mechanism for mGluR desensitization and an additional biochemical link between altered glutamate receptor signaling and Huntington disease. ..
  4. Lee H, Wall B, Wangari Talbot J, Chen S. Regulation of mGluR1 expression in human melanocytes and melanoma cells. Biochim Biophys Acta. 2012;1819:1123-31 pubmed publisher
    We demonstrated that ectopic expression of metabotropic glutamate receptor 1 (mGluR1/Grm1) in mouse melanocytes was sufficient to induce melanoma development in vivo with 100% penetrance...
  5. Guergueltcheva V, Azmanov D, Angelicheva D, Smith K, Chamova T, Florez L, et al. Autosomal-recessive congenital cerebellar ataxia is caused by mutations in metabotropic glutamate receptor 1. Am J Hum Genet. 2012;91:553-64 pubmed publisher
    ..The mutated gene, GRM1, encodes metabotropic glutamate receptor mGluR1, which is highly expressed in cerebellar Purkinje cells and plays an important role in cerebellar development and ..
  6. Namkoong J, Shin S, Lee H, MARIN Y, Wall B, Goydos J, et al. Metabotropic glutamate receptor 1 and glutamate signaling in human melanoma. Cancer Res. 2007;67:2298-305 pubmed
    ..Subsequent studies in these mice identified that the aberrant expression of metabotropic glutamate receptor 1 (GRM1) in melanocytes played a critical role in the onset of melanoma...
  7. Esseltine J, Willard M, Wulur I, Lajiness M, Barber T, Ferguson S. Somatic mutations in GRM1 in cancer alter metabotropic glutamate receptor 1 intracellular localization and signaling. Mol Pharmacol. 2013;83:770-80 pubmed publisher, we investigated the intracellular localization and G protein-dependent and -independent signaling of eight GRM1 (mGluR1a) somatic mutations...
  8. Collard C, Park K, Montalto M, Alapati S, Buras J, Stahl G, et al. Neutrophil-derived glutamate regulates vascular endothelial barrier function. J Biol Chem. 2002;277:14801-11 pubmed
    ..Furthermore, novel expression of metabotropic glutamate receptor 1 (mGluR1), mGluR4, and mGluR5 by human brain and dermal microvascular endothelial cells was ..
  9. Diraddo J, Pshenichkin S, Gelb T, Wroblewski J. Two newly identified exons in human GRM1 express a novel splice variant of metabotropic glutamate 1 receptor. Gene. 2013;519:367-73 pubmed publisher
    ..However, several shorter mGlu1 receptor splice variants lack the sequence required for these interactions, and no major functional differences ..
  10. Speyer C, Smith J, Banda M, Devries J, Mekani T, Gorski D. Metabotropic glutamate receptor-1: a potential therapeutic target for the treatment of breast cancer. Breast Cancer Res Treat. 2012;132:565-73 pubmed publisher
    ..We detected the expression of metabotropic glutamate receptor-1 (gene: GRM1; protein: mGluR1) in triple negative breast cancer cells and evaluated its role in regulating the pro-proliferative phenotype of ..
  11. Ferreira L, Dale L, Ribeiro F, Babwah A, Pampillo M, Ferguson S. Calcineurin inhibitor protein (CAIN) attenuates Group I metabotropic glutamate receptor endocytosis and signaling. J Biol Chem. 2009;284:28986-94 pubmed publisher
    ..We show here that both mGluR1 and mGluR5 interact with the calcineurin inhibitor protein (CAIN)...
  12. Xiao B, Tu J, Petralia R, Yuan J, Doan A, Breder C, et al. Homer regulates the association of group 1 metabotropic glutamate receptors with multivalent complexes of homer-related, synaptic proteins. Neuron. 1998;21:707-16 pubmed
    ..These observations support a model in which the dynamic expression of Homer 1a competes with constitutively expressed CC-Homers to modify synaptic mGluR properties. ..
  13. Francesconi A, Duvoisin R. Role of the second and third intracellular loops of metabotropic glutamate receptors in mediating dual signal transduction activation. J Biol Chem. 1998;273:5615-24 pubmed
    ..Within i3, we uncovered two residues, Arg775 and Phe781, that are crucial for coupling to both pathways, since their substitution leads to receptor inactivation. ..
  14. Shin S, Wall B, Goydos J, Chen S. AKT2 is a downstream target of metabotropic glutamate receptor 1 (Grm1). Pigment Cell Melanoma Res. 2010;23:103-11 pubmed publisher
    ..In cultured stable Grm1-mouse-melanocytic clones, as well as an metabotropic glutamate receptor 1 (Grm1) expressing human melanoma cell line, C8161, stimulation of Grm1 by its agonist led to the ..
  15. Sato T, Shimada Y, Nagasawa N, Nakanishi S, Jingami H. Amino acid mutagenesis of the ligand binding site and the dimer interface of the metabotropic glutamate receptor 1. Identification of crucial residues for setting the activated state. J Biol Chem. 2003;278:4314-21 pubmed
    ..The results demonstrate the crucial role of the dimer interface in receptor activation. ..
  16. Gupta D, McCullumsmith R, Beneyto M, Haroutunian V, Davis K, Meador Woodruff J. Metabotropic glutamate receptor protein expression in the prefrontal cortex and striatum in schizophrenia. Synapse. 2005;57:123-31 pubmed
  17. Martino J, Wall B, Mastrantoni E, Wilimczyk B, La Cava S, Degenhardt K, et al. Metabotropic glutamate receptor 1 (Grm1) is an oncogene in epithelial cells. Oncogene. 2013;32:4366-76 pubmed publisher
    ..and our laboratory previously had demonstrated the etiological role of ectopically expressed metabotropic glutamate receptor 1 (Grm1/mGluR1) in mouse models of melanoma...
  18. Lang U, Borgwardt S. Molecular mechanisms of depression: perspectives on new treatment strategies. Cell Physiol Biochem. 2013;31:761-77 pubmed publisher
    ..Hence, GABA, AMPA, EAAT, NMDA- and metabotropic glutamate receptors (mGluR1 to mGluR8) have gained interest in depression recently...
  19. Jarius S, Metz I, König F, Ruprecht K, Reindl M, Paul F, et al. Screening for MOG-IgG and 27 other anti-glial and anti-neuronal autoantibodies in 'pattern II multiple sclerosis' and brain biopsy findings in a MOG-IgG-positive case. Mult Scler. 2016;22:1541-1549 pubmed
    ..CARPVIII), anti-protein kinase gamma (PKCgamma), anti-glutamate receptor delta 2 (GluRdelta2), anti-metabotropic glutamate receptor 1 (mGluR1) and anti-mGluR5, as well as for anti-glial nuclei antibodies (AGNA) and Purkinje cell ..
  20. Jarius S, Wildemann B. 'Medusa-head ataxia': the expanding spectrum of Purkinje cell antibodies in autoimmune cerebellar ataxia. Part 1: Anti-mGluR1, anti-Homer-3, anti-Sj/ITPR1 and anti-CARP VIII. J Neuroinflammation. 2015;12:166 pubmed publisher
    ..Many of the antigens also play a role in spinocerebellar ataxia. Part 1 focuses on anti-metabotropic glutamate receptor 1-, anti-Homer protein homolog 3-, anti-Sj/inositol 1,4,5-trisphosphate receptor- and anti-carbonic ..
  21. Jarius S, Wildemann B. 'Medusa head ataxia': the expanding spectrum of Purkinje cell antibodies in autoimmune cerebellar ataxia. Part 3: Anti-Yo/CDR2, anti-Nb/AP3B2, PCA-2, anti-Tr/DNER, other antibodies, diagnostic pitfalls, summary and outlook. J Neuroinflammation. 2015;12:168 pubmed publisher
    ..Many of the antigens also play a role in spinocerebellar ataxia. Part 1 focuses on anti-metabotropic glutamate receptor 1-, anti-Homer protein homolog 3-, anti-Sj/inositol 1,4,5-trisphosphate receptor- and anti-carbonic ..
  22. Wang C, Saar V, Leung K, Chen L, Wong G. Human amyloid ? peptide and tau co-expression impairs behavior and causes specific gene expression changes in Caenorhabditis elegans. Neurobiol Dis. 2018;109:88-101 pubmed publisher
    ..Early B-cell Factor, EBF1 (unc-3), d-amino-acid oxidase, DAO (daao-1), glutamate receptor, metabotropic 1, GRM1 (mgl-2), prolyl 4-hydroxylase subunit alpha 2, P4HA2 (dpy-18 and phy-2). Taken together, our C...
  23. Jarius S, Wildemann B. 'Medusa head ataxia': the expanding spectrum of Purkinje cell antibodies in autoimmune cerebellar ataxia. Part 2: Anti-PKC-gamma, anti-GluR-delta2, anti-Ca/ARHGAP26 and anti-VGCC. J Neuroinflammation. 2015;12:167 pubmed publisher
    ..Many of the antigens also play a role in spinocerebellar ataxia. Part 1 focuses on anti-metabotropic glutamate receptor 1-, anti-Homer protein homolog 3-, anti-Sj/inositol 1,4,5-trisphosphate receptor- and anti-carbonic ..
  24. Scotton W, Karim A, Jacob S. Glutamate Receptor Antibodies in Autoimmune Central Nervous System Disease: Basic Mechanisms, Clinical Features, and Antibody Detection. Methods Mol Biol. 2019;1941:225-255 pubmed publisher
    ..The syndromes associated with the metabotropic receptor antibodies are much rarer and often can be paraneoplastic-mGluR1 (cerebellar degeneration) and mGluR5 (Ophelia syndrome) being the ones described in literature...
  25. Lin M, Zhang B, Yu C, Li J, Zhang L, Sun H, et al. L-Glutamate supplementation improves small intestinal architecture and enhances the expressions of jejunal mucosa amino acid receptors and transporters in weaning piglets. PLoS ONE. 2014;9:e111950 pubmed publisher
    ..also increased the relative mRNA expression of the jejunal mucosa Ca(2+)-sensing receptor (CaR), metabotropic glutamate receptor 1 (mGluR1) and metabotropic glutamate receptor 4 (mGluR4), and neutral amino acid transporter B(0)-..
  26. Song Q, Gou W, Zou Y. FAM3A Protects Against Glutamate-Induced Toxicity by Preserving Calcium Homeostasis in Differentiated PC12 Cells. Cell Physiol Biochem. 2017;44:2029-2041 pubmed publisher
    ..The results of western blotting showed that FAM3A significantly decreased the surface expression of metabotropic glutamate receptor 1/5 (mGluR1/5), with no effect on the expression of N-methyl-d-aspartic acid receptor (NMDAR) or α-..
  27. Notartomaso S, Mascio G, Scarselli P, Martinello K, Fucile S, Gradini R, et al. Expression of the K+/Cl- cotransporter, KCC2, in cerebellar Purkinje cells is regulated by group-I metabotropic glutamate receptors. Neuropharmacology. 2017;115:51-59 pubmed publisher
    ..In contrast, pharmacological inhibition of mGlu1 receptors with JNJ16259685 enhanced cerebellar KCC2 protein levels and KCC2 immunoreactivity in Purkinje cells, ..
  28. Valentinova K, Mameli M. mGluR-LTD at Excitatory and Inhibitory Synapses in the Lateral Habenula Tunes Neuronal Output. Cell Rep. 2016;16:2298-307 pubmed publisher
    ..mGluR-eLTD and iLTD rely on mGluR1 and PKC signaling...
  29. du Jardin K, Müller H, Sanchez C, Wegener G, Elfving B. A single dose of vortioxetine, but not ketamine or fluoxetine, increases plasticity-related gene expression in the rat frontal cortex. Eur J Pharmacol. 2016;786:29-35 pubmed publisher
    ..The main finding was that vortioxetine enhanced plasticity-related gene expression (Mtor, Mglur1, Pkc?, Homer3, Spinophilin, and Synapsin3) in the frontal cortex at 8h after a single dose...
  30. Kanaya S, Komatsu H, Shimauchi H, Nemoto E. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016;57:417-26 pubmed publisher
    ..l-Glutamate promoted the proliferation of OCCM-30 cells, which expressed mGluR1, but not mGluR5...
  31. Aseervatham G, Suryakala U, Doulethunisha -, Sundaram S, Bose P, Sivasudha T. Expression pattern of NMDA receptors reveals antiepileptic potential of apigenin 8-C-glucoside and chlorogenic acid in pilocarpine induced epileptic mice. Biomed Pharmacother. 2016;82:54-64 pubmed publisher
    ..In addition, the mRNA expression of N-methyl-d-aspartate receptor (NMDAR), mGluR1 and mGlu5 was significantly (P?0.05) inhibited by AP8CG and CA in a lower dose...
  32. Ishibashi K, Miura Y, Ishikawa K, Zhang M, Toyohara J, Ishiwata K, et al. Relationship between type 1 metabotropic glutamate receptors and cerebellar ataxia. J Neurol. 2016;263:2179-2187 pubmed
    Imaging of type 1 metabotropic glutamate receptor (mGluR1) has recently become possible using positron emission tomography (PET). We aimed to examine the relationship between mGluR1 and cerebellar ataxia...
  33. Cavalier M, Ben Sedrine A, Thevenet L, Crouzin N, Guiramand J, de Jesus Ferreira M, et al. Disturbance of Metabotropic Glutamate Receptor-Mediated Long-Term Depression (mGlu-LTD) of Excitatory Synaptic Transmission in the Rat Hippocampus After Prenatal Immune Challenge. Neurochem Res. 2019;44:609-616 pubmed publisher
    ..This switch from LTD to LTP seemed to involve the activation of metabotropic glutamate receptor subtype 1 and 5 (mGlu1/5)...
  34. David Pereira A, Puga S, Gonçalves S, Amorim D, Silva C, Pertovaara A, et al. Metabotropic glutamate 5 receptor in the infralimbic cortex contributes to descending pain facilitation in healthy and arthritic animals. Neuroscience. 2016;312:108-19 pubmed publisher
    ..Activation of the IL mGluR1 (through co-administration of mGluR1/5 agonist and mGluR5 antagonist) did not alter nociception in controls but ..
  35. Yang B, Rajput P, Kumar U, Sastry B. Regulation of GABA Equilibrium Potential by mGluRs in Rat Hippocampal CA1 Neurons. PLoS ONE. 2015;10:e0138215 pubmed publisher
    ..While blockade of mGluR1 or mGluR5 alone could interfere with TBS-induced shifts in EGABA in neonates, only a combined blockade could do ..
  36. Dąbrowska Bouta B, Strużyńska L, Chalimoniuk M, Frontczak Baniewicz M, Sulkowski G. The influence of glutamatergic receptor antagonists on biochemical and ultrastructural changes in myelin membranes of rats subjected to experimental autoimmune encephalomyelitis. Folia Neuropathol. 2015;53:317-26 pubmed
    ..receptor antagonists amantadine and memantine (antagonists of NMDA receptors), LY 367384 (an antagonist of mGluR1), and MPEP (an mGluR5 antagonist) on the development of neurological symptoms in immunized animals, morphological ..
  37. Semenov D, Belyakov A, Glushchenko T, Samoilov M, Salinska E, Lazarewicz J. Hypobaric Preconditioning Modifies Group I mGluRs Signaling in Brain Cortex. Neurochem Res. 2015;40:2200-10 pubmed publisher
    The study assessed involvement of Ca(2+) signaling mediated by the metabotropic glutamate receptors mGluR1/5 in brain tolerance induced by hypoxic preconditioning...
  38. Ishibashi K, Miura Y, Ishikawa K, Ishii K, Ishiwata K. Decreased metabotropic glutamate receptor type 1 availability in a patient with spinocerebellar ataxia type 6: A (11)C-ITMM PET study. J Neurol Sci. 2015;355:202-5 pubmed publisher
    Imaging of metabotropic glutamate receptor type 1 (mGluR1), localized exclusively in the cerebellar Purkinje cells and related to cerebellar function, has recently become possible using positron emission tomography (PET)...
  39. Liang B, Fang J. Postnatal Isoflurane Exposure Induces Cognitive Impairment and Abnormal Histone Acetylation of Glutamatergic Systems in the Hippocampus of Adolescent Rats. J Mol Neurosci. 2016;60:11-20 pubmed publisher
    ..isoflurane exposure decreased histone acetylation of hippocampal neurons in the promoter regions of GLT-1 and mGLuR1/5, but not mGLuR2/3...
  40. Speyer C, Hachem A, Assi A, Johnson J, Devries J, Gorski D. Metabotropic glutamate receptor-1 as a novel target for the antiangiogenic treatment of breast cancer. PLoS ONE. 2014;9:e88830 pubmed publisher
    ..Recently, we detected metabotropic glutamate receptor-1 (gene: GRM1; protein: mGluR1) in breast cancer and found that it plays a role in the regulation of cell proliferation and tumor growth...
  41. Butt A, Vanzulli I, Papanikolaou M, De La Rocha I, Hawkins V. Metabotropic Glutamate Receptors Protect Oligodendrocytes from Acute Ischemia in the Mouse Optic Nerve. Neurochem Res. 2017;42:2468-2478 pubmed publisher
    ..Here, we report that group 1 mGluR1/5 and group 2 mGluR3 subunits are expressed in optic nerves from mice aged postnatal day (P)8-12 and P30-35...
  42. Albasanz J, Dalfo E, Ferrer I, Martín M. Impaired metabotropic glutamate receptor/phospholipase C signaling pathway in the cerebral cortex in Alzheimer's disease and dementia with Lewy bodies correlates with stage of Alzheimer's-disease-related changes. Neurobiol Dis. 2005;20:685-93 pubmed
    ..changes, at its greatest in isocortical stages, which was associated with a decrease in the expression levels of mGluR1 detected by Western blotting...
  43. Bartko J, Derhaschnig U, Neels T, Nabozny G, Harcken C, Leuschner J, et al. Selective glucocorticoid receptor modulation inhibits cytokine responses in a canine model of mild endotoxemia. Pharmacol Res. 2017;125:215-223 pubmed publisher
    ..The present study tested the anti-inflammatory activity of two novel non-steroidal GRMs (GRM1: BI 607812 BS, GRM2: BI 653048 BS*H3PO4) in comparison to prednisolone in a canine model of low dose endotoxemia...
  44. Liberatore F, Bucci D, Mascio G, Madonna M, Di Pietro P, Beneventano M, et al. Permissive role for mGlu1 metabotropic glutamate receptors in excitotoxic retinal degeneration. Neuroscience. 2017;363:142-149 pubmed publisher
    ..Here, we show that activation of mGlu1 metabotropic glutamate receptors largely contributes to excitotoxic degeneration of RGCs...
  45. Li G, Jorgensen M, Campbell B, Doller D. Recent Developments in Group I Metabotropic Glutamate Receptor Allosteric Modulators for the Treatment of Psychiatric and Neurological Disorders (2014-May 2015). Curr Top Med Chem. 2016;16:3470-3526 pubmed
    ..The current status of clinical mGlu5 negative allosteric modulators (NAMs) and the development of mGlu1 and mGlu5 PET ligands are also highlighted...
  46. Power E, English N, Empson R. Are Type 1 metabotropic glutamate receptors a viable therapeutic target for the treatment of cerebellar ataxia?. J Physiol. 2016;594:4643-52 pubmed publisher
    ..brain regions, the cerebellum expresses a particularly high level of Type 1 metabotropic glutamate receptors (mGluR1)...
  47. Topiol S, Sabio M. 7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5. Bioorg Med Chem Lett. 2016;26:484-494 pubmed publisher
    ..a focus on mGluR5, how the recently published, first X-ray structures of mGluR 7TM domains, specifically those of mGluR1 and mGluR5 complexed with negative allosteric modulators (NAMs), will begin to influence ligand- (e.g...
  48. Zanotti Fregonara P, Xu R, Zoghbi S, Liow J, Fujita M, Veronese M, et al. The PET Radioligand 18F-FIMX Images and Quantifies Metabotropic Glutamate Receptor 1 in Proportion to the Regional Density of Its Gene Transcript in Human Brain. J Nucl Med. 2016;57:242-7 pubmed publisher from our laboratory found that (18)F-FIMX is an excellent PET radioligand for quantifying metabotropic glutamate receptor 1 (mGluR1) in monkey brain...
  49. García Barrantes P, Cho H, Metts A, Blobaum A, Niswender C, Conn P, et al. Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool. Bioorg Med Chem Lett. 2016;26:751-756 pubmed publisher
    This Letter describes the further lead optimization of the VU0486321 series of mGlu1 positive allosteric modulators (PAMs), driven by recent genetic data linking loss of function GRM1 to schizophrenia...
  50. López Chiriboga A, Komorowski L, Kümpfel T, Probst C, Hinson S, Pittock S, et al. Metabotropic glutamate receptor type 1 autoimmunity: Clinical features and treatment outcomes. Neurology. 2016;86:1009-13 pubmed publisher
    To describe retrospectively the clinical associations of immunoglobulin G (IgG) targeting metabotropic glutamate receptor 1 (mGluR1-IgG)...
  51. King J, Eugenin E, Buckner C, Berman J. HIV tat and neurotoxicity. Microbes Infect. 2006;8:1347-57 pubmed
    ..This review discusses the most recent data addressing tat-induced neurotoxicity and integrates these new findings in the context of NeuroAIDS. ..
  52. Meera P, Pulst S, Otis T. A positive feedback loop linking enhanced mGluR function and basal calcium in spinocerebellar ataxia type 2. elife. 2017;6: pubmed publisher
    b>Metabotropic glutamate receptor 1 (mGluR1) function in Purkinje neurons (PNs) is essential for cerebellar development and for motor learning and altered mGluR1 signaling causes ataxia...
  53. Lum J, Fernandez F, Matosin N, Andrews J, Huang X, Ooi L, et al. Neurodevelopmental Expression Profile of Dimeric and Monomeric Group 1 mGluRs: Relevance to Schizophrenia Pathogenesis and Treatment. Sci Rep. 2016;6:34391 pubmed publisher
    Group 1 metabotropic glutamate receptors (mGluR1/mGluR5) play an integral role in neurodevelopment and are implicated in psychiatric disorders, such as schizophrenia...
  54. Sánchez Fuentes A, Marichal Cancino B, Méndez Díaz M, Becerril Meléndez A, Ruiz Contreras A, Prospero Garcia O. mGluR1/5 activation in the lateral hypothalamus increases food intake via the endocannabinoid system. Neurosci Lett. 2016;631:104-8 pubmed publisher
    ..Stimulation of hypothalamic mGluR1/5 and CB1 receptors induces hyperphagia suggesting a possible interaction between these systems to control food ..
  55. Majumdar A, Ahmad F, Sheikh T, Bhagat R, Pathak P, Joshi S, et al. miR-217-casein kinase-2 cross talk regulates ERK activation in ganglioglioma. J Mol Med (Berl). 2017;95:1215-1226 pubmed publisher
    ..miR-217 over-expression-mediated decrease in pERK, CK-2α, and mGluR1 levels was accompanied with increase in glycogen accumulation...
  56. Lindberg P, Teremetz M, Charron S, Kebir O, Saby A, Bendjemaa N, et al. Altered cortical processing of motor inhibition in schizophrenia. Cortex. 2016;85:1-12 pubmed publisher
    ..An exploratory genetic analysis of selected markers of inhibition (GABRB2, GAD1, GRM1, and GRM3) did not explain task-related differences in SICI or cortical activation...
  57. Hammad A, Alasmari F, Althobaiti Y, Sari Y. Modulatory effects of Ampicillin/Sulbactam on glial glutamate transporters and metabotropic glutamate receptor 1 as well as reinstatement to cocaine-seeking behavior. Behav Brain Res. 2017;332:288-298 pubmed publisher
    ..We also investigated the effects of AMP/SUL on the expression of glial glutamate transporters and metabotropic glutamate receptor 1 (mGluR1) in the nucleus accumbens (NAc) core and shell and the dorsomedial prefrontal cortex (dmPFC)...
  58. Yamasaki T, Fujinaga M, Mori W, Zhang Y, Wakizaka H, Nengaki N, et al. In Vivo Monitoring for Regional Changes of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Pilocarpine-Induced Epileptic Rat Brain by Small-Animal PET. Sci Rep. 2017;7:14945 pubmed publisher
    Metabotropic glutamate receptor subtype 1 (mGluR1) is a crucial pharmacological target for several central nervous system disorders...
  59. Gong P, Zheng A, Zhang K, Lei X, Li F, Chen D, et al. Association analysis between 12 genetic variants of ten genes and personality traits in a young chinese Han population. J Mol Neurosci. 2010;42:120-6 pubmed publisher
    ..This finding suggests that T102C in 5-TH(2A) and Val158Met in COMT play roles in some human personality traits. ..
  60. Francesconi A, Duvoisin R. Opposing effects of protein kinase C and protein kinase A on metabotropic glutamate receptor signaling: selective desensitization of the inositol trisphosphate/Ca2+ pathway by phosphorylation of the receptor-G protein-coupling domain. Proc Natl Acad Sci U S A. 2000;97:6185-90 pubmed
  61. Teh J, Shah R, La Cava S, Dolfi S, Mehta M, Kongara S, et al. Metabotropic glutamate receptor 1 disrupts mammary acinar architecture and initiates malignant transformation of mammary epithelial cells. Breast Cancer Res Treat. 2015;151:57-73 pubmed publisher
    b>Metabotropic glutamate receptor 1 (mGluR1/Grm1) is a member of the G-protein-coupled receptor superfamily, which was once thought to only participate in synaptic transmission and neuronal excitability, but has more recently been ..
  62. Parent A, Matagne V, Westphal M, Heger S, Ojeda S, Jung H. Gene expression profiling of hypothalamic hamartomas: a search for genes associated with central precocious puberty. Horm Res. 2008;69:114-23 pubmed
    ..They include IA-1 and MEF2A, two transcription factors required for neuronal development; mGluR1 and VILIP-1, which encode proteins involved in neuronal communication, and TSG-6 that encodes a protein involved ..
  63. Armbrust K, Wang X, Hathorn T, Cramer S, Chen G, Zu T, et al. Mutant ?-III spectrin causes mGluR1? mislocalization and functional deficits in a mouse model of spinocerebellar ataxia type 5. J Neurosci. 2014;34:9891-904 pubmed publisher
    ..We show that endogenous ?-III spectrin interacts with the metabotropic glutamate receptor 1? (mGluR1?) and that mice expressing mutant ?-III spectrin have cerebellar dysfunction with altered ..
  64. Lee A, Wong R, Chuang S, Shin H, Bianchi R. Role of synaptic metabotropic glutamate receptors in epileptiform discharges in hippocampal slices. J Neurophysiol. 2002;88:1625-33 pubmed
    ..Addition of 4-aminopyridine (4-AP; 100 microM) prolonged these bursts to 0.7-2 s. The mGluR1 antagonist (S)-(+)-alpha-amino-4-carboxy-2-methylbenzeneacetic acid (LY 367385; 25-100 microM) and the mGluR5 ..
  65. Tomiyama M, Kimura T, Maeda T, Tanaka H, Furusawa K, Kurahashi K, et al. Expression of metabotropic glutamate receptor mRNAs in the human spinal cord: implications for selective vulnerability of spinal motor neurons in amyotrophic lateral sclerosis. J Neurol Sci. 2001;189:65-9 pubmed
    ..spinal cord in patients with amyotrophic lateral sclerosis (ALS), we investigated the distribution of mRNAs coding mGluR1-5 in the normal human spinal cord...
  66. Brakeman P, Lanahan A, O Brien R, Roche K, Barnes C, Huganir R, et al. Homer: a protein that selectively binds metabotropic glutamate receptors. Nature. 1997;386:284-8 pubmed
    ..This dynamic transcriptional control suggests that Homer mediates a novel cellular mechanism that regulates metabotropic glutamate signalling. ..
  67. Dubovyk V, Manahan Vaughan D. Less means more: The magnitude of synaptic plasticity along the hippocampal dorso-ventral axis is inversely related to the expression levels of plasticity-related neurotransmitter receptors. Hippocampus. 2017;: pubmed publisher
    ..gradient (DH< IH< VH) was evident in the hippocampus for GluN1, the metabotropic glutamate receptors mGlu1 and mGlu2/3, GABAB and the dopamine-D1 receptor...
  68. Downey P, Petrò R, Simon J, Devlin D, Lozza G, Veltri A, et al. Identification of single nucleotide polymorphisms of the human metabotropic glutamate receptor 1 gene and pharmacological characterization of a P993S variant. Biochem Pharmacol. 2009;77:1246-53 pubmed publisher
    b>mGluR1 receptors are believed to play major roles in the pathophysiology of diseases such as anxiety and chronic pain and are being actively investigated as targets for drug development...
  69. Stephan D, Bon C, Holzwarth J, Galvan M, Pruss R. Human metabotropic glutamate receptor 1: mRNA distribution, chromosome localization and functional expression of two splice variants. Neuropharmacology. 1996;35:1649-60 pubmed
    We have isolated clones from a human brain cDNA library coding for two splice variants of mGluR1. The combined sequences account for 6864 base pairs (bp) of the approximately 7 kilobase (kb) transcript seen on northern blots of human ..
  70. Ferraguti F, Shigemoto R. Metabotropic glutamate receptors. Cell Tissue Res. 2006;326:483-504 pubmed
    ..Molecular cloning has revealed eight different subtypes (mGlu1-8) with distinct molecular and pharmacological properties...
  71. Hlavackova V, Goudet C, Kniazeff J, Zikova A, Maurel D, Vol C, et al. Evidence for a single heptahelical domain being turned on upon activation of a dimeric GPCR. EMBO J. 2005;24:499-509 pubmed
    ..These data are consistent with a model in which a single HD is turned on upon activation of such homodimeric receptors and raise important issues in deciphering the functional role of GPCR dimer formation for G-protein activation. ..
  72. Choi Y, Lee S. Enhancement of brain plasticity and recovery of locomotive function after lumbar spinal cord stimulation in combination with gait training with partial weight support in rats with cerebral ischemia. Brain Res. 2017;1662:31-38 pubmed publisher
    ..Protein expression of mGluR2 and mRNA expression of mGluR1 measured in the contralateral cortex were lower in groups 3 and 4...
  73. Ango F, Prezeau L, Muller T, Tu J, Xiao B, Worley P, et al. Agonist-independent activation of metabotropic glutamate receptors by the intracellular protein Homer. Nature. 2001;411:962-5 pubmed
    ..Our results show that these glutamate GPCRs can be directly activated by intracellular proteins as well as by agonists. ..
  74. Atluri V, Kanthikeel S, Reddy P, Yndart A, Nair M. Human synaptic plasticity gene expression profile and dendritic spine density changes in HIV-infected human CNS cells: role in HIV-associated neurocognitive disorders (HAND). PLoS ONE. 2013;8:e61399 pubmed publisher
    ..down-regulation of postsynaptic density and dendrite spine morphology regulatory proteins (ARC, NMDAR1 and GRM1) was confirmed in both clade B and C infected primary human astrocytes and SK-N-MC neuroblastoma cells...
  75. Menke A, Sämann P, Kloiber S, Czamara D, Lucae S, Hennings J, et al. Polymorphisms within the metabotropic glutamate receptor 1 gene are associated with depression phenotypes. Psychoneuroendocrinology. 2012;37:565-75 pubmed publisher
    ..Growing evidence suggests an important role of the metabotropic glutamate receptor 1 (mGlu1) in depression-related phenotypes...
  76. Mody N, Hermans E, Nahorski S, Challiss R. Inhibition of N-linked glycosylation of the human type 1alpha metabotropic glutamate receptor by tunicamycin: effects on cell-surface receptor expression and function. Neuropharmacology. 1999;38:1485-92 pubmed
    ..Our data suggest that non-N-glycosylated human mGlu1alpha receptors can traffic to the cell surface and activate phospholipase C. ..
  77. Jiang Y, Huang Y, Wong H, Zhou Y, Wang X, Yang J, et al. Elucidation of a novel extracellular calcium-binding site on metabotropic glutamate receptor 1{alpha} (mGluR1{alpha}) that controls receptor activation. J Biol Chem. 2010;285:33463-74 pubmed publisher
    b>Metabotropic glutamate receptor 1? (mGluR1?) exerts important effects on numerous neurological processes...
  78. Meldrum B, Akbar M, Chapman A. Glutamate receptors and transporters in genetic and acquired models of epilepsy. Epilepsy Res. 1999;36:189-204 pubmed
    ..acid), kainate and NMDA (N-methyl-D-aspartate) receptors and three families of metabotropic receptor (Group I: mGlu1 and mGlu5; Group II: mGlu2 and mGlu3; Group III: mGlu4, mGlu6, mGlu7 and mGlu8)...
  79. Gelb T, Pshenichkin S, Hathaway H, Grajkowska E, Dalley C, Wolfe B, et al. Atypical signaling of metabotropic glutamate receptor 1 in human melanoma cells. Biochem Pharmacol. 2015;98:182-9 pubmed publisher
    The metabotropic glutamate 1 (mGlu1) receptor has emerged as a novel target for the treatment of metastatic melanoma and various other cancers...
  80. Ali S, Shourideh M, Koochekpour S. Identification of novel GRM1 mutations and single nucleotide polymorphisms in prostate cancer cell lines and tissues. PLoS ONE. 2014;9:e103204 pubmed publisher
    b>Metabotropic glutamate receptor 1 (GRM1) signaling has been implicated in benign and malignant disorders including prostate cancer (PCa)...
  81. Jantzie L, Talos D, Selip D, An L, Jackson M, Folkerth R, et al. Developmental regulation of group I metabotropic glutamate receptors in the premature brain and their protective role in a rodent model of periventricular leukomalacia. Neuron Glia Biol. 2010;6:277-88 pubmed publisher
    ..Group I mGluRs (mGluR1 and mGluR5) were strongly expressed on OLs in neonatal rodent cerebral white matter throughout normal development, ..
  82. Ciruela F, Escriche M, Burgueno J, Angulo E, Casado V, Soloviev M, et al. Metabotropic glutamate 1alpha and adenosine A1 receptors assemble into functionally interacting complexes. J Biol Chem. 2001;276:18345-51 pubmed
  83. Kitano J, Kimura K, Yamazaki Y, Soda T, Shigemoto R, Nakajima Y, et al. Tamalin, a PDZ domain-containing protein, links a protein complex formation of group 1 metabotropic glutamate receptors and the guanine nucleotide exchange factor cytohesins. J Neurosci. 2002;22:1280-9 pubmed
    ..The results indicate that tamalin plays a key role in the association of group 1 mGluRs with the ARF-specific GEF proteins and contributes to intracellular trafficking and the macromolecular organization of group 1 mGluRs at synapses. ..
  84. Blacker C, Lewis C, Frye M, Veldic M. Metabotropic glutamate receptors as emerging research targets in bipolar disorder. Psychiatry Res. 2017;257:327-337 pubmed publisher
    ..of psychosis (rs6465084), mRNA binding protein Fragile X Mental Retardation Protein associated with altered mGluR1/5 activity in BD populations, and lithium decreasing mGluR5 expression and mGluR-mediated intracellular calcium ..
  85. Ha D, Bing S, Ahn G, Kim J, Cho J, Kim A, et al. Blocking glutamate carboxypeptidase II inhibits glutamate excitotoxicity and regulates immune responses in experimental autoimmune encephalomyelitis. FEBS J. 2016;283:3438-56 pubmed publisher
    ..Furthermore, 2-PMPA dampened the function of Th1 cell lineage and down-regulated mGluR1 expression in both periphery and CNS contributing to glutamate-mediated immune regulation...
  86. Wilkerson J, Albanesi J, Huber K. Roles for Arc in metabotropic glutamate receptor-dependent LTD and synapse elimination: Implications in health and disease. Semin Cell Dev Biol. 2018;77:51-62 pubmed publisher dendrites, where it can be rapidly and locally translated by activation of metabotropic glutamate receptors (mGluR1/5)...
  87. Sakai R, Swanson G, Shimamoto K, Green T, Contractor A, Ghetti A, et al. Pharmacological properties of the potent epileptogenic amino acid dysiherbaine, a novel glutamate receptor agonist isolated from the marine sponge Dysidea herbacea. J Pharmacol Exp Ther. 2001;296:650-8 pubmed calcium imaging experiments we found that DH also activated recombinant mGluR5 receptors but did not activate mGluR1 receptors. DH did not activate glutamate transporters or gamma-aminobutyric acid A (GABA(A)) receptors...
  88. Xie J, Chen S, Pan H. Presynaptic mGluR5 receptor controls glutamatergic input through protein kinase C-NMDA receptors in paclitaxel-induced neuropathic pain. J Biol Chem. 2017;292:20644-20654 pubmed publisher
    ..effects were blocked by the selective mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP), but not by an mGluR1 antagonist...
  89. Ganesh S, Amano K, Yamakawa K. Assignment of the gene GRM1 coding for metabotropic glutamate receptor 1 to human chromosome band 6q24 by in situ hybridization. Cytogenet Cell Genet. 2000;88:314-5 pubmed
  90. Kim S, Kim Y, Yuan J, Petralia R, Worley P, Linden D. Activation of the TRPC1 cation channel by metabotropic glutamate receptor mGluR1. Nature. 2003;426:285-91 pubmed
    Group I metabotropic glutamate receptors (consisting of mGluR1 and mGluR5) are G-protein-coupled neurotransmitter receptors that are found in the perisynaptic region of the postsynaptic membrane...
  91. Boer K, Encha Razavi F, Sinico M, Aronica E. Differential distribution of group I metabotropic glutamate receptors in developing human cortex. Brain Res. 2010;1324:24-33 pubmed publisher
    ..These findings show a differential expression pattern of group I mGluR subtypes, suggesting a role for both receptors in the early stages of corticogenesis with, however, a different contribution to human cortical developmental events. ..