Property Summary

NCBI Gene PubMed Count 77
PubMed Score 1295.52
PubTator Score 75.46

Knowledge Summary

Patent (62,373)

Expression

  Differential Expression (10)

Disease log2 FC p
astrocytic glioma -2.900 3.0e-03
posterior fossa group A ependymoma -3.800 2.1e-14
oligodendroglioma -2.100 1.1e-09
glioblastoma -4.000 6.1e-05
medulloblastoma -3.900 4.5e-07
atypical teratoid / rhabdoid tumor -3.900 4.2e-07
medulloblastoma, large-cell -3.600 2.4e-04
adult high grade glioma -3.300 5.9e-05
pituitary cancer 1.800 2.6e-02
psoriasis -1.200 3.4e-02

MLP Assay (2)

AID Type Active / Inconclusive / Inactive Description
588737 other 2 / 0 / 0 hmGluR5_Calcium_Fold_Shift
743419 confirmatory 0 / 0 / 1 Selectivity Studies of mglur8 probe at mglur5

Gene RIF (66)

PMID Text
26667279 The interaction between GRM5 and cellular prion protein has a central role in transgenic mouse model of Alzheimer's disease pathogenesis.
26645628 The metabotropic glutamate receptor subtype 5 (mGluR5) has been implicated in the pathophysiology of mood and anxiety disorders.
26311002 Data suggest that metabotropic glutamate receptors recycling is completely dependent on the activity of PP2A whereas, PP2B has partial effect on this process.
26052099 findings provide evidence for decreased expression of metabotropic glutamate receptor 5 and its signaling components representing a key pathophysiological hallmark in autism spectrum disorder.
26048293 Study provided evidence that protein expression of mGluR5 is significantly higher (total: 42%; monomer: 25%; dimer: 52%) in the hippocampal CA1 region of schizophrenia subjects relative to healthy controls
25778620 Results provide compelling evidence that mGluR5 regulation is altered in schizophrenia, likely contributing to the altered glutamatergic signaling that is associated with the disorder
25704074 This review supports altered mGluR5 functioning as a convergent point in ASD pathogenesis and indicates more research is warranted into mGluR5 as a potential therapeutic target.
25613138 The gene expression of GRM5 is significantly upregulated in both clade B and clade C Tat treated SK-N-MC neuroblastoma cells
25115540 Findings demonstrate a developmental regulation of mGluR5 in the hippocampus and suggest a role for this receptor in astrocytes during early development in Down's syndrome hippocampus
25003238 reflected in the immunoblotting data Mglur5 receptors were detected at higher levels of expression in patient with cortical dysplasia with intractable epilepsy.
24969128 Decrease of mGluR5 receptor density goes parallel with changes in enkephalin and substance P immunoreactivity in Huntington's disease
24949866 Findings suggest that mGluR2/3 and mGluR5s are unaltered in the anterior cingulate cortex in psychotic and nonpsychotic depression, bipolar disorder and schizophrenia
24925192 gnificantly higher expression level in the metabotropic receptor genes GRM5 in Locus coeruleus neurons.
24833114 significant positive correlation between Yale-Brown Obsessive Compulsive Scale obsession sub-score and mGluR5 distribution volume ratio in the cortico-striatal-thalamo-cortical brain circuit; results suggest obsessions in particular might have an underlying glutamatergic pathology related to mGluR5
24548786 both an increased and reduced mGlu5 functioning seem to be associated with Intellectual Disability and autism spectrum disorders.
24528109 Our findings highlight the subtleties of allosteric modulator binding to mGlu5 and demonstrate the utility in incorporating SAR information to strengthen the interpretation and analyses of docking and mutational data.
24332449 a dysregulation of its signaling in fragile X mental retardation gene 1 premutation carriers, which would likely contribute to the development and severity of fragile X-associated tremor/atasia syndrome.
24040811 Review provides an update of the current state of the art of mGlu5 receptor-based manipulations to alleviate the symptoms of Parkinson's disease.
23804486 This study demonistrated that mGluR5 upregulation also participates in counterbalance mechanisms along the hyperexcitable circuitry uniquely altered in TLE hippocampal formation.
23705503 this study provides evidence that GRK2 mediates phosphorylation-independent mGluR5 desensitization via the interaction between the RGS domain and Galphaq in HEK 293 cells.
23628984 tobacco smoking was associated with lower mGluR5 availability in the brain in both cocaine users and controls, while cocaine use was not linked to detectable mGluR5 alterations
23627706 This study demonistrated that metabotropic receptor mGluR5 was found to be expressed by just 40% of striatal neurons in young individuals, with significant intensity variations among the neurons.
23524143 Knockdown of mGluR5 inhibited icariin induced reactive oxygen species generation and NF-kappaB nuclear translocation.
23478188 Plasma glutamate-modulated interaction of A2AR and mGluR5 on BMDCs aggravates traumatic brain injury-induced acute lung injury.
23225313 The pattern of mGluR5 expression by neural stem/progenitor cells, neuroblasts and neurons provides important anatomical evidence for the role of mGluR5 in the regulation of human hippocampal development
23152621 Calmodulin-regulated Siah-1A binding to mGluR5 dynamically regulates mGluR5 trafficking
23149219 the promoter methylation of the GMR2 and GMR5 genes greatly decreased the risk of schizophrenia, and the expression level of the GRM2, GRM5, and GRIA3 genes increased significantly in patients in comparison to healthy controls.
22995293 data demonstrate that mGluR5 receptors internalize without the application of ligand and the internalized receptors recycle back to the cell surface following constitutive endocytosis.
22543119 mGluR5 is expressed by a variety of cells such as neural stem cells in the frontal cortex, ventricular zone and subventricular zone in human fetuses.
22340009 mGluR5 inhibition and stimulation in the nucleus accumbens can regulate cocaine-seeking, and demonstrate that one mechanism for this effect is via interactions with Homer proteins
22256945 Human mGluR5, GABA(A,B), and CB(1,2) receptors are abundantly expressed along the vago-vagal neural pathway and involved in the triggering of transient lower esophageal sphincter relaxations
22032949 the results of this study show that using the equilibrium method is an acceptable alternative to the standard kinetic method when using 18F-SP203 to measure mGluR5
21901840 Metabotropic glutamate receptor 5 upregulation in children with autism is associated with underexpression of both Fragile X mental retardation protein and GABAA receptor beta 3 in adults with autism.
21723923 mGluR5 promoted the proliferation of human embryonic cortical neural stem/progenitor cells
21103359 Results highlight the therapeutic importance of mGluR5 antagonists in alpha-synucleinopathies.
20628086 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
20468064 Observational study of gene-disease association. (HuGE Navigator)
20398908 Observational study of gene-disease association. (HuGE Navigator)
20379614 Clinical trial of gene-disease association and gene-environment interaction. (HuGE Navigator)
20149785 These findings show a differential expression pattern of mGluR1a and mGluR5, suggesting a role for both receptors in the early stages of corticogenesis with, however, a different contribution to human cortical developmental events.
20036444 Elevated glutamatergic transmission as measured with increased mGluR5 specific binding is associated with human motor complications; its antagonism can be targeted for patients' treatment.
19913121 Observational study of gene-disease association. (HuGE Navigator)
19694902 NECAB2 by its physical interaction with mGlu(5b) receptor modulates receptor function
19401173 findings suggest that changes in astrocyte mGlu5 receptors may be part of an adaptive response to the progressive nature of Alzheimer's disease
19156168 Clinical trial of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
19086053 Observational study of gene-disease association. (HuGE Navigator)
18991960 Review. The structure and function of mGLUR5 and the mechanisms and SARs of its antagonists are reviewed.
18606955 Observational study of gene-disease association. (HuGE Navigator)
18541671 These results provide insight into a glutamate-induced regulatory pathway distinct from that described for cytokine-induced NF-kappaB activation and have important implications with regard to both normal glial cell physiology and pathogenesis.
18337251 the nucleus can function as an autonomous organelle independent of signals originating in the cytoplasm, and nuclear mGlu5 receptors play a dynamic role in mobilizing Ca2+ in a specific, localized fashion
18182392 deletion of the C terminus of the mGlu5a receptor abolishes both its interaction with the NMDA receptor and reciprocal inhibition of the receptors
17998106 This study provides the first quantitative demonstration and direct comparison of a PET tracer candidate identifying mGluR5 binding sites in mammalian cerebellum.
17627080 We documented for the first time the expression of the mGluR5 and EAAT1 in MG-63 cells, as well as the ability of dexamethasone to upregulate the expression of the mGluR5 and EAAT1 in the MG-63 cells.
17311919 there is an alpha-actinin-1-dependent mGlu(5b) receptor association with the actin cytoskeleton modulating receptor cell surface expression and functioning
15894802 it is phosphorylation of Ser-839, not Thr-840, that is absolutely required for the unique Ca2+ oscillations produced by mGluR5 activation
15184389 metabotropic glutamate receptors 1 and 5 mediate opposite glutamate effects in human lymphocyte activation
15158450 glial progenitor cells present in the adult human CNS express mGluR3 and mGluR5a
15076751 We found a selective expression of the group I receptor mGluR5 in human parasympathetic Onuf's nucleus, strengthening the hypothesis that mGluR expression may provide a possible clue to the selective vulnerability in ALS.
14561742 activation of mGluR5 causes translocation of both gammaPKC and deltaPKC to the plasma membrane. deltaPKC, but not gammaPKC, phosphorylates mGluR5 Thr(840), leading to the blockade of both Ca2+ oscillations and gammaPKC cycling.
12786977 mGluR3 and mGluR5 can critically and differentially modulate the expression of glutamate transporters and may represent interesting pharmacological targets to regulate the extracellular levels of glutamate in pathological conditions.
12783878 alternative 5'-splicing and usage of multiple promoters may contribute to regulatory mechanisms for tissue- and context-specific expression of the mGluR5 gene
12736269 mGlu5 on nuclear membranes has a role in mediating intranuclear Ca2+ changes in heterologous cell types and neurons
12531526 Data report the identification of a novel variant of the G-protein coupled metabotropic glutamate receptor mGlu5 (hmGlu5d) generated by alternative splicing at the C-terminal domain.
12531512 Data report the isolation of a novel gene termed metabotropic glutamate receptor 5-related (mGluR5R) [mGluR5R].
12119301 mGLUR5 and 1,4,5-InsP3 signaling control calcium release
11326300 Observational study of gene-disease association. (HuGE Navigator)

AA Sequence

MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAVREQYGIQRVE      1 - 70
AMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISSEEEEGLVRCVDGSSSSFRSK     71 - 140
KPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLSDKTLFKYFMRVVPSDAQQARAMVDIVKRYN    141 - 210
WTYVSAVHTEGNYGESGMEAFKDMSAKEGICIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEG    211 - 280
MTVRGLLMAMRRLGLAGEFLLLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNH    281 - 350
RNPWFQEFWQHRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCP    351 - 420
GYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFDYINVGSWDNG    421 - 490
ELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKENEYVFDEYTCKACQLGSWPTD    491 - 560
DLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVVFIIYRDTPVVKSSSRELCYIILAGICLGYL    561 - 630
CTFCLIAKPKQIYCYLQRIGIGLSPAMSYSALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFIL    631 - 700
ICIQLGIIVALFIMEPPDIMHDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNE    701 - 770
AKYIAFTMYTTCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTS    771 - 840
TVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMGNGGRATMSSS    841 - 910
NGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRGLGAGAGAGGSAGGVGATGGA    911 - 980
GCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPSPISTLSHRAGSASRTDDDVPSLHSEPVARS    981 - 1050
SSSQGSLMEQISSVVTRFTANISELNSMMLSTAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPA   1051 - 1120
IEVTGGAQPAAGAQAAGDAARESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALC   1121 - 1190
IPSSPKYDTLIIRDYTQSSSSL                                                   1191 - 1212
//

Text Mined References (78)

PMID Year Title
26667279 2016 Metabotropic glutamate receptor 5 couples cellular prion protein to intracellular signalling in Alzheimer's disease.
26645628 2015 Characterization of brain mGluR5 binding in a pilot study of late-life major depressive disorder using positron emission tomography and [¹¹C]ABP688.
26311002 2015 Differential effects of protein phosphatases in the recycling of metabotropic glutamate receptor 5.
26052099 2015 Decreased expression of mGluR5 within the dorsolateral prefrontal cortex in autism and increased microglial number in mGluR5 knockout mice: Pathophysiological and neurobehavioral implications.
26048293 2015 Metabotropic glutamate receptor 5, and its trafficking molecules Norbin and Tamalin, are increased in the CA1 hippocampal region of subjects with schizophrenia.
25778620 2015 Alterations of mGluR5 and its endogenous regulators Norbin, Tamalin and Preso1 in schizophrenia: towards a model of mGluR5 dysregulation.
25704074 2015 Convergent evidence for mGluR5 in synaptic and neuroinflammatory pathways implicated in ASD.
25115540 2014 Metabotropic glutamate receptor 5 in Down's syndrome hippocampus during development: increased expression in astrocytes.
25003238 2014 Expression of astrocyte-related receptors in cortical dysplasia with intractable epilepsy.
24969128 2015 Decrease of mGluR5 receptor density goes parallel with changes in enkephalin and substance P immunoreactivity in Huntington's disease: a preliminary investigation in the postmortem human brain.
24949866 2014 Metabotropic glutamate receptor mGluR2/3 and mGluR5 binding in the anterior cingulate cortex in psychotic and nonpsychotic depression, bipolar disorder and schizophrenia: implications for novel mGluR-based therapeutics.
24925192 2014 Elevated gene expression of glutamate receptors in noradrenergic neurons from the locus coeruleus in major depression.
24833114 2014 Metabotropic glutamate receptor 5 binding in patients with obsessive-compulsive disorder.
24548786 2014 Dysregulation of group-I metabotropic glutamate (mGlu) receptor mediated signalling in disorders associated with Intellectual Disability and Autism.
24532677 2015 A genome-wide association study of rheumatoid arthritis without antibodies against citrullinated peptides.
24528109 2014 Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.
24332449 2014 Reduced excitatory amino acid transporter 1 and metabotropic glutamate receptor 5 expression in the cerebellum of fragile X mental retardation gene 1 premutation carriers with fragile X-associated tremor/ataxia syndrome.
24040811 2013 Targeting striatal metabotropic glutamate receptor type 5 in Parkinson's disease: bridging molecular studies and clinical trials.
23804486 2013 Distinct increased metabotropic glutamate receptor type 5 (mGluR5) in temporal lobe epilepsy with and without hippocampal sclerosis.
23705503 [Phosphorylation-independent desensitization of metabotropic glutamate receptor 5 by G protein-coupled receptor kinase 2 in HEK 293 cells].
23628984 2014 Smoking but not cocaine use is associated with lower cerebral metabotropic glutamate receptor 5 density in humans.
23627706 2013 Glutamate receptors in human caudate nucleus in normal aging and Alzheimer's disease.
23524143 2013 mGluR5 stimulating Homer-PIKE formation initiates icariin induced cardiomyogenesis of mouse embryonic stem cells by activating reactive oxygen species.
23478188 2013 Plasma glutamate-modulated interaction of A2AR and mGluR5 on BMDCs aggravates traumatic brain injury-induced acute lung injury.
23376485 2013 Proteomic analysis of podocyte exosome-enriched fraction from normal human urine.
23227193 2012 Analysis of copy number variation in Alzheimer's disease in a cohort of clinically characterized and neuropathologically verified individuals.
23225313 2012 Developmental distribution pattern of metabotropic glutamate receptor 5 in prenatal human hippocampus.
23152621 2012 PKC phosphorylation regulates mGluR5 trafficking by enhancing binding of Siah-1A.
23149219 2013 Evaluation of hypermethylation and expression pattern of GMR2, GMR5, GMR8, and GRIA3 in patients with schizophrenia.
22995293 2012 Constitutive internalization and recycling of metabotropic glutamate receptor 5 (mGluR5).
22543119 2012 [Developmental expression and cellular distribution of metabotropic glutamate receptor 5 in the frontal cortex of human fetus].
22340009 2013 Role of mGluR5 neurotransmission in reinstated cocaine-seeking.
22256945 2012 Localization of mGluR5, GABAB, GABAA, and cannabinoid receptors on the vago-vagal reflex pathway responsible for transient lower esophageal sphincter relaxation in humans: an immunohistochemical study.
22032949 2012 Quantification of metabotropic glutamate subtype 5 receptors in the brain by an equilibrium method using 18F-SP203.
22012869 2011 Genome-wide association study in German patients with attention deficit/hyperactivity disorder.
21901840 2011 Metabotropic glutamate receptor 5 upregulation in children with autism is associated with underexpression of both Fragile X mental retardation protein and GABAA receptor beta 3 in adults with autism.
21723923 2011 Metabotropic glutamate receptor 5 promotes proliferation of human neural stem/progenitor cells with activation of mitogen-activated protein kinases signaling pathway in vitro.
21103359 2010 Alterations in mGluR5 expression and signaling in Lewy body disease and in transgenic models of alpha-synucleinopathy--implications for excitotoxicity.
20628086 2010 Variation at the NFATC2 locus increases the risk of thiazolidinedione-induced edema in the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM) study.
20468064 2010 Association study of 182 candidate genes in anorexia nervosa.
20398908 2010 Comprehensive copy number variant (CNV) analysis of neuronal pathways genes in psychiatric disorders identifies rare variants within patients.
20379614 Personalized smoking cessation: interactions between nicotine dose, dependence and quit-success genotype score.
20149785 2010 Differential distribution of group I metabotropic glutamate receptors in developing human cortex.
20041166 2009 Common genetic variation and the control of HIV-1 in humans.
20036444 2011 Metabotropic glutamate receptor type 5 in levodopa-induced motor complications.
19913121 2009 Gene-centric association signals for lipids and apolipoproteins identified via the HumanCVD BeadChip.
19694902 2009 The association of metabotropic glutamate receptor type 5 with the neuronal Ca2+-binding protein 2 modulates receptor function.
19401173 2009 Up-regulation of astrocyte metabotropic glutamate receptor 5 by amyloid-? peptide.
19340012 2009 Genome-wide association study of tanning phenotype in a population of European ancestry.
19156168 2009 Pharmacogenetics of antipsychotic response in the CATIE trial: a candidate gene analysis.
19086053 2009 Identification of new putative susceptibility genes for several psychiatric disorders by association analysis of regulatory and non-synonymous SNPs of 306 genes involved in neurotransmission and neurodevelopment.
18991960 2008 Antagonists at metabotropic glutamate receptor subtype 5: structure activity relationships and therapeutic potential for addiction.
18606955 2008 Systematic analysis of glutamatergic neurotransmission genes in alcohol dependence and adolescent risky drinking behavior.
18541671 2008 Essential role for epidermal growth factor receptor in glutamate receptor signaling to NF-kappaB.
18337251 2008 Activated nuclear metabotropic glutamate receptor mGlu5 couples to nuclear Gq/11 proteins to generate inositol 1,4,5-trisphosphate-mediated nuclear Ca2+ release.
18182392 2008 Direct interaction enables cross-talk between ionotropic and group I metabotropic glutamate receptors.
17998106 2007 Species differences in mGluR5 binding sites in mammalian central nervous system determined using in vitro binding with [18F]F-PEB.
17627080 Regulation of the mGluR5, EAAT1 and GS expression by glucocorticoids in MG-63 osteoblast-like osteosarcoma cells.
17311919 2007 Actin-binding protein alpha-actinin-1 interacts with the metabotropic glutamate receptor type 5b and modulates the cell surface expression and function of the receptor.
16554811 2006 Human chromosome 11 DNA sequence and analysis including novel gene identification.
15894802 2005 Protein kinase C phosphorylation of the metabotropic glutamate receptor mGluR5 on Serine 839 regulates Ca2+ oscillations.
15184389 2004 Group I metabotropic glutamate receptors mediate a dual role of glutamate in T cell activation.
15158450 2004 Metabotropic glutamate receptors are expressed in adult human glial progenitor cells.
15076751 2004 Differential expression of mGluR5 in human lumbosacral motoneurons.
14561742 2004 Isoform-specific phosphorylation of metabotropic glutamate receptor 5 by protein kinase C (PKC) blocks Ca2+ oscillation and oscillatory translocation of Ca2+-dependent PKC.
12786977 2003 Expression and functional role of mGluR3 and mGluR5 in human astrocytes and glioma cells: opposite regulation of glutamate transporter proteins.
12783878 2003 Gene structure of the human metabotropic glutamate receptor 5 and functional analysis of its multiple promoters in neuroblastoma and astroglioma cells.
12736269 2003 Activation of metabotropic glutamate receptor mGlu5 on nuclear membranes mediates intranuclear Ca2+ changes in heterologous cell types and neurons.
12531526 2002 Identification and characterization of a novel splice variant of the metabotropic glutamate receptor 5 gene in human hippocampus and cerebellum.
12531512 2002 Characterization of mGluR5R, a novel, metabotropic glutamate receptor 5-related gene.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12119301 2002 Determinants of metabotropic glutamate receptor-5-mediated Ca2+ and inositol 1,4,5-trisphosphate oscillation frequency. Receptor density versus agonist concentration.
11326300 2001 The genomic organisation of the metabotropic glutamate receptor subtype 5 gene, and its association with schizophrenia.
9110174 1997 Large-scale concatenation cDNA sequencing.
8619474 1996 A "double adaptor" method for improved shotgun library construction.
8532169 1995 Molecular and functional characterization of recombinant human metabotropic glutamate receptor subtype 5.
7908515 1994 Molecular cloning and the functional expression of two isoforms of human metabotropic glutamate receptor subtype 5.
7688218 1993 A variant of metabotropic glutamate receptor subtype 5: an evolutionally conserved insertion with no termination codon.