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Gene and Protein Information | ||||||
class C G protein-coupled receptor | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 7 | 1194 | 6q24.3 | GRM1 | glutamate metabotropic receptor 1 | 20,33,101 |
Mouse | 7 | 1199 | 10 A1 | Grm1 | glutamate receptor, metabotropic 1 | 125 |
Rat | 7 | 1199 | 1p13 | Grm1 | glutamate metabotropic receptor 1 | 44,77 |
Previous and Unofficial Names |
GPRC1A | metabotropic glutamate receptor 1 | wobl | MGLUR1 | SCAR13 | glutamate receptor, metabotropic 1 | glutamate receptor |
Database Links | |
Specialist databases | |
GPCRdb | grm1_human (Hs), grm1_mouse (Mm), grm1_rat (Rn) |
Other databases | |
Alphafold | Q13255 (Hs), P97772 (Mm), P23385 (Rn) |
ChEMBL Target | CHEMBL3772 (Hs), CHEMBL2892 (Mm), CHEMBL4477 (Rn) |
Ensembl Gene | ENSG00000152822 (Hs), ENSMUSG00000019828 (Mm), ENSRNOG00000068415 (Rn), ENSRNOG00000014290 (Rn) |
Entrez Gene | 2911 (Hs), 14816 (Mm), 24414 (Rn) |
Human Protein Atlas | ENSG00000152822 (Hs) |
KEGG Gene | hsa:2911 (Hs), mmu:14816 (Mm), rno:24414 (Rn) |
OMIM | 604473 (Hs) |
Orphanet | ORPHA327283 (Hs) |
Pharos | Q13255 (Hs) |
RefSeq Nucleotide | NM_001278067 (Hs), NM_001278066 (Hs), NM_001278064 (Hs), NM_001278065 (Hs), NM_016976 (Mm), NM_001114333 (Mm), NM_017011 (Rn), NM_001114330 (Rn) |
RefSeq Protein | NP_001264995 (Hs), NP_001264994 (Hs), NP_001264996 (Hs), NP_001264993 (Hs), NP_001107805 (Mm), NP_058672 (Mm), NP_001107802 (Rn), NP_058707 (Rn) |
UniProtKB | Q13255 (Hs), P97772 (Mm), P23385 (Rn) |
Wikipedia | GRM1 (Hs) |
Selected 3D Structures | |||||||||||||
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Natural/Endogenous Ligands |
L-glutamic acid |
Comments: Other endogenous ligands include L-aspartic acid, L-serine-O-phosphate, NAAG and L-cysteine sulphinic acid |
Download all structure-activity data for this target as a CSV file
Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Agonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Values indicated are those determined from binding studies on recombinant mGlu1a receptors. Further information on agonist pharmacology as based on functional assays can be found in [95]. So far no differences in the agonist pharmacological profile has been reported between the rat and human mGlu1 receptors using functional assays. The best characterized agonists of the ionotropic glutamate receptors, AMPA, NMDA and kainate are inactive on mGlu1. Although several splice variants of mGlu1 have been identified (see below), all are likely to have an identical agonist pharmacology since they possess an indentical agonist binding site. The agonist binding site is located in the large extracellular domain of this receptor, that retains its ability to bind ligands when produced as a soluble protein. The structure of this binding domain has been solved [57,114]. This domain is formed of two lobes, and agonists bind in the cleft between the two lobes. Agonists likely stabilize a closed form of this domain, whereas antagonists prevent closure. Functional importance of critical residues involved in agonist action has been confirmed by mutagenesis studies [84,93]. Cations such as Ca2+ have been proposed to directly activate mGlu1 receptors [28,56,109]. However, it is still unclear whether this is a direct agonist effect or if this is due to a potentiation of ambient glutamate produced by the cells expressing the recombinant receptor. |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific antagonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Indicated affinities were determined by displacement studies of [3H]quisqualate bound on HEK cell membranes expressing a recombinant rat mGlu1 (except for LY341495 value determined from functional studies). More information on agonist potencies determined from functional studies can be obtained from [95]. So far no differences have been reported for the antagonist affinities between the rat and the human receptor. Although LY367385 and AIDA have been shown to specifically antagonize mGlu1 receptors versus mGlu5, both compounds are able to displace bound [3H]quisqualate to mGlu5 (see [95]). |
Allosteric Modulators | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific allosteric modulator tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Allosteric Modulator Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Values for Ro67-4853 and Ro67-7476 were determined by binding studies using [3H]R214127 binding [59] or from functional studies [11,53,65]. Among these allosteric regulators only NPS2390 is not mGlu1 selective, being also active as a negative allosteric modulator of mGlu5. Among the positive modulators, only Ro67-4853 is active on the human receptor [53]. The binding site of all allosteric regulators have been mapped within the 7 transmembrane domain of the receptor [11,53,65,71]. |
Primary Transduction Mechanisms | |
Transducer | Effector/Response |
Gq/G11 family | Phospholipase C stimulation |
Comments: The primary action of the mGlu1 is to activate PLC through stimulating Gq/11, resulting in the PIP2 breakdown which can be monitored as the production of inositol phosphate. The PIP2 breakdown causes the increases in the intracellular calcium concentration and the activation of the TRPC channels [39]. The primary transduction is observed both in cell lines and the native tissue expressing the mGlu1. | |
References: 3,17,25,88 |
Secondary Transduction Mechanisms | |
Transducer | Effector/Response |
Gs family Gi/Go family G protein independent mechanism |
Adenylyl cyclase stimulation Adenylyl cyclase inhibition Phospholipase A2 stimulation Phospholipase D stimulation Other - See Comments |
Comments: Stimulation of adenylyl cyclase via mGlu1 has been reported in transfected cell lines [25] and suggested in neuronal cells [104]. Activation of the mGlu1 triggers the PTX-sensitive Gi/o signaling pathway in transfected cell lines, but its physiological role is unclear. The mGlu1 also induces the phospohrylation of the ERK in the G protein dependent and independent manner. In the latter case, the effects are mediated via beta-arrestin and dependent on the type of the ligands [23]. Activation of PLD has been reported in a cell line and native tissues [25,96]. The mGlu1 has been reported to activate the TRPC1 channels indepedently of G protein [51]. | |
References: 3,17,25,88 |
Tissue Distribution | ||||||||
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Expression Datasets | |
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Physiological Functions | ||||||||
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Physiological Consequences of Altering Gene Expression | ||||||||||
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Phenotypes, Alleles and Disease Models | Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Clinically-Relevant Mutations and Pathophysiology | ||||||||||||||||||||||||||||||||
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Clinically-Relevant Mutations and Pathophysiology Comments | ||||||||||||||||||||||||||||||||
In patients with congenital cerebellar ataxia, the mutated receptor is predicted not to possess the 7 transmembrane domain and therefore to be nonfunctional. Besides mutation, autoantibodies against the mGlu1 receptor have been reported in patients with paraneoplastic cerebellar ataxia [16,99]. |
Biologically Significant Variants | ||||||||||||||
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Biologically Significant Variant Comments | ||||||||||||||
In humans mGlu1, mGlu1(c) and mGlu1(e) have not been identified. The amino acid sequence of the mGlu1(f) is predicted to be same as the mGlu1(b). Genomic data supports the existance of mGlu(1d) in mice According to genomic sequences mGlu1e appears possible in rat but does not seem to be present in human genomic sequences. |
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