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GluA3

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Target not currently curated in GtoImmuPdb

Target id: 446

Nomenclature: GluA3

Family: Ionotropic glutamate receptors

Gene and Protein Information Click here for help
Species TM P Loops AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 1 894 Xq25-q26 GRIA3 glutamate ionotropic receptor AMPA type subunit 3 2,6,10
Mouse 3 1 888 X A3.3-A4 Gria3 glutamate receptor, ionotropic, AMPA3 (alpha 3) 11,13
Rat 3 1 888 Xq11 Gria3 glutamate ionotropic receptor AMPA type subunit 3 1,3,9,12
Previous and Unofficial Names Click here for help
GluR3 | GluRC | MRX94 | AMPA-selective glutamate receptor 3 | glutamate receptor, ionotropic, AMPA 3 | glutamate receptor
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
L-glutamic acid

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
(S)-5-fluorowillardiine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist - -
AMPA Small molecule or natural product Click here for species-specific activity table Hs Full agonist - -
Antagonists
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Ligand Sp. Action Value Parameter Reference
ATPO Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
GYKI53655 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
GYKI53784 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
active isomer, non-competitive
tezampanel Small molecule or natural product Click here for species-specific activity table Hs Antagonist - -
NBQX Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - -
Channel Blockers
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Use-dependent Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
extracellular argiotoxin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs - no - - - no

Not voltage dependent
extracellular joro toxin Small molecule or natural product Click here for species-specific activity table Hs - no - - - no
selective for channels lacking GluA2
Not voltage dependent
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Concentration range (M) Voltage-dependent (mV) Reference
LY404187 Small molecule or natural product Click here for species-specific activity table Hs Positive 5.8 pEC50 - no 7
pEC50 5.8 (EC50 1.66x10-6 M) [7]
Not voltage dependent
LY392098 Small molecule or natural product Click here for species-specific activity table Hs Positive 5.7 pEC50 - no 7
pEC50 5.7 (EC50 1.89x10-6 M) [7]
Not voltage dependent
cyclothiazide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Positive 4.9 pEC50 - no 7
pEC50 4.9 (EC50 1.37x10-5 M) [7]
Not voltage dependent
aniracetam Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Positive - - - no

Not voltage dependent
CX516 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Positive - - - no

Not voltage dependent
CX546 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
IDRA-21 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
LY503430 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
piracetam Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Positive - - - no

Not voltage dependent
S18986 Small molecule or natural product Click here for species-specific activity table Hs Positive - - - no

Not voltage dependent
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Mental retardation, X-linked, syndromic, Wu type; MRXSW
Synonyms: X-linked intellectual disability due to GRIA3 anomalies [Orphanet: ORPHA364028]
OMIM: 300699
Orphanet: ORPHA364028
Biologically Significant Variants Click here for help
Type:  Splice variant
Species:  Human
Description:  ‘flop’ isoform
Nucleotide accession: 
Protein accession: 
References:  2,6,10
Type:  Splice variant
Species:  Rat
Description:  ‘flop’ isoform
Nucleotide accession: 
Protein accession: 
References:  1,3,9,12
Type:  Splice variant
Species:  Rat
Description:  'flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  1,3,9,12
Type:  Splice variant
Species:  Mouse
Description:  ‘flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  11,13
Type:  Splice variant
Species:  Human
Description:  ‘flip’ isoform
Nucleotide accession: 
Protein accession: 
References:  2,6,10
Biologically Significant Variant Comments
GluA3 exists as alternatively spliced ‘flip’ and ‘flop’ isoforms which differ with respect to a cassette of 35 amino acids in the extracellular loop between M3 and M4 [3,12]. Tetrameric receptors assembled from the ‘flip’ isoform enter the desensitized state more slowly, and recover more quickly, than those formed from the ‘flop’ isoform [4,8]. RNA editing (AGA->IGA) occurs at a codon for arginine (unedited), or glycine (edited) at a locus with the extracellular loop that immediately precedes the alternatively spliced ‘flip’ and ‘flop’ modules. Edited channels recover from desensitization at a faster rate than those that are unedited [5].

References

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1. Boulter J, Hollmann M, O'Shea-Greenfield A, Hartley M, Deneris E, Maron C, Heinemann S. (1990) Molecular cloning and functional expression of glutamate receptor subunit genes. Science, 249 (4972): 1033-7. [PMID:2168579]

2. Hollmann M, Hartley M, Heinemann S. (1991) Ca2+ permeability of KA-AMPA--gated glutamate receptor channels depends on subunit composition. Science, 252 (5007): 851-3. [PMID:1709304]

3. Keinänen K, Wisden W, Sommer B, Werner P, Herb A, Verdoorn TA, Sakmann B, Seeburg PH. (1990) A family of AMPA-selective glutamate receptors. Science, 249 (4968): 556-60. [PMID:2166337]

4. Koike M, Tsukada S, Tsuzuki K, Kijima H, Ozawa S. (2000) Regulation of kinetic properties of GluR2 AMPA receptor channels by alternative splicing. J. Neurosci., 20 (6): 2166-74. [PMID:10704491]

5. Lomeli H, Mosbacher J, Melcher T, Höger T, Geiger JR, Kuner T, Monyer H, Higuchi M, Bach A, Seeburg PH. (1994) Control of kinetic properties of AMPA receptor channels by nuclear RNA editing. Science, 266 (5191): 1709-13. [PMID:7992055]

6. McNamara JO, Eubanks JH, McPherson JD, Wasmuth JJ, Evans GA, Heinemann SF. (1992) Chromosomal localization of human glutamate receptor genes. J. Neurosci., 12 (7): 2555-62. [PMID:1319477]

7. Miu P, Jarvie KR, Radhakrishnan V, Gates MR, Ogden A, Ornstein PL, Zarrinmayeh H, Ho K, Peters D, Grabell J et al.. (2001) Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. Neuropharmacology, 40 (8): 976-83. [PMID:11406188]

8. Mosbacher J, Schoepfer R, Monyer H, Burnashev N, Seeburg PH, Ruppersberg JP. (1994) A molecular determinant for submillisecond desensitization in glutamate receptors. Science, 266 (5187): 1059-62. [PMID:7973663]

9. Nakanishi N, Shneider NA, Axel R. (1990) A family of glutamate receptor genes: evidence for the formation of heteromultimeric receptors with distinct channel properties. Neuron, 5 (5): 569-81. [PMID:1699567]

10. Rampersad V, Elliott CE, Nutt SL, Foldes RL, Kamboj RK. (1994) Human glutamate receptor hGluR3 flip and flop isoforms: cloning and sequencing of the cDNAs and primary structure of the proteins. Biochim. Biophys. Acta, 1219 (2): 563-6. [PMID:7918660]

11. Sakimura K, Morita T, Kushiya E, Mishina M. (1992) Primary structure and expression of the gamma 2 subunit of the glutamate receptor channel selective for kainate. Neuron, 8 (2): 267-74. [PMID:1310861]

12. Sommer B, Keinänen K, Verdoorn TA, Wisden W, Burnashev N, Herb A, Köhler M, Takagi T, Sakmann B, Seeburg PH. (1990) Flip and flop: a cell-specific functional switch in glutamate-operated channels of the CNS. Science, 249 (4976): 1580-5. [PMID:1699275]

13. Sommer B, Köhler M, Sprengel R, Seeburg PH. (1991) RNA editing in brain controls a determinant of ion flow in glutamate-gated channels. Cell, 67 (1): 11-9. [PMID:1717158]

Contributors

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