Tclin GRIA3 Glutamate receptor 3

Protein Summary

Description

Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate. Glutamate receptors are the predominant excitatory neurotransmitter receptors in the mammalian brain and are activated in a variety of normal neurophysiologic processes. These receptors are heteromeric protein complexes composed of multiple subunits, arranged to form ligand-gated ion channels. The classification of glutamate receptors is based on their activation by different pharmacologic agonists. The subunit encoded by this gene belongs to a family of AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate)-sensitive glutamate receptors, and is subject to RNA editing (AGA->GGA; R->G). Alternative splicing at this locus results in different isoforms, which may vary in their signal transduction properties. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P42263
• D3DTF1
• Q4VXD5
• Q4VXD6
• Q9HDA0
• Q9HDA1
• Q9HDA2
• Q9P0H1
• GluR-3

Gene Name

• GRIA3

Ensembl ID

• ENST00000541091
• ENSP00000446440
• ENSG00000125675
• ENST00000620443
• ENSP00000478489
• ENST00000622768
• ENSP00000481554

Symbol

• GLUR3
• GLURC
• GLUR3
• GLURC
• GluA3
• MRX94
• GLUR-C
• GLUR-K3

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
cellular component	0.81
molecular function	0.81
transcription factor perturbation	0.74
protein domain	0.73
ligand (chemical)	0.72

Protein Classes

DTO Classes

Protein / Ion Channel / Glutamate-gated Ion Channel (Gic) Family Of Neurotransmitter Receptors / Gria3 Subfamily / Glutamate Receptor 3

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 159.03   (req: < 5)

Gene RIFs: 31   (req: <= 3)

Antibodies: 310   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 159.03   (req: >= 5)

Gene RIFs: 31   (req: > 3)

Antibodies: 310   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 4

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 17

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 5

Expression Data (0 Tissues)

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No expression data found

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Related Tools (3)

GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (5)

Explore Approved Drugs

1 – 5 of 5

topiramate

GRIA3Tclin IC

BLOCKER :

glutamic acid

GRIA3Tclin IC

AGONIST pKi : 7.4

ketamine

GRIA3Tclin IC

OPENER :

cyclothiazide

GRIA3Tclin IC

INHIBITOR :

perampanel

GRIA3Tclin IC

ANTAGONIST pIC50 : 6.61

Active Ligands (17)

Explore Active Ligands

1 – 10 of 17

CHEMBL276815

GRIA3Tclin IC

pKi : 6.99

CHEMBL370038

GRIA3Tclin IC

pKi : 8.28

CHEMBL13378

GRIA3Tclin IC

pKi : 7.66

CHEMBL370941

GRIA3Tclin IC

pKi : 6.84

CHEMBL372643

GRIA3Tclin IC

pKi : 5.29

LY392098

GRIA3Tclin IC

pEC50 : 6.7

LY404187

GRIA3Tclin IC

pEC50 : 6.82

CHEMBL429594

GRIA3Tclin IC

pKi : 6.73

2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(f)quinoxaline

GRIA3Tclin IC

pKi : 5.8

CHEMBL402444

GRIA3Tclin IC

pKi : 6.82

Protein-Protein Interactions (157)

Explore Interacting Targets

1 – 10 of 157

• See Interactions on String-DB

GRIA4

Tclin

Family:  IC

Novelty:  0.00284417

p_int:  1

Score:  0.948

Data Source:  BioPlex,Reactome,STRINGDB

HECTD4

Tbio

Family:  Enzyme

Novelty:  0.10275533

p_int:  0.999999982

p_ni:  4e-9

p_wrong:  1.4e-8

Score:  0.21

Data Source:  BioPlex,STRINGDB

GLRB

Tclin

Family:  IC

Novelty:  0.01721113

p_int:  0.999113019

p_ni:  0.000886937

p_wrong:  4.5e-8

Score:  0.492

Data Source:  BioPlex,STRINGDB

CCPG1

Tbio

Novelty:  0.07685013

p_int:  0.992590689

p_ni:  0.007409311

Data Source:  BioPlex

CLTCL1

Tbio

Novelty:  0.05667807

p_int:  0.989431447

p_ni:  0.010568553

Score:  0.194

Data Source:  BioPlex,STRINGDB

DNAJB9

Tbio

Novelty:  0.00536296

p_int:  0.987711075

p_ni:  0.012288925

Score:  0.158

Data Source:  BioPlex,STRINGDB

GLB1L2

Tdark

Family:  Enzyme

Novelty:  1.03866932

p_int:  0.956903554

p_ni:  0.043096446

Data Source:  BioPlex

SEMA4F

Tbio

Novelty:  0.00574057

p_int:  0.948245937

p_ni:  0.051754063

Score:  0.177

Data Source:  BioPlex,STRINGDB

FAM69A

Tdark

Novelty:  0.35978059

p_int:  0.945062949

p_ni:  0.054937051

Data Source:  BioPlex

ALG9

Tbio

Family:  Enzyme

Novelty:  0.02975572

p_int:  0.934310629

p_ni:  0.065689368

p_wrong:  3e-9

Score:  0.18

Data Source:  BioPlex,STRINGDB

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (30)

Reactome (11)

KEGG (10)

PathwayCommons (2)

WikiPathways (7)

Activation of AMPA receptors (R-HSA-399710)

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5

1 – 5 of 11

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Activation of AMPA receptors	4 targets	R-HSA-399710
Reactome	Activation of NMDA receptors and postsynaptic events	74 targets	R-HSA-442755
Reactome	Glutamate binding, activation of AMPA receptors and synaptic plasticity	31 targets	R-HSA-399721
Reactome	Neuronal System	398 targets	R-HSA-112316
Reactome	Neurotransmitter receptors and postsynaptic signal transmission	186 targets	R-HSA-112314

Name	Explore in Pharos	Explore in Source
Activation of AMPA receptors	4 targets	R-HSA-399710
Activation of NMDA receptors and postsynaptic events	74 targets	R-HSA-442755
Glutamate binding, activation of AMPA receptors and synaptic plasticity	31 targets	R-HSA-399721
Neuronal System	398 targets	R-HSA-112316
Neurotransmitter receptors and postsynaptic signal transmission	186 targets	R-HSA-112314

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (10)

Functions (3)

Components (6)

Processes (1)

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Items per page:

10

1 – 3 of 3

GO Term	Evidence	Assigned by
AMPA glutamate receptor activity	Inferred from Direct Assay (IDA)	UniProtKB
amyloid-beta binding	Inferred from Sequence or structural Similarity (ISS)	ARUK-UCL
transmitter-gated ion channel activity involved in regulation of postsynaptic membrane potential	Inferred from Electronic Annotation (IEA)	Ensembl

Disease Associations (null)

No disease associations found

GWAS Traits (0)

No GWAS traits found

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UniProt Keyword Find Similar Targets

No Header	No Header
Alternative splicing
Cell junction
Cell membrane
Complete proteome
Disease mutation
Disulfide bond
Glycoprotein
Ion channel
Ion transport
Ligand-gated ion channel

MGI Phenotype Find Similar Targets

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behavior/neurological phenotype
growth/size/body region phenotype
integument phenotype
nervous system phenotype
reproductive system phenotype

IDG Resources

No IDG generated resources found

Orthologs (9)

1 – 5 of 9

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Macaque	glutamate ionotropic receptor AMPA type subunit 3		698396
Mouse	glutamate receptor, ionotropic, AMPA3 (alpha 3)	MGI:95810	53623
Rat	glutamate ionotropic receptor AMPA type subunit 3	RGD:70958	29628
Dog	glutamate ionotropic receptor AMPA type subunit 3	VGNC:41482	492110
Horse	glutamate ionotropic receptor AMPA type subunit 3	VGNC:18580	100055136

Species	Name	OMA	EggNOG	Inparanoid
Macaque	glutamate ionotropic receptor AMPA type subunit 3
Mouse	glutamate receptor, ionotropic, AMPA3 (alpha 3)
Rat	glutamate ionotropic receptor AMPA type subunit 3
Dog	glutamate ionotropic receptor AMPA type subunit 3
Horse	glutamate ionotropic receptor AMPA type subunit 3

Publication Statistics

PubMed Score 159.03

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PubTator Score 159.18

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Related Publications

Text Mined References (62)

GeneRif Annotations (31)

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PMID	Year	Title