Tclin GRIA1 Glutamate receptor 1

Protein Classes

DTO Classes

Protein / Ion Channel / Glutamate-gated Ion Channel (Gic) Family Of Neurotransmitter Receptors / Gria1 Subfamily / Glutamate Receptor 1

Protein Summary

Description

Ionotropic glutamate receptor. 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 with multiple subunits, each possessing transmembrane regions, and all arranged to form a ligand-gated ion channel. The classification of glutamate receptors is based on their activation by different pharmacologic agonists. This gene belongs to a family of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptors. Alternatively spliced transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P42261
• B7Z2S0
• B7Z2W8
• B7Z3F6
• B7Z9G9
• D3DQI4
• E7ESV8
• Q2NKM6
• GluR-1

Gene Name

• GRIA1

Ensembl ID

• ENST00000285900
• ENSP00000285900
• ENSG00000155511
• ENST00000340592
• ENSP00000339343
• ENST00000448073
• ENSP00000415569
• ENST00000518142
• ENSP00000427920
• ENST00000518783
• ENSP00000428994
• ENST00000521843
• ENSP00000427864

Symbol

• GLUH1
• GLUR1
• GLUH1
• GLUR1
• GLURA
• GluA1
• HBGR1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	0.9
hub protein	0.88
biological term	0.81
kinase	0.8
trait	0.75

Related Tools

Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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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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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: 2072.47   (req: < 5)

Gene RIFs: 55   (req: <= 3)

Antibodies: 932   (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: 2072.47   (req: >= 5)

Gene RIFs: 55   (req: > 3)

Antibodies: 932   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 13

Tchem

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

Active Ligands: 68

Tclin

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

Active Drugs: 6

Approved Drugs (6)

Explore Approved Drugs

1 – 6 of 6

topiramate

GRIA1Tclin IC

ANTAGONIST :

glutamic acid

GRIA1Tclin IC

Ki : 5.87

ketamine

GRIA1Tclin IC

OPENER :

kainic acid

GRIA1Tclin IC

Ki : 5.13

cyclothiazide

GRIA1Tclin IC

EC50 : 5.7

perampanel

GRIA1Tclin IC

ANTAGONIST IC50 : 6.61

Active Ligands (68)

Explore Active Ligands

1 – 10 of 68

CHEMBL51660

GRIA1Tclin IC

Ki : 5.96

CHEMBL299180

GRIA1Tclin IC

Ki : 6.16

CHEMBL276815

GRIA1Tclin IC

Ki : 7.66

CHEMBL372643

GRIA1Tclin IC

Ki : 5.29

CHEMBL370941

GRIA1Tclin IC

Ki : 6.84

CHEMBL13378

GRIA1Tclin IC

Ki : 7.66

CHEMBL370038

GRIA1Tclin IC

Ki : 8.28

CHEMBL222519

GRIA1Tclin IC

Ki : 5.8

CHEMBL193087

GRIA1Tclin IC

Ki : 5

CHEMBL1097939,CHEMBL435582

GRIA1Tclin IC

EC50 : 5.25

GWAS Traits (10)

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5

1 – 5 of 10

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
C-reactive protein measurement	EFO_0004458	1	1	1		67.5
self reported educational attainment	EFO_0004784	1	1	1		58.9
insomnia measurement	EFO_0007876	1	2	0	1	56.5
sudden cardiac arrest	EFO_0004278	1	1	0	1.5	35.9
grip strength measurement	EFO_0006941	1	1	1		34.9

• Explore on Target Illumination GWAS Analytics (TIGA)

Items per page:

5

1 – 5 of 10

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
C-reactive protein measurement	EFO_0004458	1		67.5
self reported educational attainment	EFO_0004784	1		58.9
insomnia measurement	EFO_0007876	0	1	56.5
sudden cardiac arrest	EFO_0004278	0	1.5	35.9
grip strength measurement	EFO_0006941	1		34.9

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Orthologs (14)

1 – 5 of 14

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	glutamate ionotropic receptor AMPA type subunit 1	VGNC:8622	471714
Macaque	glutamate ionotropic receptor AMPA type subunit 1		714117
Mouse	glutamate receptor, ionotropic, AMPA1 (alpha 1)	MGI:95808	14799
Rat	glutamate ionotropic receptor AMPA type subunit 1	RGD:621531	50592
Dog	glutamate ionotropic receptor AMPA type subunit 1	VGNC:41480	489168

Species	Name	OMA	EggNOG	Inparanoid
Chimp	glutamate ionotropic receptor AMPA type subunit 1
Macaque	glutamate ionotropic receptor AMPA type subunit 1
Mouse	glutamate receptor, ionotropic, AMPA1 (alpha 1)
Rat	glutamate ionotropic receptor AMPA type subunit 1
Dog	glutamate ionotropic receptor AMPA type subunit 1

Protein Structure (0 Structures, 1 AlphaFold Model)

Representation

  axes   backbone   ball+stick   cartoon   rocket   rope   spacefill

Color Scheme

  target   atomindex   bfactor   chainname   electrostatic   element   hydrophobicity   resname   sstruc

AF-P42261-F1-model_v1

AlphaFold Structures Developed by DeepMind and EMBL-EBI

Pathways (103)

Reactome (22)

KEGG (11)

PathwayCommons (2)

WikiPathways (68)

Activation of AMPA receptors (R-HSA-399710)

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5

1 – 5 of 22

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	Asparagine N-linked glycosylation	286 targets	R-HSA-446203
Reactome	COPII-mediated vesicle transport	68 targets	R-HSA-204005
Reactome	Cargo concentration in the ER	33 targets	R-HSA-5694530

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
Asparagine N-linked glycosylation	286 targets	R-HSA-446203
COPII-mediated vesicle transport	68 targets	R-HSA-204005
Cargo concentration in the ER	33 targets	R-HSA-5694530

Gene Ontology Terms (36)

Functions (6)

Components (23)

Processes (7)

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Items per page:

10

1 – 6 of 6

GO Term	Evidence	Assigned by
AMPA glutamate receptor activity	Inferred from Direct Assay (IDA)	UniProtKB
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
amyloid-beta binding	Inferred from Sequence or structural Similarity (ISS)	ARUK-UCL
PDZ domain binding	Inferred from Sequence or structural Similarity (ISS)	BHF-UCL
glutamate receptor activity	Traceable Author Statement (TAS)	ProtInc
transmitter-gated ion channel activity involved in regulation of postsynaptic membrane potential	Inferred from Electronic Annotation (IEA)	Ensembl

Protein-Protein Interactions (366)

Explore Interacting Targets

1 – 10 of 366

• See Interactions on String-DB

DLG1

Tbio

Novelty: 0.0050926

Score: 0.997

Data Source: STRINGDB

DLG4

Tchem

Novelty: 0.00057285

Score: 0.993

Data Source: STRINGDB

CACNG2

Tbio

Family: IC

Novelty: 0.00808502

Score: 0.992

Data Source: STRINGDB

PICK1

Tbio

Novelty: 0.0058265

Score: 0.981

Data Source: Reactome,STRINGDB

PRKCA

Tchem

Family: Kinase

Novelty: 0.00057611

Score: 0.981

Data Source: STRINGDB

CNIH2

Tbio

Novelty: 0.08676822

Score: 0.981

Data Source: Reactome,STRINGDB

EPB41L1

Tbio

Novelty: 0.02937451

Score: 0.978

Data Source: STRINGDB

GRIP1

Tbio

Novelty: 0.00343871

Score: 0.976

Data Source: Reactome,STRINGDB

CAMK2A

Tchem

Family: Kinase

Novelty: 0.00534906

Score: 0.97

Data Source: Reactome,STRINGDB

GRIA2

Tclin

Family: IC

Novelty: 0.00141257

Score: 0.967

Data Source: Reactome,STRINGDB

Publication Statistics

PubMed Score  2072.47

PubMed score by year

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PubTator Score  599.08

PubTator score by year

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Patents

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Amino Acid Sequence

Residue Counts

Protein Sequence

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Alternative splicing
Cell junction
Cell membrane
Cell projection
Complete proteome
Disulfide bond
Endoplasmic reticulum
Endosome
Glycoprotein
Ion channel

GWAS Trait Find Similar Targets

blood protein measurement
body height
C-reactive protein measurement
grip strength measurement
high density lipoprotein cholesterol measurement
insomnia measurement
schizophrenia
self reported educational attainment
sudden cardiac arrest
visceral adipose tissue measurement

MGI Phenotype Find Similar Targets

behavior/neurological phenotype
growth/size/body region phenotype
hematopoietic system phenotype
homeostasis/metabolism phenotype
integument phenotype
nervous system phenotype