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

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: 1513.92   (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: 1513.92   (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

kainic acid

GRIA1Tclin IC

Ki: 5.13

ketamine

GRIA1Tclin IC

OPENER :

perampanel

GRIA1Tclin IC

ANTAGONIST IC50: 6.61

cyclothiazide

GRIA1Tclin IC

EC50: 5.7

Active Ligands (68)

Explore Active Ligands

1 – 10 of 68

CHEMBL1097939,CHEMBL435582

GRIA1Tclin IC

EC50: 5.25

CHEMBL14935

GRIA1Tclin IC

Ki: 5.04

CHEMBL276815

GRIA1Tclin IC

Ki: 7.66

CHEMBL222519

GRIA1Tclin IC

Ki: 5.8

CHEMBL1098240

GRIA1Tclin IC

IC50: 6.46

CHEMBL51660

GRIA1Tclin IC

Ki: 5.96

CHEMBL299180

GRIA1Tclin IC

Ki: 6.16

CHEMBL370941

GRIA1Tclin IC

Ki: 6.84

CHEMBL13378

GRIA1Tclin IC

Ki: 7.66

CHEMBL370038

GRIA1Tclin IC

Ki: 8.28

Pathways (103)

Reactome (22)

KEGG (11)

PathwayCommons (2)

WikiPathways (68)

Activation of AMPA receptors (R-HSA-399710)

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Items per page:

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)

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: 0.00644048

Score: 0.997

Data Source: STRINGDB

DLG4

Tchem

Novelty: 0.00079421

Score: 0.993

Data Source: STRINGDB

CACNG2

Tbio

Family: IC

Novelty: 0.01171137

Score: 0.992

Data Source: STRINGDB

PICK1

Tbio

Novelty: 0.00686801

Score: 0.981

Data Source: Reactome,STRINGDB

PRKCA

Tchem

Family: Kinase

Novelty: 0.00099987

Score: 0.981

Data Source: STRINGDB

CNIH2

Tbio

Novelty: 0.11088352

Score: 0.981

Data Source: Reactome,STRINGDB

EPB41L1

Tbio

Novelty: 0.01521218

Score: 0.978

Data Source: STRINGDB

GRIP1

Tbio

Novelty: 0.00647926

Score: 0.976

Data Source: Reactome,STRINGDB

CAMK2A

Tchem

Family: Kinase

Novelty: 0.01196206

Score: 0.97

Data Source: Reactome,STRINGDB

GRIA2

Tclin

Family: IC

Novelty: 0.00187801

Score: 0.967

Data Source: Reactome,STRINGDB

Publication Statistics

PubMed Score  1513.92

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

Sequence

MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEM

1-70

TYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQDALISIIDHY

70-140

KWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLN

140-210

AILGQIIKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTR

210-280

VDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLT

280-350

GNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYV

350-420

MLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAV

420-490

APLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRF

490-560

SPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSY

560-630

TANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTT

630-700

EEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQ

700-770

GLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMK

770-840

GFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMPLGATGL

840-906

MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQIDIVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQFVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTTTEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDLNKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVMAEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGRRTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYVMLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGELVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIAYGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKWWYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMKGFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMPLGATGL

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Uniprot Keyword

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