Details of the Target

General Information of Target

Target ID LDTP03973
Target Name Glutamate receptor 2 (GRIA2)
Gene Name GRIA2
Gene ID 2891
Synonyms
GLUR2; Glutamate receptor 2; GluR-2; AMPA-selective glutamate receptor 2; GluR-B; GluR-K2; Glutamate receptor ionotropic, AMPA 2; GluA2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTP
HIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDG
THPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINV
GNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANL
GFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALT
YDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNI
KFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTT
ILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKI
WNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLD
PLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWF
SLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDL
SKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGK
YAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLL
DKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSR
AEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Glutamate-gated ion channel (TC 1.A.10.1) family, GRIA2 subfamily
Subcellular location
Cell membrane
Function
Receptor for glutamate that functions as a ligand-gated ion channel in the central nervous system. It 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. Through complex formation with NSG1, GRIP1 and STX12 controls the intracellular fate of AMPAR and the endosomal sorting of the GRIA2 subunit toward recycling and membrane targeting.
TTD ID
T42392
Uniprot ID
P42262
DrugMap ID
TT9HLZ0
Ensemble ID
ENST00000264426.14
HGNC ID
HGNC:4572
ChEMBL ID
CHEMBL4016

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A375 SNV: p.Q261Ter .
AGS SNV: p.Y265F .
CALU6 SNV: p.A454T .
COLO792 SNV: p.E320K .
GB2 SNV: p.A332E .
HCT116 SNV: p.T707A .
HCT15 SNV: p.I62V .
IPC298 SNV: p.D244N .
LS180 Deletion: p.F552LfsTer8
SNV: p.W692R		 .
MEWO SNV: p.G355S .
NCIH1793 SNV: p.L247V .
NCIH2291 SNV: p.S839P .
NCIH358 SNV: p.L774Q .
NCIH446 SNV: p.G486Ter .
NCIH82 SNV: p.G674C .
RKO SNV: p.I546N .
RL952 SNV: p.T707M .
SW1271 SNV: p.S115R; p.D611H .
SW837 SNV: p.N326I .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
ONAyne
 Probe Info  		K414(4.60)  LDD0275  [1]

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270