Target General Infomation
Target ID
T42392 (Former ID: TTDI01970)
Target Name
Glutamate receptor AMPA 2 (GRIA2)
Synonyms
Glutamate receptor ionotropic, AMPA 2; Glutamate receptor 2; GluRK2; GluRB; GluR2; GluR-K2; GluR-B; GluR-2; GluA2; AMPAselective glutamate receptor 2; AMPA-selective glutamate receptor 2
Gene Name
GRIA2
Target Type
Successful target
[1]
Disease [+] 1 Target-related Diseases +
1 Neuropathy [ICD-11: 8C0Z]
Function
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. Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission.
BioChemical Class
Glutamate-gated ion channel
UniProt ID
GRIA2_HUMAN
Sequence
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTP
HIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDG
THPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINV
GNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANL
GFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALT
YDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNI
KFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTT
ILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKI
WNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLD
PLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWF
SLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDL
SKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGK
YAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLL
DKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSR
AEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
Drugs and Modes of Action
Approved Drug(s) [+] 1 Approved Drugs +
1 E-2007 Drug Info Approved Diabetic neuropathy [2], [3]
Clinical Trial Drug(s) [+] 1 Clinical Trial Drugs +
1 Paliroden Drug Info Phase 2 Parkinson disease [4]
Mode of Action [+] 4 Modes of Action +
Inhibitor [+] 1 Inhibitor drugs +
1 E-2007 Drug Info [1]
Modulator [+] 1 Modulator drugs +
1 Paliroden Drug Info [5]
Agonist [+] 3 Agonist drugs +
1 (R,S)-AMPA Drug Info [6]
2 (S)-5-fluorowillardiine Drug Info [6]
3 [3H]AMPA Drug Info [6]
Antagonist [+] 2 Antagonist drugs +
1 ATPO Drug Info [6]
2 [3H]CNQX Drug Info [6]
Target Regulators
Target-regulating microRNAs
Target-interacting Proteins
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
NetPath Pathway [+] 1 NetPath Pathways +
1 IL2 Signaling Pathway
Panther Pathway [+] 2 Panther Pathways +
1 Ionotropic glutamate receptor pathway
2 Metabotropic glutamate receptor group III pathway
PID Pathway [+] 1 PID Pathways +
1 N-cadherin signaling events
References
REF 1 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
REF 2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7050).
REF 3 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 4 ClinicalTrials.gov (NCT00285025) Study of the Effect of SR57667B in Patients With Alzheimer's Disease. U.S. National Institutes of Health.
REF 5 Mechanism of inhibition of the GluA2 AMPA receptor channel opening by talampanel and its enantiomer: the stereochemistry of the 4-methyl group on the diazepine ring of 2,3-benzodiazepine derivatives.ACS Chem Neurosci.2013 Apr 17;4(4):635-44.
REF 6 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 445).

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