Target Information

Target General Infomation
Target ID
T42392
Former ID
TTDI01970
Target Name
Glutamate receptor 2
Gene Name
GRIA2
Synonyms
AMPAselective glutamate receptor 2; GluA2; GluR2; GluRB; GluRK2; Glutamate receptor ionotropic, AMPA 2; GRIA2
Target Type
Clinical Trial
Disease Parkinson's disease [ICD9: 332; ICD10: G20]
Function
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 whichis characterized by a delayed accumulation of current flux upon continued application of glutamate.
BioChemical Class
Glutamate-gated ion channel
UniProt ID
P42262
Sequence
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTP
HIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDG
THPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINV
GNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANL
GFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALT
YDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNI
KFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTT
ILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKI
WNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLD
PLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWF
SLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDL
SKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGK
YAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLL
DKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSR
AEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
Drugs and Mode of Action
Drug(s) Paliroden Drug Info Phase 2 Parkinson's disease [521794]
Agonist (S)-5-fluorowillardiine Drug Info [543828]
AMPA Drug Info [543828]
[3H]AMPA Drug Info [543828]
Antagonist ATPO Drug Info [543828]
[3H]CNQX Drug Info [543828]
Modulator Paliroden Drug Info
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Ionotropic glutamate receptor pathway
Metabotropic glutamate receptor group III pathway
Pathway Interaction Database N-cadherin signaling events
References
Ref 521794ClinicalTrials.gov (NCT00285025) Study of the Effect of SR57667B in Patients With Alzheimer's Disease. U.S. National Institutes of Health.
Ref 543828(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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