Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0U2VJ)
Name
Glutamate receptor AMPA 2 (GRIA2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
AMPA-selective glutamate receptor 2; AMPAselective glutamate receptor 2; GluA2; GluR-2; GluR-B; GluR-K2; GluR2; GluRB; GluRK2; Glutamate receptor 2; Glutamate receptor ionotropic, AMPA 2
Family Transmembrane channel/porin (TC/P)  >>  Glutamate-gated ion channel (GIC)
Organism
Homo sapiens (Human)
Gene Name GRIA2 Gene ID
2891
UniProt ID GRIA2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T42392 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MQKIMHISVLLSPVLWGLIFGVSSNSIQIGGLFPRGADQEYSAFRVGMVQFSTSEFRLTP
HIDNLEVANSFAVTNAFCSQFSRGVYAIFGFYDKKSVNTITSFCGTLHVSFITPSFPTDG
THPFVIQMRPDLKGALLSLIEYYQWDKFAYLYDSDRGLSTLQAVLDSAAEKKWQVTAINV
GNINNDKKDEMYRSLFQDLELKKERRVILDCERDKVNDIVDQVITIGKHVKGYHYIIANL
GFTDGDLLKIQFGGANVSGFQIVDYDDSLVSKFIERWSTLEEKEYPGAHTTTIKYTSALT
YDAVQVMTEAFRNLRKQRIEISRRGNAGDCLANPAVPWGQGVEIERALKQVQVEGLSGNI
KFDQNGKRINYTINIMELKTNGPRKIGYWSEVDKMVVTLTELPSGNDTSGLENKTVVVTT
ILESPYVMMKKNHEMLEGNERYEGYCVDLAAEIAKHCGFKYKLTIVGDGKYGARDADTKI
WNGMVGELVYGKADIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLD
PLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEFEDGRETQSSESTNEFGIFNSLWF
SLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDL
SKQTEIAYGTLDSGSTKEFFRRSKIAVFDKMWTYMRSAEPSVFVRTTAEGVARVRKSKGK
YAYLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSSLRNAVNLAVLKLNEQGLL
DKLKNKWWYDKGECGSGGGDSKEKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKSR
AEAKRMKVAKNAQNINPSSSQNSQNFATYKEGYNVYGIESVKI
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.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Glutamic acid hydrochloride Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Acidulant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 940 nM (estimated based on the structural similarity with CHEMBL575060 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRIA2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 280 nM (estimated based on the structural similarity with CHEMBL575060 ) [2]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID GRIA2_RAT
          DIG Name: Monosodium glutamate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent; Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 2190 nM (estimated based on the structural similarity with CHEMBL575060 ) [3]
                   Structural Similarity Tanimoto coefficient = 0.979166667
                   Tested Species Homo sapiens (Human)
                   UniProt ID GRIA2_HUMAN
References
1 Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J Med Chem. 1997 Oct 24; 40(22):3645-50.
2 4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues. J Med Chem. 2010 May 27; 53(10):4110-8.
3 Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands. Bioorg Med Chem. 2010 Feb 15; 18(4):1381-7.

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