Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTPJR0G)

DTT Name Glutamate receptor AMPA 4 (GRIA4)
Synonyms Glutamate receptor ionotropic, AMPA 4; GluRD; GluR4; GluA4; GRIA4; AMPAselective glutamate receptor 4
Gene Name GRIA4
DTT Type
Successful target
 [1]
BioChemical Class
Glutamate-gated ion channel
UniProt ID
GRIA4_HUMAN
TTD ID
T96235
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRIISRQIVLLFSGFWGLAMGAFPSSVQIGGLFIRNTDQEYTAFRLAIFLHNTSPNASEA
PFNLVPHVDNIETANSFAVTNAFCSQYSRGVFAIFGLYDKRSVHTLTSFCSALHISLITP
SFPTEGESQFVLQLRPSLRGALLSLLDHYEWNCFVFLYDTDRGYSILQAIMEKAGQNGWH
VSAICVENFNDVSYRQLLEELDRRQEKKFVIDCEIERLQNILEQIVSVGKHVKGYHYIIA
NLGFKDISLERFIHGGANVTGFQLVDFNTPMVIKLMDRWKKLDQREYPGSETPPKYTSAL
TYDGVLVMAETFRSLRRQKIDISRRGNAGDCLANPAAPWGQGIDMERTLKQVRIQGLTGN
VQFDHYGRRVNYTMDVFELKSTGPRKVGYWNDMDKLVLIQDVPTLGNDTAAIENRTVVVT
TIMESPYVMYKKNHEMFEGNDKYEGYCVDLASEIAKHIGIKYKIAIVPDGKYGARDADTK
IWNGMVGELVYGKAEIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFL
DPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEPEDGKEGPSDQPPNEFGIFNSLW
FSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAED
LAKQTEIAYGTLDSGSTKEFFRRSKIAVYEKMWTYMRSAEPSVFTRTTAEGVARVRKSKG
KFAFLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGVATPKGSSLRTPVNLAVLKLSEAGV
LDKLKNKWWYDKGECGPKDSGSKDKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKS
RAEAKRMKLTFSEAIRNKARLSITGSVGENGRVLTPDCPKAVHTGTAIRQSSGLAVIASD
LP
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 centralnervous 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.
KEGG Pathway
cAMP signaling pathway (hsa04024 )
Neuroactive ligand-receptor interaction (hsa04080 )
Circadian entrainment (hsa04713 )
Retrograde endocannabinoid signaling (hsa04723 )
Glutamatergic synapse (hsa04724 )
Dopaminergic synapse (hsa04728 )
Amphetamine addiction (hsa05031 )
Nicotine addiction (hsa05033 )
Reactome Pathway
Trafficking of GluR2-containing AMPA receptors (R-HSA-416993 )
Unblocking of NMDA receptor, glutamate binding and activation (R-HSA-438066 )
Trafficking of AMPA receptors (R-HSA-399719 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
E-2007 DMJDYNQ Diabetic neuropathy 8C0Z Approved [1]
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6 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(S)-5-fluorowillardiine DMCIZ7P Discovery agent N.A. Investigative [2]
AMG-889436 DMKP8L9 Parkinson disease 8A00.0 Investigative [2]
ATPO DMXLS78 Discovery agent N.A. Investigative [2]
joro toxin DMYBJ4K Discovery agent N.A. Investigative [2]
[3H]AMPA DMLF7SG N. A. N. A. Investigative [2]
[3H]CNQX DMIFKUX Discovery agent N.A. Investigative [2]
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⏷ Show the Full List of 6 Investigative Drug(s)

References

1 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
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. (Target id: 447).