Details of the Target
General Information of Target
| Target ID | LDTP04155 | |||||
|---|---|---|---|---|---|---|
| Target Name | Glutamate receptor 4 (GRIA4) | |||||
| Gene Name | GRIA4 | |||||
| Gene ID | 2893 | |||||
| Synonyms |
GLUR4; Glutamate receptor 4; GluR-4; GluR4; AMPA-selective glutamate receptor 4; GluR-D; Glutamate receptor ionotropic, AMPA 4; GluA4 |
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| 3D Structure | ||||||
| Sequence |
MRIISRQIVLLFSGFWGLAMGAFPSSVQIGGLFIRNTDQEYTAFRLAIFLHNTSPNASEA
PFNLVPHVDNIETANSFAVTNAFCSQYSRGVFAIFGLYDKRSVHTLTSFCSALHISLITP SFPTEGESQFVLQLRPSLRGALLSLLDHYEWNCFVFLYDTDRGYSILQAIMEKAGQNGWH VSAICVENFNDVSYRQLLEELDRRQEKKFVIDCEIERLQNILEQIVSVGKHVKGYHYIIA NLGFKDISLERFIHGGANVTGFQLVDFNTPMVIKLMDRWKKLDQREYPGSETPPKYTSAL TYDGVLVMAETFRSLRRQKIDISRRGNAGDCLANPAAPWGQGIDMERTLKQVRIQGLTGN VQFDHYGRRVNYTMDVFELKSTGPRKVGYWNDMDKLVLIQDVPTLGNDTAAIENRTVVVT TIMESPYVMYKKNHEMFEGNDKYEGYCVDLASEIAKHIGIKYKIAIVPDGKYGARDADTK IWNGMVGELVYGKAEIAIAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFL DPLAYEIWMCIVFAYIGVSVVLFLVSRFSPYEWHTEEPEDGKEGPSDQPPNEFGIFNSLW FSLGAFMQQGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAED LAKQTEIAYGTLDSGSTKEFFRRSKIAVYEKMWTYMRSAEPSVFTRTTAEGVARVRKSKG KFAFLLESTMNEYIEQRKPCDTMKVGGNLDSKGYGVATPKGSSLRTPVNLAVLKLSEAGV LDKLKNKWWYDKGECGPKDSGSKDKTSALSLSNVAGVFYILVGGLGLAMLVALIEFCYKS RAEAKRMKLTFSEAIRNKARLSITGSVGENGRVLTPDCPKAVHTGTAIRQSSGLAVIASD LP |
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| Target Type |
Successful
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| Target Bioclass |
Transporter and channel
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| Family |
Glutamate-gated ion channel (TC 1.A.10.1) family, GRIA4 subfamily
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| Subcellular location |
Cell membrane
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| Function |
Receptor for glutamate that functions as a 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 which is characterized by a delayed accumulation of current flux upon continued application of glutamate.
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| TTD ID | ||||||
| Uniprot ID | ||||||
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Target Site Mutations in Different Cell Lines
Probe(s) Labeling This Target
ABPP Probe
| Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
|---|---|---|---|---|---|
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DBIA Probe Info |
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C878(2.24) | LDD2469 | [1] | |
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IA-alkyne Probe Info |
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C878(0.42) | LDD2182 | [2] | |
Competitor(s) Related to This Target
| Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
|---|---|---|---|---|---|
| LDCM0625 | F8 | Ramos | C878(0.39) | LDD2187 | [2] |
| LDCM0576 | Fragment14 | Ramos | C878(0.73) | LDD2193 | [2] |
| LDCM0566 | Fragment4 | Ramos | C878(0.39) | LDD2184 | [2] |
| LDCM0569 | Fragment7 | Ramos | C878(0.47) | LDD2186 | [2] |
| LDCM0022 | KB02 | Ramos | C878(0.42) | LDD2182 | [2] |
| LDCM0023 | KB03 | Ramos | C878(0.06) | LDD2183 | [2] |
| LDCM0024 | KB05 | MGG123 | C878(2.42) | LDD3303 | [1] |
References