Target Information
Target General Infomation | |||||
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Target ID |
T73495
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Former ID |
TTDS00122
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Target Name |
Glutamate receptor, ionotropic kainate 1
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Gene Name |
GRIK1
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Synonyms |
EAA3; Excitatory amino acid receptor 3; GluR-5; GluR5; GluR5 kainate receptor; Glutamate receptor 5; GRIK1
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Target Type |
Successful
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Disease | Convulsions [ICD9: 780.3; ICD10: R56.0] | ||||
Epilepsy; Neuropathic pain [ICD9:356.0, 356.8; ICD10: G40, G64, G90.0] | |||||
Epilepsy; Alcohol use disorders [ICD9:303; ICD10: G40, F10.2] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Function |
Ionotropic glutamate receptor. 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 tothe 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. May be involved in the transmission of light information from the retina to the hypothalamus.
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BioChemical Class |
Glutamate-gated ion channel
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Target Validation |
T73495
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UniProt ID | |||||
Sequence |
MEHGTLLAQPGLWTRDTSWALLYFLCYILPQTAPQVLRIGGIFETVENEPVNVEELAFKF
AVTSINRNRTLMPNTTLTYDIQRINLFDSFEASRRACDQLALGVAALFGPSHSSSVSAVQ SICNALEVPHIQTRWKHPSVDNKDLFYINLYPDYAAISRAILDLVLYYNWKTVTVVYEDS TGLIRLQELIKAPSRYNIKIKIRQLPSGNKDAKPLLKEMKKGKEFYVIFDCSHETAAEIL KQILFMGMMTEYYHYFFTTLDLFALDLELYRYSGVNMTGFRLLNIDNPHVSSIIEKWSME RLQAPPRPETGLLDGMMTTEAALMYDAVYMVAIASHRASQLTVSSLQCHRHKPWRLGPRF MNLIKEARWDGLTGHITFNKTNGLRKDFDLDIISLKEEGTEKAAGEVSKHLYKVWKKIGI WNSNSGLNMTDSNKDKSSNITDSLANRTLIVTTILEEPYVMYRKSDKPLYGNDRFEGYCL DLLKELSNILGFIYDVKLVPDGKYGAQNDKGEWNGMVKELIDHRADLAVAPLTITYVREK VIDFSKPFMTLGISILYRKPNGTNPGVFSFLNPLSPDIWMYVLLACLGVSCVLFVIARFT PYEWYNPHPCNPDSDVVENNFTLLNSFWFGVGALMQQGSELMPKALSTRIVGGIWWFFTL IIISSYTANLAAFLTVERMESPIDSADDLAKQTKIEYGAVRDGSTMTFFKKSKISTYEKM WAFMSSRQQTALVRNSDEGIQRVLTTDYALLMESTSIEYVTQRNCNLTQIGGLIDSKGYG VGTPIGSPYRDKITIAILQLQEEGKLHMMKEKWWRGNGCPEEDNKEASALGVENIGGIFI VLAAGLVLSVFVAIGEFIYKSRKNNDIEQAFCFFYGLQCKQTHPTNSTSGTTLSTDLECG KLIREERGIRKQSSVHTV |
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Drugs and Mode of Action | |||||
Drug(s) | Topiramate | Drug Info | Approved | Epilepsy; Alcohol use disorders | [536756], [541929], [551871] |
LY293558 | Drug Info | Phase 2 | Pain | [467580], [531212] | |
NS 1209 | Drug Info | Phase 2 | Epilepsy; Neuropathic pain | [530030], [536498] | |
NBQX | Drug Info | Phase 1 | Neurological disease | [467600] | |
YM-90K | Drug Info | Discontinued in Phase 2 | Convulsions | [545107] | |
Inhibitor | (2S,4R)-4-(3-Methoxy-3-oxopropyl)glutamic Acid | Drug Info | [529560] | ||
(R,S)-AMPA | Drug Info | [529714] | |||
2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid | Drug Info | [527354] | |||
2-(3-bromobenzoylamino)-4-chlorobenzoic acid | Drug Info | [527354] | |||
2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) | Drug Info | [530863] | |||
2S,4R-4-METHYLGLUTAMATE | Drug Info | [529560] | |||
DIHYDROKAINATE | Drug Info | [529559] | |||
DNQX | Drug Info | [534261] | |||
Domoric acid | Drug Info | [529560] | |||
GLUTAMATE | Drug Info | [530863] | |||
KAINATE | Drug Info | [529560] | |||
NBQX | Drug Info | [525786] | |||
QUISQUALATE | Drug Info | [529560] | |||
S-ATPO | Drug Info | [530297] | |||
TQX-173 | Drug Info | [526134] | |||
UBP-302 | Drug Info | [528453] | |||
YM-90K | Drug Info | [525786] | |||
Agonist | (S)-4-AHCP | Drug Info | [543831] | ||
(S)-5-iodowillardiine | Drug Info | [543831] | |||
8-deoxy-neodysiherbaine | Drug Info | [543831] | |||
ATPA | Drug Info | [543831] | |||
domoic acid | Drug Info | [543831] | |||
dysiherbaine | Drug Info | [543831] | |||
LY339434 | Drug Info | [543831] | |||
SYM2081 | Drug Info | [543831] | |||
[3H](2S,4R)-4-methylglutamate | Drug Info | [543831] | |||
[3H]kainate | Drug Info | [543831] | |||
Antagonist | 2,4-epi-neodysiherbaine | Drug Info | [543831] | ||
ACET | Drug Info | [543831] | |||
LY382884 | Drug Info | [543831] | |||
LY466195 | Drug Info | [543831] | |||
MSVIII-19 | Drug Info | [543831] | |||
NS3763 | Drug Info | [543831] | |||
Topiramate | Drug Info | [536096] | |||
UBP310 | Drug Info | [543831] | |||
[3H]UBP310 | Drug Info | [531158] | |||
Modulator | LY293558 | Drug Info | [531212] | ||
NS 1209 | Drug Info | [530030] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Glutamatergic synapse | |||||
PANTHER Pathway | Huntington disease | ||||
Ionotropic glutamate receptor pathway | |||||
Metabotropic glutamate receptor group III pathway | |||||
Metabotropic glutamate receptor group I pathway | |||||
WikiPathways | Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | ||||
References | |||||
Ref 467580 | (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: 4245). | ||||
Ref 467600 | (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: 4264). | ||||
Ref 530030 | The efficacy of the AMPA receptor antagonist NS1209 and lidocaine in nerve injury pain: a randomized, double-blind, placebo-controlled, three-way crossover study. Anesth Analg. 2009 Apr;108(4):1311-9. | ||||
Ref 536756 | Use of second-generation antiepileptic drugs in the pediatric population. Paediatr Drugs. 2008;10(4):217-54. | ||||
Ref 541929 | (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: 6849). | ||||
Ref 525786 | Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with in vivo activity. | ||||
Ref 526134 | J Med Chem. 2001 Sep 13;44(19):3157-65.Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173. | ||||
Ref 527354 | J Med Chem. 2004 Dec 30;47(27):6948-57.Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5. | ||||
Ref 528453 | J Med Chem. 2006 Oct 5;49(20):6015-26.Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies. | ||||
Ref 529559 | J Med Chem. 2008 Jul 24;51(14):4085-92. Epub 2008 Jun 25.Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2. | ||||
Ref 529560 | J Med Chem. 2008 Jul 24;51(14):4093-103. Epub 2008 Jun 25.Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation ofionotropic glutamate receptor subtypes 5, 6, and 7. | ||||
Ref 529714 | J Med Chem. 2008 Oct 23;51(20):6614-8. Epub 2008 Sep 24.1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators. | ||||
Ref 530030 | The efficacy of the AMPA receptor antagonist NS1209 and lidocaine in nerve injury pain: a randomized, double-blind, placebo-controlled, three-way crossover study. Anesth Analg. 2009 Apr;108(4):1311-9. | ||||
Ref 530297 | Bioorg Med Chem. 2009 Sep 1;17(17):6390-401. Epub 2009 Jul 16.3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands. | ||||
Ref 530863 | J Med Chem. 2010 May 27;53(10):4110-8.4-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. | ||||
Ref 531158 | Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310. Mol Pharmacol. 2010 Dec;78(6):1036-45. | ||||
Ref 534261 | J Med Chem. 1996 Oct 25;39(22):4430-8.Synthesis of chiral 1-(2'-amino-2'-carboxyethyl)-1,4-dihydro-6,7-quinoxaline-2,3-diones: alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor agonists and antagonists. |
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