Target Information
Target General Infomation | |||||
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Target ID |
T62184
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Former ID |
TTDR01179
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Target Name |
Sodium- and chloride-dependent GABA transporter 1
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Gene Name |
SLC6A1
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Synonyms |
GABA transporter 1; SLC6A1
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Target Type |
Successful
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Disease | Convulsions [ICD9: 780.3; ICD10: R56.0] | ||||
Myeloma [ICD9: 203; ICD10: C90] | |||||
Function |
Terminates the action of GABA by its high affinity sodium-dependent reuptake into presynaptic terminals.
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BioChemical Class |
Neurotransmitter:sodium symporter
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Target Validation |
T62184
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UniProt ID | |||||
Sequence |
MATNGSKVADGQISTEVSEAPVANDKPKTLVVKVQKKAADLPDRDTWKGRFDFLMSCVGY
AIGLGNVWRFPYLCGKNGGGAFLIPYFLTLIFAGVPLFLLECSLGQYTSIGGLGVWKLAP MFKGVGLAAAVLSFWLNIYYIVIISWAIYYLYNSFTTTLPWKQCDNPWNTDRCFSNYSMV NTTNMTSAVVEFWERNMHQMTDGLDKPGQIRWPLAITLAIAWILVYFCIWKGVGWTGKVV YFSATYPYIMLIILFFRGVTLPGAKEGILFYITPNFRKLSDSEVWLDAATQIFFSYGLGL GSLIALGSYNSFHNNVYRDSIIVCCINSCTSMFAGFVIFSIVGFMAHVTKRSIADVAASG PGLAFLAYPEAVTQLPISPLWAILFFSMLLMLGIDSQFCTVEGFITALVDEYPRLLRNRR ELFIAAVCIISYLIGLSNITQGGIYVFKLFDYYSASGMSLLFLVFFECVSISWFYGVNRF YDNIQEMVGSRPCIWWKLCWSFFTPIIVAGVFIFSAVQMTPLTMGNYVFPKWGQGVGWLM ALSSMVLIPGYMAYMFLTLKGSLKQRIQVMVQPSEDIVRPENGPEQPQAGSSTSKEAYI |
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Drugs and Mode of Action | |||||
Inhibitor | (R)-EF-1520 | Drug Info | [543977] | ||
(R)-Piperidine-3-carboxylic acid | Drug Info | [527271] | |||
(R/S) EF-1500 | Drug Info | [543977] | |||
(S)-EF-1520 | Drug Info | [543977] | |||
(S)-Piperidine-3-carboxylic acid | Drug Info | [527271] | |||
2,4-Diamino-butyric acid(GABA) | Drug Info | [533404] | |||
4-Hydroxy-piperidine-3-carboxylic acid | Drug Info | [533544] | |||
GAMMA-AMINO-BUTANOIC ACID | Drug Info | [527271] | |||
LU32-176B | Drug Info | [527297] | |||
NIPECOTIC ACID | Drug Info | [533538] | |||
SKF89976A | Drug Info | [543977] | |||
[3H]tiagabine | Drug Info | [543977] | |||
Modulator | CI-966 | Drug Info | [533771] | ||
Metadoxine | Drug Info | ||||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | GABAergic synapse | ||||
Reactome | Na+/Cl- dependent neurotransmitter transporters | ||||
WikiPathways | Monoamine Transport | ||||
NRF2 pathway | |||||
References | |||||
Ref 467852 | (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: 4612). | ||||
Ref 524626 | ClinicalTrials.gov (NCT02051842) Effect of Metadoxine on Oxidative Stress in Non-alcoholic Hepatic Steatosis. U.S. National Institutes of Health. | ||||
Ref 527271 | J Med Chem. 2004 Nov 4;47(23):5620-9.Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling. | ||||
Ref 527297 | First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J Pharmacol Exp Ther. 2005 Feb;312(2):866-74. Epub 2004 Nov 18. | ||||
Ref 533404 | J Med Chem. 1986 Feb;29(2):224-9.Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions. | ||||
Ref 533538 | J Med Chem. 1981 Jul;24(7):788-94.Epimeric cis-decahydroquinoline-5-carboxylic acids: effects on gamma-aminobutyric acid uptake and receptor binding in vitro. | ||||
Ref 533544 | J Med Chem. 1982 Oct;25(10):1157-62.Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors. |
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