Target Information

Target General Infomation
Target ID
T62184
Former ID
TTDR01179
Target Name
Sodium- and chloride-dependent GABA transporter 1
Gene Name
SLC6A1
Synonyms
GABA transporter 1; SLC6A1
Target Type
Successful
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.
BioChemical Class
Neurotransmitter:sodium symporter
Target Validation
T62184
UniProt ID
P30531
Sequence
MATNGSKVADGQISTEVSEAPVANDKPKTLVVKVQKKAADLPDRDTWKGRFDFLMSCVGY
AIGLGNVWRFPYLCGKNGGGAFLIPYFLTLIFAGVPLFLLECSLGQYTSIGGLGVWKLAP
MFKGVGLAAAVLSFWLNIYYIVIISWAIYYLYNSFTTTLPWKQCDNPWNTDRCFSNYSMV
NTTNMTSAVVEFWERNMHQMTDGLDKPGQIRWPLAITLAIAWILVYFCIWKGVGWTGKVV
YFSATYPYIMLIILFFRGVTLPGAKEGILFYITPNFRKLSDSEVWLDAATQIFFSYGLGL
GSLIALGSYNSFHNNVYRDSIIVCCINSCTSMFAGFVIFSIVGFMAHVTKRSIADVAASG
PGLAFLAYPEAVTQLPISPLWAILFFSMLLMLGIDSQFCTVEGFITALVDEYPRLLRNRR
ELFIAAVCIISYLIGLSNITQGGIYVFKLFDYYSASGMSLLFLVFFECVSISWFYGVNRF
YDNIQEMVGSRPCIWWKLCWSFFTPIIVAGVFIFSAVQMTPLTMGNYVFPKWGQGVGWLM
ALSSMVLIPGYMAYMFLTLKGSLKQRIQVMVQPSEDIVRPENGPEQPQAGSSTSKEAYI
Drugs and Mode of Action
Drug(s) Metadoxine Drug Info Approved Myeloma [524626], [531706]
CI-966 Drug Info Phase 1 Convulsions [467852], [533771]
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 524626ClinicalTrials.gov (NCT02051842) Effect of Metadoxine on Oxidative Stress in Non-alcoholic Hepatic Steatosis. U.S. National Institutes of Health.
Ref 531706Preliminary findings on the use of metadoxine for the treatment of alcohol dependence and alcoholic liver disease. Hum Psychopharmacol. 2011 Dec;26(8):554-9.
Ref 533771Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24.
Ref 527271J 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 527297First 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 533404J Med Chem. 1986 Feb;29(2):224-9.Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions.
Ref 533538J 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 533544J Med Chem. 1982 Oct;25(10):1157-62.Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
Ref 533771Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24.
Ref 543977(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: 929).

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