Details of the Drug Transporter (DTP)

General Information of Drug Transporter (DTP) (ID: DT8Z563)

DTP Name Sodium- and chloride-dependent GABA transporter 1 (SLC6A1)
Gene Name SLC6A1
UniProt ID
P30531 (SC6A1_HUMAN)
VARIDT ID
DTD0440
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Synonyms Solute carrier family 6 member 1; GAT-1; SLC6A1; GABATR; GABT1; GAT1
DTP Family Neurotransmitter:Sodium Symporter (NSS) Family ;
Sequence
MATNGSKVADGQISTEVSEAPVANDKPKTLVVKVQKKAADLPDRDTWKGRFDFLMSCVGY
AIGLGNVWRFPYLCGKNGGGAFLIPYFLTLIFAGVPLFLLECSLGQYTSIGGLGVWKLAP
MFKGVGLAAAVLSFWLNIYYIVIISWAIYYLYNSFTTTLPWKQCDNPWNTDRCFSNYSMV
NTTNMTSAVVEFWERNMHQMTDGLDKPGQIRWPLAITLAIAWILVYFCIWKGVGWTGKVV
YFSATYPYIMLIILFFRGVTLPGAKEGILFYITPNFRKLSDSEVWLDAATQIFFSYGLGL
GSLIALGSYNSFHNNVYRDSIIVCCINSCTSMFAGFVIFSIVGFMAHVTKRSIADVAASG
PGLAFLAYPEAVTQLPISPLWAILFFSMLLMLGIDSQFCTVEGFITALVDEYPRLLRNRR
ELFIAAVCIISYLIGLSNITQGGIYVFKLFDYYSASGMSLLFLVFFECVSISWFYGVNRF
YDNIQEMVGSRPCIWWKLCWSFFTPIIVAGVFIFSAVQMTPLTMGNYVFPKWGQGVGWLM
ALSSMVLIPGYMAYMFLTLKGSLKQRIQVMVQPSEDIVRPENGPEQPQAGSSTSKEAYI
Function This transporter has high affinity sodium-dependent of GABA.
TCDB ID
2.A.22.3.2
Gene ID
6529
KEGG Pathway
Synaptic vesicle cycle (hsa04721 )
GABAergic synapse (hsa04727 )
Reactome Pathway
Reuptake of GABA (R-HSA-888593 )
Na+/Cl- dependent neurotransmitter transporters (R-HSA-442660 )

Molecular Interaction Atlas (MIA) of This DTP

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTP
1 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
GSK683699 DMTW79H Inflammatory bowel disease DD72 Phase 2 [9]
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Molecular Expression Atlas (MEA) of This DTP

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTP
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 8.85E-02 5.66E-04 4.38E-03
Adrenocortical carcinoma 2D11.Z Kidney 3.12E-01 -2.38E-02 -5.94E-02
Alopecia ED70 Skin from scalp 3.47E-01 -2.20E-01 -3.73E-01
Alzheimer's disease 8A20 Entorhinal cortex 7.12E-02 -1.09E-01 -2.65E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 8.17E-01 6.64E-04 5.12E-03
Aortic stenosis BB70 Calcified aortic valve 6.44E-02 -5.31E-01 -7.53E-01
Apnea 7A40 Hyperplastic tonsil 3.06E-01 3.35E-01 1.11E+00
Arthropathy FA00-FA5Z Peripheral blood 1.37E-01 -2.40E-02 -1.54E-01
Asthma CA23 Nasal and bronchial airway 9.90E-01 -1.45E-02 -3.34E-02
Atopic dermatitis EA80 Skin 5.55E-03 2.46E-01 8.54E-01
Autism 6A02 Whole blood 4.85E-01 1.90E-02 1.63E-01
Autoimmune uveitis 9A96 Peripheral monocyte 1.32E-01 -1.82E-01 -1.34E+00
Autosomal dominant monocytopenia 4B04 Whole blood 9.22E-01 3.60E-02 3.03E-01
Bacterial infection of gingival 1C1H Gingival tissue 2.76E-06 1.30E-01 7.18E-01
Batten disease 5C56.1 Whole blood 5.52E-01 5.01E-02 6.15E-01
Behcet's disease 4A62 Peripheral blood 6.45E-01 4.64E-03 1.62E-02
Bipolar disorder 6A60-6A6Z Prefrontal cortex 2.34E-01 1.08E-01 4.74E-01
Bladder cancer 2C94 Bladder tissue 1.29E-03 4.88E-01 2.15E+00
Breast cancer 2C60-2C6Z Breast tissue 8.62E-25 1.41E-01 5.37E-01
Cardioembolic stroke 8B11.20 Whole blood 4.75E-01 1.15E-02 8.89E-02
Cervical cancer 2C77 Cervical tissue 8.54E-01 6.03E-02 1.75E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 1.81E-01 3.15E-02 3.35E-01
Chronic hepatitis C 1E51.1 Whole blood 7.70E-01 -8.72E-03 -1.40E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 4.84E-01 -2.91E-02 -7.54E-02
Chronic obstructive pulmonary disease CA22 Small airway epithelium 5.25E-03 -6.70E-02 -2.40E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 6.74E-02 1.52E-01 7.77E-01
Colon cancer 2B90 Colon tissue 5.76E-16 1.12E-01 5.59E-01
Coronary artery disease BA80-BA8Z Peripheral blood 1.27E-01 -1.17E-01 -8.99E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 9.46E-01 5.81E-02 2.80E-01
Endometriosis GA10 Endometrium tissue 3.56E-02 9.66E-02 4.22E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 4.08E-01 -6.16E-02 -4.44E-01
Familial hypercholesterolemia 5C80.00 Whole blood 6.45E-02 -6.85E-02 -4.68E-01
Gastric cancer 2B72 Gastric tissue 4.15E-01 -5.43E-02 -3.75E-01
Glioblastopma 2A00.00 Nervous tissue 1.67E-75 -1.19E+00 -1.33E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 1.71E-01 -1.25E+00 -7.20E-01
Head and neck cancer 2D42 Head and neck tissue 5.57E-05 -1.97E-01 -2.46E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 4.79E-01 -2.11E-01 -3.37E-01
Huntington's disease 8A01.10 Whole blood 4.31E-01 -1.71E-02 -1.15E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 1.80E-04 1.17E+00 3.75E+00
Immunodeficiency 4A00-4A20 Peripheral blood 5.66E-01 -8.02E-03 -1.09E-01
Influenza 1.00E+30 Whole blood 5.89E-01 1.79E-02 3.49E-01
Interstitial cystitis GC00.3 Bladder tissue 1.03E-02 6.93E-01 3.52E+00
Intracranial aneurysm 8B01.0 Intracranial artery 5.88E-02 1.11E+00 1.63E+00
Irritable bowel syndrome DD91.0 Rectal colon tissue 8.49E-01 -1.02E-02 -2.61E-02
Ischemic stroke 8B11 Peripheral blood 5.10E-01 -1.37E-02 -8.62E-02
Juvenile idiopathic arthritis FA24 Peripheral blood 4.22E-02 1.26E-02 8.69E-02
Lateral sclerosis 8B60.4 Cervical spinal cord 1.21E-01 -9.01E-01 -7.31E-01
Lateral sclerosis 8B60.4 Skin 2.20E-01 1.20E-01 5.68E-01
Liver cancer 2C12.0 Liver tissue 1.54E-05 -2.39E-01 -2.48E-01
Liver failure DB99.7-DB99.8 Liver tissue 2.52E-09 -4.70E+00 -8.98E+00
Lung cancer 2C25 Lung tissue 5.79E-02 -1.72E-01 -3.66E-01
Lupus erythematosus 4A40 Whole blood 1.78E-02 -5.82E-02 -2.20E-01
Major depressive disorder 6A70-6A7Z Whole blood 1.72E-01 1.56E-02 8.80E-02
Major depressive disorder 6A70-6A7Z Hippocampus 5.31E-01 -3.03E-02 -1.38E-01
Melanoma 2C30 Skin 3.88E-01 -9.72E-02 -1.16E-01
Multiple myeloma 2A83.1 Bone marrow 4.99E-02 -2.37E-01 -6.24E-01
Multiple myeloma 2A83.1 Peripheral blood 5.23E-01 4.77E-02 5.53E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 1.90E-01 1.03E-01 4.90E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 2.77E-01 -4.78E-02 -2.91E-01
Myelofibrosis 2A20.2 Whole blood 2.29E-02 1.44E-01 1.32E+00
Myocardial infarction BA41-BA50 Peripheral blood 1.84E-01 5.31E-02 1.75E-01
Myopathy 8C70.6 Muscle tissue 1.37E-02 -6.10E-01 -1.71E+00
Neonatal sepsis KA60 Whole blood 3.53E-01 4.24E-02 2.95E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 2.71E-16 -1.95E+00 -6.29E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 5.32E-01 1.03E-01 1.86E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 5.29E-01 4.92E-02 1.79E-01
Olive pollen allergy CA08.00 Peripheral blood 7.01E-01 -2.94E-02 -3.16E-01
Oral cancer 2B6E Oral tissue 6.97E-02 -1.94E-01 -2.85E-01
Osteoarthritis FA00-FA0Z Synovial tissue 8.56E-01 3.95E-01 5.49E-01
Osteoporosis FB83.1 Bone marrow 4.92E-01 7.07E-02 9.54E-01
Ovarian cancer 2C73 Ovarian tissue 4.50E-01 -5.20E-02 -9.44E-02
Pancreatic cancer 2C10 Pancreas 7.61E-05 4.34E-01 1.18E+00
Parkinson's disease 8A00.0 Substantia nigra tissue 1.74E-02 -3.29E-01 -1.16E+00
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 2.19E-01 -6.15E-02 -4.83E-01
Pituitary cancer 2D12 Pituitary tissue 5.54E-01 1.51E-01 4.69E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 9.23E-02 5.45E-01 1.34E+00
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 1.61E-01 -1.89E-03 -5.12E-03
Polycythemia vera 2A20.4 Whole blood 7.23E-05 6.76E-02 6.87E-01
Pompe disease 5C51.3 Biceps muscle 7.96E-03 -4.52E-01 -1.60E+00
Preterm birth KA21.4Z Myometrium 8.11E-01 4.44E-02 1.37E-01
Prostate cancer 2C82 Prostate 9.13E-01 3.58E-01 3.41E-01
Psoriasis EA90 Skin 8.52E-18 4.01E-01 8.23E-01
Rectal cancer 2B92 Rectal colon tissue 1.81E-02 1.87E-01 9.20E-01
Renal cancer 2C90-2C91 Kidney 4.02E-04 4.96E-01 1.16E+00
Retinoblastoma 2D02.2 Uvea 9.74E-08 -5.10E+00 -1.55E+01
Rheumatoid arthritis FA20 Synovial tissue 3.19E-01 -2.79E-01 -4.96E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 4.25E-01 -3.77E-02 -3.40E-01
Schizophrenia 6A20 Prefrontal cortex 9.75E-02 -1.80E-01 -5.84E-02
Schizophrenia 6A20 Superior temporal cortex 2.19E-01 -7.27E-02 -3.24E-01
Scleroderma 4A42.Z Whole blood 8.46E-01 2.13E-02 1.24E-01
Seizure 8A60-8A6Z Whole blood 3.56E-01 -7.83E-02 -4.06E-01
Sensitive skin EK0Z Skin 1.70E-01 -5.64E-03 -5.00E-02
Sepsis with septic shock 1G41 Whole blood 8.41E-03 7.60E-02 4.35E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 1.39E-01 1.28E-01 1.04E+00
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 6.65E-01 4.92E-02 4.23E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 2.46E-01 5.93E-02 3.08E+00
Sjogren's syndrome 4A43.2 Salivary gland tissue 5.66E-01 -6.30E-02 -6.36E-01
Skin cancer 2C30-2C3Z Skin 5.91E-06 2.00E-01 3.86E-01
Thrombocythemia 3B63 Whole blood 2.38E-03 1.89E-01 1.75E+00
Thrombocytopenia 3B64 Whole blood 5.63E-01 4.98E-02 1.83E-01
Thyroid cancer 2D10 Thyroid 1.04E-17 5.12E-01 9.38E-01
Tibial muscular dystrophy 8C75 Muscle tissue 1.02E-01 1.83E-01 3.96E-01
Tuberous sclerosis complex LD2D.2 Perituberal tissue 2.30E-01 -4.12E-01 -3.85E+00
Type 2 diabetes 5A11 Liver tissue 6.65E-01 2.07E-01 5.99E-01
Ureter cancer 2C92 Urothelium 8.80E-02 -7.98E-02 -4.98E-01
Uterine cancer 2C78 Endometrium tissue 8.33E-03 1.55E-01 2.93E-01
Vitiligo ED63.0 Skin 1.91E-01 -5.85E-01 -7.21E-01
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⏷ Show the Full List of Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DTP

DTP DTT Name GABA transporter GAT-1 (SLC6A1) DTT Info
DTP DTT Type Successful
2 Approved Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metadoxine DMM4QOJ Multiple myeloma 2A83 Approved [1]
Tiagabine DMKSQG0 Epilepsy 8A60-8A68 Approved [2]
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2 Clinical Trial Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
GSK683699 DMTW79H Inflammatory bowel disease DD72 Phase 2 [3]
CI-966 DM8T2KA Convulsion 8A68.Z Phase 1 [4]
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10 Investigative Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(R)-EF-1520 DM297MU Discovery agent N.A. Investigative [2]
(R)-nipecotic acid DMWGB40 Discovery agent N.A. Investigative [3]
(R/S) EF-1500 DMYDG27 Discovery agent N.A. Investigative [2]
(S)-EF-1520 DM0EQTM Discovery agent N.A. Investigative [2]
(S)-Piperidine-3-carboxylic acid DMST89H Discovery agent N.A. Investigative [3]
2,4-Diamino-butyric acid(GABA) DMAOGBP Discovery agent N.A. Investigative [5]
4-Hydroxy-piperidine-3-carboxylic acid DM9VQ0T Discovery agent N.A. Investigative [6]
LU32-176B DM2YOVC Discovery agent N.A. Investigative [7]
NIPECOTIC ACID DMPV450 Discovery agent N.A. Investigative [8]
SKF89976A DM0WNHQ Discovery agent N.A. Investigative [2]
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⏷ Show the Full List of 10 Investigative Drug(s)

References

1 Company report (Alcobra pharma)
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: 929).
3 Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling. J Med Chem. 2004 Nov 4;47(23):5620-9.
4 Tiagabine, 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.
5 Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions. J Med Chem. 1986 Feb;29(2):224-9.
6 Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors. J Med Chem. 1982 Oct;25(10):1157-62.
7 First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anti... J Pharmacol Exp Ther. 2005 Feb;312(2):866-74.
8 Epimeric cis-decahydroquinoline-5-carboxylic acids: effects on gamma-aminobutyric acid uptake and receptor binding in vitro. J Med Chem. 1981 Jul;24(7):788-94.
9 Mutations in the GABA Transporter SLC6A1 Cause Epilepsy with Myoclonic-Atonic Seizures. Am J Hum Genet. 2015 May 7;96(5):808-15.