Proteins > Sodium- and chloride-dependent GABA transporter 1
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Sodium- and chloride-dependent GABA transporter 1
A sodium- and chloride-dependent GABA transporter 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P30531]
Synonyms
GAT-1;
Solute carrier family 6 member 1
Research
Bioassay Publications (15)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (6.67) | 18.2507 |
| 2000's | 2 (13.33) | 29.6817 |
| 2010's | 11 (73.33) | 24.3611 |
| 2020's | 1 (6.67) | 2.80 |
Compounds (17)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tiagabine | Homo sapiens (human) | Kd | 0.0937 | 2 | 2 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tiagabine | Homo sapiens (human) | INH | 0.0700 | 1 | 1 |
| tiagabine | Homo sapiens (human) | Km | 24.5500 | 2 | 2 |
| nnc 711 | Homo sapiens (human) | INH | 0.0400 | 1 | 1 |
| ci 966 | Homo sapiens (human) | INH | 0.2600 | 1 | 1 |
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).Journal of medicinal chemistry, , 11-09, Volume: 60, Issue:21, 2017
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Novel Allosteric Ligands of γ-Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids.Bioorganic & medicinal chemistry, , Mar-15, Volume: 23, Issue:6, 2015
The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities.Journal of natural products, , Oct-25, Volume: 76, Issue:10, 2013
Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.European journal of medicinal chemistry, , Volume: 45, Issue:6, 2010
The lignan (-)-hinokinin displays modulatory effects on human monoamine and GABA transporter activities.Journal of natural products, , Oct-25, Volume: 76, Issue:10, 2013
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.ACS medicinal chemistry letters, , Aug-14, Volume: 5, Issue:8, 2014
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Aminomethyltetrazoles as potential inhibitors of the γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Nov-01, Volume: 19, Issue:21, 2011
Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| gamma-aminobutyric acid:sodium:chloride symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: gamma-aminobutyric acid(out) + Na+(out) + Cl-(out) = gamma-aminobutyric acid(in) + Na+(in) + Cl(in). [PMID:7589472, PMID:7861179] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| gamma-aminobutyric acid transmembrane transporter activity | molecular function | Enables the transfer of gamma-aminobutyric acid from one side of a membrane to the other. Gamma-aminobutyric acid is 4-aminobutyrate (GABA). [GOC:go_curators, GOC:mtg_transport, ISBN:0198506732, ISBN:0815340729] |
| sodium:chloride symporter activity | molecular function | Enables the transfer of a solute or solutes from one side of a membrane to the other according to the reaction: Na+(out) + Cl-(out) = Na+(in) + Cl-(in). [TC:2.A.30.4.-] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
| GABA-ergic synapse | cellular component | A synapse that uses GABA as a neurotransmitter. These synapses are typically inhibitory. [GOC:dos] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
Involved In
This protein is involved in 19 target(s):
| Target | Category | Definition |
|---|
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
| response to toxic substance | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a toxic stimulus. [GOC:lr] |
| response to sucrose | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a sucrose stimulus. [GOC:jl] |
| response to inorganic substance | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an inorganic substance stimulus. [GOC:sm] |
| response to lead ion | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lead ion stimulus. [GOC:tair_curators, PMID:16461380] |
| positive regulation of gamma-aminobutyric acid secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of gamma-aminobutyric acid. [GOC:ef] |
| response to purine-containing compound | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a purine-containing compound stimulus. [GOC:ef] |
| negative regulation of synaptic transmission, GABAergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of GABAergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter gamma-aminobutyric acid (GABA). [GOC:mah] |
| response to estradiol | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |
| response to cocaine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
| response to calcium ion | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a calcium ion stimulus. [GOC:ai] |
| gamma-aminobutyric acid reuptake | biological process | The uptake of gamma-aminobutyric acid (GABA, 4-aminobutyrate) by neurons or glial cells. This process leads to inactivation and recycling of neurotransmitters. [ISBN:0123668387] |
| gamma-aminobutyric acid import | biological process | The directed movement of gamma-aminobutyric acid (GABA, 4-aminobutyrate) into a cell or organelle. [GOC:ai] |
| inorganic anion import across plasma membrane | biological process | The directed movement of inorganic anions from outside of a cell, across the plasma membrane and into the cytosol. [GOC:dos] |
| sodium ion import across plasma membrane | biological process | The directed movement of sodium ions from outside of a cell, across the plasma membrane and into the cytosol. [GOC:dos] |
| transport across blood-brain barrier | biological process | The directed movement of substances (e.g. macromolecules, small molecules, ions) through the blood-brain barrier. [GOC:aruk, GOC:bc, PMID:29377008] |
| chloride transmembrane transport | biological process | The process in which chloride is transported across a membrane. [GOC:TermGenie, GOC:vw] |
| sodium ion transmembrane transport | biological process | A process in which a sodium ion is transported from one side of a membrane to the other by means of some agent such as a transporter or pore. [GOC:vw] |
| amino acid transport | biological process | The directed movement of amino acids, organic acids containing one or more amino substituents, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |