Search Results - "Sijben, Hubert J."
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A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery
Published in Scientific reports (14-01-2021)“…Members of the solute carrier (SLC) transporter protein family are increasingly recognized as therapeutic drug targets. The majority of drug screening assays…”
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MPP + -Induced Changes in Cellular Impedance as a Measure for Organic Cation Transporter (SLC22A1-3) Activity and Inhibition
Published in International journal of molecular sciences (21-01-2022)“…The organic cation transporters OCT1-3 ( ) facilitate the transport of cationic endo- and xenobiotics and are important mediators of drug distribution and…”
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Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors
Published in Scientific reports (10-06-2021)“…The human norepinephrine transporter (NET) is an established drug target for a wide range of psychiatric disorders. Conventional methods that are used to…”
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Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters
Published in Frontiers in pharmacology (23-05-2022)“…Excitatory amino acid transporters (EAAT/SLC1) mediate Na -dependent uptake of extracellular glutamate and are potential drug targets for neurological…”
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Molecular insights into disease-associated glutamate transporter (EAAT1 / SLC1A3 ) variants using in silico and in vitro approaches
Published in Frontiers in molecular biosciences (2023)“…Glutamate is an essential excitatory neurotransmitter and an intermediate for energy metabolism. Depending on the tumor site, cancer cells have increased or…”
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Targeting solute carriers to modulate receptor–ligand interactions
Published in Trends in pharmacological sciences (Regular ed.) (01-05-2022)“…Solute carrier transporters (SLCs) limit receptor activation via uptake of extracellular ligands. Novel concepts are emerging that describe the modulation of…”
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An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters
Published in Frontiers in pharmacology (10-08-2021)“…The solute carrier (SLC) superfamily represents the biggest family of transporters with important roles in health and disease. Despite being attractive and…”
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Still in Search for an EAAT Activator: GT949 Does Not Activate EAAT2, nor EAAT3 in Impedance and Radioligand Uptake Assays
Published in ACS chemical neuroscience (03-04-2024)“…Excitatory amino acid transporters (EAATs) are important regulators of amino acid transport and in particular glutamate. Recently, more interest has arisen in…”
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Advancing drug discovery through assay development: a survey of tool compounds within the human solute carrier superfamily
Published in Frontiers in pharmacology (09-07-2024)“…With over 450 genes, solute carriers (SLCs) constitute the largest transporter superfamily responsible for the uptake and efflux of nutrients, metabolites, and…”
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