ArticleScientific reports2021
A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery.
Article in Scientific reports, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 13 citations in OpenAlex.
- TRACT assay-based in vitro characterization of substituted cathinones: inhibition and release at the serotonin transporter.Archives of toxicology · 2026Article
- Advancing drug discovery through assay development: a survey of tool compounds within the human solute carrier superfamily.Frontiers in pharmacology · 2024Article
- Label-free detection of prostaglandin transporter (SLCO2A1) function and inhibition: insights by wound healing and TRACT assays.Frontiers in pharmacology · 2024Article
- Proteochemometric Modeling Identifies Chemically Diverse Norepinephrine Transporter Inhibitors.Journal of chemical information and modeling · 2023Article
- Functional characterization of SLC39 family members ZIP5 and ZIP10 in overexpressing HEK293 cells reveals selective copper transport activity.Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine · 2023Article
- MPPInternational journal of molecular sciences · 2022Article
- Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters.Frontiers in pharmacology · 2022Article
- Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors.Scientific reports · 2021Article
- An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters.Frontiers in pharmacology · 2021Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Members of the solute carrier (SLC) transporter protein family are increasingly recognized as therapeutic drug targets. The majority of drug screening assays for SLCs are based on the uptake of radiolabeled or fluorescent substrates. Thus, these approaches often have limitations that compromise on throughput or the physiological environment of the SLC. In this study, we report a novel application of an impedance-based biosensor, xCELLigence, to investigate dopamine transporter (DAT) activity via substrate-induced activation of G protein-coupled receptors (GPCRs). The resulting assay, which is coined the 'transporter activity through receptor activation' (TRACT) assay, is based on the hypothesis that DAT-mediated removal of extracellular dopamine directly affects the ability of dopamine to activate cognate membrane-bound GPCRs. In two human cell lines with heterologous DAT expression, dopamine-induced GPCR signaling was attenuated. Pharmacological inhibition or the absence of DAT restored the apparent potency of dopamine for GPCR activation. The inhibitory potencies for DAT inhibitors GBR12909 (pIC
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