ArticleScientific reports2021
Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors.
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 8 papers.
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Who cites it
8 citing papers in PubMed, 9 citations in OpenAlex.
- TRACT assay-based in vitro characterization of substituted cathinones: inhibition and release at the serotonin transporter.Archives of toxicology · 2026Article
- Roles of Single Nucleotide Polymorphisms in the SLC6A2 Gene in the Risk of Vasovagal Syncope Among Children in Eastern China: A Case-Control Study.Health science reports · 2025Article
- Label-free detection of prostaglandin transporter (SLCO2A1) function and inhibition: insights by wound healing and TRACT assays.Frontiers in pharmacology · 2024Article
- Advancing drug discovery through assay development: a survey of tool compounds within the human solute carrier superfamily.Frontiers in pharmacology · 2024Article
- Proteochemometric Modeling Identifies Chemically Diverse Norepinephrine Transporter Inhibitors.Journal of chemical information and modeling · 2023Article
- Accelerating SLC Transporter Research: Streamlining Knowledge and Validated Tools.Clinical pharmacology and therapeutics · 2022Article
- MPPInternational journal of molecular sciences · 2022Article
- Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters.Frontiers in pharmacology · 2022Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The human norepinephrine transporter (NET) is an established drug target for a wide range of psychiatric disorders. Conventional methods that are used to functionally characterize NET inhibitors are based on the use of radiolabeled or fluorescent substrates. These methods are highly informative, but pose limitations to either high-throughput screening (HTS) adaptation or physiologically accurate representation of the endogenous uptake events. Recently, we developed a label-free functional assay based on the activation of G protein-coupled receptors by a transported substrate, termed the TRACT assay. In this study, the TRACT assay technology was applied to NET expressed in a doxycycline-inducible HEK 293 JumpIn cell line. Three endogenous substrates of NET-norepinephrine (NE), dopamine (DA) and epinephrine (EP)-were compared in the characterization of the reference NET inhibitor nisoxetine. The resulting assay, using NE as a substrate, was validated in a manual HTS set-up with a Z' = 0.55. The inhibitory potencies of several reported NET inhibitors from the TRACT assay showed positive correlation with those from an established fluorescent substrate uptake assay. These findings demonstrate the suitability of the TRACT assay for HTS characterization and screening of NET inhibitors and provide a basis for investigation of other solute carrier transporters with label-free biosensors.
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