Key result
Novel fluorescence-based thallium flux assay successfully detects potassium channel modulators for high-throughput screening.
Why the study?
Current high-throughput techniques for screening potassium channel modulators are limited by data quality, temporal resolution, ease of use, and specialized instrumentation requirements.
A novel fluorescence-based thallium flux assay enables high-throughput screening of large chemical libraries for potassium channel modulators using standard laboratory equipment.
May enable HTS of potassium channel modulators; leaves open clinical translation from mammalian cell data.
Potassium channels have been identified as targets for a large number of therapeutic indications. The ability to use a high-throughput functional assay for the detection and characterization of small-molecule modulators of potassium channels is very desirable. However, present techniques capable of screening very large chemical libraries are limited in terms of data quality, temporal resolution, ease of use, and requirements for specialized instrumentation. To address these issues, the authors have developed a fluorescence-based thallium flux assay. This assay is capable of detecting modulators of both voltage and ligand-gated potassium channels expressed in mammalian cells. The thallium flux assay can use instruments standard to most high-throughput screening laboratories, and using such equipment has been successfully employed to screen large chemical libraries consisting of hundreds of thousands of compounds.
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Weaver et al. (2004) studied this question. Fluorescence-based thallium flux assay vs. Present techniques was evaluated on Detection of modulators of voltage and ligand-gated potassium channels. A novel fluorescence-based thallium flux assay successfully detected modulators of voltage- and ligand-gated potassium channels in mammalian cells for high-throughput screening.
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