ArticleSLAS discovery : advancing life sciences R & D2023
HTS driven by fluorescence lifetime detection of FRET identifies activators and inhibitors of cardiac myosin.
Article in SLAS discovery : advancing life sciences R & D, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
4 citing papers in PubMed, 7 citations in OpenAlex.
- Expanding Horizons in Advancements of FRET Biosensing Technologies.Biosensors · 2025Review
- Exploiting allosteric modulation: a new frontier for precision medicine.Molecular biology reports · 2025Review
- Structural Dynamics of Protein Interactions Using Site-Directed Spin Labeling of Cysteines to Measure Distances and Rotational Dynamics with EPR Spectroscopy.Applied magnetic resonance · 2024Article
- Extract2Chip-Bypassing Protein Purification in Drug Discovery Using Surface Plasmon Resonance.Biosensors · 2023Article
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Authors and funding
19 authors at 2 institutions in 1 country.
Funding
Abstract
Small molecules that bind to allosteric sites on target proteins to alter protein function are highly sought in drug discovery. High-throughput screening (HTS) assays are needed to facilitate the direct discovery of allosterically active compounds. We have developed technology for high-throughput time-resolved fluorescence lifetime detection of fluorescence resonance energy transfer (FRET), which enables the detection of allosteric modulators by monitoring changes in protein structure. We tested this approach at the industrial scale by adapting an allosteric FRET sensor of cardiac myosin to high-throughput screening (HTS), based on technology provided by Photonic Pharma and the University of Minnesota, and then used the sensor to screen 1.6 million compounds in the HTS facility at Bristol Myers Squibb. The results identified allosteric activators and inhibitors of cardiac myosin that do not compete with ATP binding, demonstrating high potential for FLT-based drug discovery.
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Registered trials
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