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Phosphinate Esters as Novel Warheads for Quenched Activity-Based Probes Targeting Serine Proteases

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Download Hi-Res ImageDownload to MS-PowerPointCite This:ACS Chem. Biol. 2024, 19, 7, 1409-1415
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    Phosphinate Esters as Novel Warheads for Quenched Activity-Based Probes Targeting Serine Proteases
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    • Jan Pascal Kahler
      Jan Pascal Kahler
      Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, KU Leuven − University of Leuven, Herestraat 49 box 901b, 3000 Leuven, Belgium
      More by Jan Pascal Kahler
    • Shanping Ji
      Shanping Ji
      Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, KU Leuven − University of Leuven, Herestraat 49 box 901b, 3000 Leuven, Belgium
      More by Shanping Ji
    • Femke Speelman-Rooms
      Femke Speelman-Rooms
      Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, KU Leuven − University of Leuven, Herestraat 49 box 901b, 3000 Leuven, Belgium
      Laboratory of Molecular & Cellular Signaling, Department of Cellular and Molecular Medicine, Herestraat 49 box 802, 3000 Leuven, Belgium
      More by Femke Speelman-Rooms
    • Roeland Vanhoutte
      Roeland Vanhoutte
      Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, KU Leuven − University of Leuven, Herestraat 49 box 901b, 3000 Leuven, Belgium
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    • Steven H. L. Verhelst*
      Steven H. L. Verhelst
      Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, KU Leuven − University of Leuven, Herestraat 49 box 901b, 3000 Leuven, Belgium
      AG Chemical Proteomics, Leibniz Institute for Analytical Sciences − ISAS, Otto-Hahn-Str. 6b, 44227 Dortmund, Germany
      *[email protected]; [email protected]
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      Orcidhttps://orcid.org/0000-0002-7400-1319
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    ACS Chemical Biology

    Cite this: ACS Chem. Biol. 2024, 19, 7, 1409–1415
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    https://doi.org/10.1021/acschembio.3c00203
    Published June 24, 2024
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    Abstract

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    Quenched activity-based probes (qABP) are invaluable tools to visualize aberrant protease activity. Unfortunately, most studies so far have only focused on cysteine proteases, and only a few studies describe the synthesis and use of serine protease qABPs. We recently used phosphinate ester electrophiles as a novel type of reactive group to construct ABPs for serine proteases. Here, we report on the construction of qABPs based on the phosphinate warhead, exemplified by probes for the neutrophil serine proteases. The most successful probes show sub-stoichiometric reaction with human neutrophil elastase, efficient fluorescence quenching, and rapid unquenching of fluorescence upon reaction with target proteases.

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    • Synthesis schemes, structures and quenching properties of qABPs, quantification of labeling of purified enzymes, flow cytometry, stability test, methods, NMR spectra, and LCMS chromatograms (PDF)

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    ACS Chemical Biology

    Cite this: ACS Chem. Biol. 2024, 19, 7, 1409–1415
    Click to copy citationCitation copied!
    https://doi.org/10.1021/acschembio.3c00203
    Published June 24, 2024
    Copyright © 2024 American Chemical Society
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