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J Med Chem. 2020 Mar 26;63(6):3359-3369. doi: 10.1021/acs.jmedchem.9b02042. Epub 2020 Mar 16.

Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe.

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Wrocław University of Science and Technology, Department of Chemical Biology and Bioimaging, Wyb. Wyspiańskiego 29, 50-370 Wroclaw, Poland.
Monash University, Monash Biomedicine Discovery Institute, Department of Biochemistry and Molecular Biology, 23 Innovation Walk, Clayton, VIC 3800, Australia.
NCI-designated Cancer Center, Sanford-Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States.


Cytotoxic T-lymphocytes (CTLs) and natural killer cells (NKs) kill compromised cells to defend against tumor and viral infections. Both effector cell types use multiple strategies to induce target cell death including Fas/CD95 activation and the release of perforin and a group of lymphocyte granule serine proteases called granzymes. Granzymes have relatively broad and overlapping substrate specificities and may hydrolyze a wide range of peptidic epitopes; it is therefore challenging to identify their natural and synthetic substrates and to distinguish their localization and functions. Here, we present a specific and potent substrate, an inhibitor, and an activity-based probe of Granzyme A (GrA) that can be used to follow functional GrA in cells.

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