Cancer Institute A national cancer institute
designated cancer center

Matthew Bogyo

Publication Details

  • Dynamic imaging of protease activity with fluorescently quenched activity-based probes NATURE CHEMICAL BIOLOGY Blum, G., Mullins, S. R., Keren, K., Fonovic, M., Jedeszko, C., RICE, M. J., Sloane, B. F., Bogyo, M. 2005; 1 (4): 203-209


    Protease activity is tightly regulated in both normal and disease conditions. However, it is often difficult to monitor the dynamic nature of this regulation in the context of a live cell or whole organism. To address this limitation, we developed a series of quenched activity-based probes (qABPs) that become fluorescent upon activity-dependent covalent modification of a protease target. These reagents freely penetrate cells and allow direct imaging of protease activity in living cells. Targeted proteases are directly identified and monitored biochemically by virtue of the resulting covalent tag, thereby allowing unambiguous assignment of protease activities observed in imaging studies. We report here the design and synthesis of a selective, cell-permeable qABP for the study of papain-family cysteine proteases. This probe is used to monitor real-time protease activity in live human cells with fluorescence microscopy techniques as well as standard biochemical methods.

    View details for DOI 10.1038/nchembo728

    View details for Web of Science ID 000232649000011

    View details for PubMedID 16408036

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