Cancer Institute A national cancer institute
designated cancer center

Matthew Bogyo

Publication Details

  • Noninvasive optical imaging of cysteine protease activity using fluorescently quenched activity-based probes NATURE CHEMICAL BIOLOGY Blum, G., von Degenfeld, G., Merchant, M. J., Blau, H. M., Bogyo, M. 2007; 3 (10): 668-677


    We have generated a series of quenched near-infrared fluorescent activity-based probes (qNIRF-ABPs) that covalently target the papain-family cysteine proteases shown previously to be important in multiple stages of tumorigenesis. These 'smart' probes emit a fluorescent signal only after covalently modifying a specific protease target. After intravenous injection of NIRF-ABPs into mice bearing grafted tumors, noninvasive, whole-body imaging allowed direct monitoring of cathepsin activity. Importantly, the permanent nature of the probes also allowed secondary, ex vivo biochemical profiling to identify specific proteases and to correlate their activity with whole-body images. Finally, we demonstrate that these probes can be used to monitor small-molecule inhibition of protease targets both biochemically and by direct imaging methods. Thus, NIRF-ABPs are (i) potentially valuable new imaging agents for disease diagnosis and (ii) powerful tools for preclinical and clinical testing of small-molecule therapeutic agents in vivo.

    View details for Web of Science ID 000249642700017

    View details for PubMedID 17828252

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