The ability to achieve live cancer cell detection, and microscopic imaging of cellular components (organelles), will be of great importance for diagnosis and individualized treatment of this disease.  Enzyme-activation of probes that results in decloaking of probe fluorescence is a highly promising route for these oncology goals, namely visualization of diseased tissue during guided surgery, and cellular imaging of the effects of cancer treatments.  Here, we describe the synthesis and in vitro evaluation of probe molecules whose fluorescence is turned on by the reductase enzyme NQO1 that is highly upregulated in a variety of cancer tissues.   The resulting fluorescence-active dyes allow for the visualization and imaging of cancer cells with unprecedented selectivity and imaging figures of merit (signal-to-background), due to probe/dye molecular design.  Detection of ovarian, colon, and lung cancer cells will be discussed.  These probes greatly diversify the limited number of synthetically accessible probes that can be activated by cancer-associated enzymes.

Cancer cell detection and imaging via enzyme-activation of cloaked fluorophore probes

247th National Meeting (2014)

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