Molecular turn-on probes have a potential in selective identification of living cancer cells by targeting highly upregulated intracellular biomarkers such as human NAD(P)H:quinone oxidoreductase isoenzyme 1 (hNQO1). We report a napthalimide-based fluorescent reporter conjugated with a trimethyl-locked quinone as a trigger group; the resulting probe is activated in the presence of hNQO1. Quantum yields, thermodynamic feasibility of quenching, and cell viability in the presence of probe and reporter is obtained. In vitro enzyme assays are performed for probe kinetic activation parameters. Confocal microscopy is used for the visualization of cancer cell lines with NQO1 (HT29 and OVCAR-3) and without NQO1 (H596 and H446).

Characterization of an hNQO1-activatable fluorescent probe and its use for visualization of human cancer cells

247th National Meeting (2014)

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