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Self-assembling fluorescent small molecule probe to image tumor response to chemotherapy in vivo

Cell culture and mouse studies have identified an apoptosis-sensing molecular probe that could be used to image tumor response to treatment in vivo. A biocompatible, caspase-sensitive fluorescent probe that self-assembles within cells after caspase cleavage and thiol-mediated cyclization was identified. In cultured tumor cell lines, staurosporine- or doxorubicin-induced apoptosis led to a dose- and time-dependent increase in probe fluorescence within cells compared with no treatment. In a mouse xenograft model of cervical cancer, i.v. infusion of the probe plus doxorubicin led to greater fluorescence within tumor cells than either infusion of the probe plus saline or doxorubicin alone. Next steps include adapting the probe for PET or MRI imaging.
Staurosporine is a research reagent that acts as a pan-kinase inhibitor.
Doxorubicin is a generic chemotherapy drug.

SciBX 7(21); doi:10.1038/scibx.2014.630
Published online May 29, 2014

Patented; available for licensing

Ye, D. et al. Nat. Chem.;
published online April 28, 2014;
Contact: Jianghong Rao, Stanford University, Stanford, Calif.