Bimodal Fluorescence/129Xe NMR Probe for Molecular Imaging and Biological Inhibition of EGFR in Non-Small Cell Lung Cancer

Publication date: Available online 6 November 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Gaëlle Milanole, Bo Gao, Audrey Paoletti, Grégory Pieters, Christophe Dugave, Eric Deutsch, Sofia Rivera, Frédéric Law, Jean-Luc Perfettini, Emilie Mari, Estelle Léonce, Céline Boutin, Patrick Berthault, Hervé Volland, François Fenaille, Thierry Brotin, Bernard Rousseau
Although Non-Small Cell Lung Cancer (NSCLC) is one of the main causes of cancer death, very little improvement has been made in the last decades regarding diagnosis and outcomes. In this study, a bimodal fluorescence/¹²⁹Xe NMR probe containing a xenon host, a fluorescent moiety and a therapeutic antibody has been designed to target the Epidermal Growth Factor Receptors (EGFR) overexpressed in cancer cells. This biosensor shows high selectivity for the EGFR, and a biological activity similar to that of the antibody. It is detected with high specificity and high sensitivity (sub-nanomolar range) through hyperpolarized ¹²⁹Xe NMR. This promising system should find important applications for theranostic use.

Graphical abstract

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