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

Gaëlle Milanole (1) , Bo Gao (1) , Audrey Paoletti (2) , Grégory Pieters (1) , Christophe Dugave (1) , Eric Deutsch (2, 3, 4) , Sofia Rivera (2, 3, 4) , Fredéric Law (3) , Jean-Luc Perfettini (3) , Emilie Mari (5) , Estelle Léonce (5) , Céline Boutin (5) , Patrick Berthault (5) , Hervé Volland (6) , François Fenaille (6) , Thierry Brotin (7) , Bernard Rousseau (1)

1 SCBM - Service de Chimie Bio-Organique et de Marquage
2 UMR 1030 - Radiothérapie moléculaire
3 Département de radiothérapie [Gustave Roussy]
4 UP11 UFR Médecine - Université Paris-Sud - Paris 11 - Faculté de médecine
5 LSDRM - Laboratoire Structure et Dynamique par Résonance Magnétique (LCF)
6 IBITECS - Institut de Biologie et de Technologies de Saclay
7 LC - Laboratoire de Chimie - UMR5182

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/$^{129}$Xe 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 $^{129}$Xe NMR. This promising system should find important applications for theranostic use.

Keywords: Cetuximab; Hyperpolarized Xenon; NMR; EGFR; Biosensor

Domains: Chemical Sciences; Material chemistry; Life Sciences [q-bio]

Gaëlle Milanole, Bo Gao, Audrey Paoletti, Grégory Pieters, Christophe Dugave, et al.. Bimodal Fluorescence/{129}Xe NMR Probe for Molecular Imaging and Biological Inhibition of EGFR in Non-Small Cell Lung Cancer. Bioorganic and Medicinal Chemistry, 2017, 25, pp.6653-6660. ⟨10.1016/j.bmc.2017.11.002⟩. ⟨cea-01630103⟩