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Bimodal fluorescence/129Xe NMR probe for molecular imaging and biological inhibition of EGFR in Non-Small Cell Lung Cancer
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2017-11-06 , DOI: 10.1016/j.bmc.2017.11.002
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.



中文翻译:

双峰荧光/ 129 Xe NMR探针用于非小细胞肺癌的EGFR分子成像和生物学抑制

尽管非小细胞肺癌(NSCLC)是癌症死亡的主要原因之一,但在过去的几十年中,关于诊断和结果的改善甚微。在这项研究中,已设计出包含氙主体,荧光部分和治疗性抗体的双峰荧光/ 129 Xe NMR探针,以靶向在癌细胞中过表达的表皮生长因子受体(EGFR)。该生物传感器显示出对EGFR的高选择性以及与抗体相似的生物活性。通过超极化的129 Xe NMR可以高特异性和高灵敏度(亚纳摩尔范围)检测到它。这个有前途的系统应该找到治疗学用途的重要应用。

更新日期:2017-11-06
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