C-glycosyl compounds for bimodal TEP/FPIR imaging and application for RGD peptide labelling - Université de Lorraine Access content directly
Conference Papers Year : 2021

C-glycosyl compounds for bimodal TEP/FPIR imaging and application for RGD peptide labelling

Abstract

Combined [18F]PET/NIRF imaging (Positron Emission Tomography/Near Infra-Red Fluorescence) holds a huge potential for enhancing disease diagnosis and patient care. Such a combination conjugates the non-invasive diagnosis of PET with the intraoperative imaging guided surgery or ex vivo histopathology of NIRF imaging. In this context, we developed innovative dual [18F]PET/NIRF imaging agents based on a Cglycosyl derivative as central core functionalized in a regiocontrolled manner with a fluorescent cyanine derivative and a fluorine bound to a carbon which is optimal for in vivo stability. Two c(RGDfK) peptides targeting integrins, overexpressed in some malignant tumours, were grafted by CuAAC. The binding affinities towards integrins are in the same range or even better than the c(RGDfK) peptide reference, highlighting the benefit of the divalence. The in vitro optical imaging of the synthetic dual agents evaluated in U87MG cells shows a great cellular incorporation of the fluorinated and fluorescent compounds. The radiofluorination and the in vivo PET and NIRF imaging are currently in development.
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Dates and versions

hal-04466490 , version 1 (19-02-2024)

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  • HAL Id : hal-04466490 , version 1

Cite

Julen Ariztia, Kamal Jouad, Cédric Boura, Valérie Jouan-Hureaux, Sandrine Lamandé-Langle, et al.. C-glycosyl compounds for bimodal TEP/FPIR imaging and application for RGD peptide labelling. Journées du WP "Agents d'imagerie", WP1, de France Live Imaging et du GDR Agent d’imagerie Moléculaire, Nov 2021, Grenoble, France. ⟨hal-04466490⟩
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