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ÉVALUATION D'UN RADIOLIGAND DE L'INTÉGRINE αVβ3 (RAFT-RGD) POUR L'IMAGERIE MOLÉCULAIRE DE L'ANGIOGENÈSE TUMORALE.

Abstract : Tumoral neoangiogenesis targeting is currently a major field of research for the diagnostic and treatment of solid tumors. Endothelial cells from neovessels overexpress several specific markers such as the avb3 integrin, which binds RGD (-Arg-Gly-Asp-)-containing peptides. We evaluated the potential of a novel radiotracer – RAFT-RGD – for the molecular nuclear imaging of neovessels. In vitro, the coupling of 4 c(RGDfK) to the RAFT platform resulted in an increased cellular uptake of the tracer by avb3 positive cells when compared to c(RGDfK). Furthermore, RAFTRGD has a higher affinity than c(RGDfK) and similar properties for angiogenesis inhibition. In vivo, both avb3 positive and negative tumors were visible by non invasive whole body planar and tomographic imaging from 30 min to 24 h post-injection, using a gamma camera dedicated to small animal imaging.
Despite a lack of significant contrast improvement compare with c(RGDfK), RAFT-RGD could represent a promising tracer for tumoral angiogenesis since it could provide invaluable information about tumor development and treatment efficacy in Nuclear Medicine departments. Furthermore, thanks to its chemical structure, RAFT-RGD can be labelled with a variety of radioisotopes including γ and b- emitters, allowing interesting therapeutical applications such as internal targeted radiotherapy.
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Lucie Sancey. ÉVALUATION D'UN RADIOLIGAND DE L'INTÉGRINE αVβ3 (RAFT-RGD) POUR L'IMAGERIE MOLÉCULAIRE DE L'ANGIOGENÈSE TUMORALE.. Sciences du Vivant [q-bio]. Université Joseph-Fourier - Grenoble I, 2006. Français. ⟨tel-00398973⟩

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