Preliminary biological evaluation of 68 Ga-labeled cyclic RGD dimer as an integrin α v β 3 -targeting radiotracer for tumor PET imaging

AbstractRadiolabeled cyclic arginine-glycine-aspartic acid (RGD) peptides have been widely prepared for noninvasive monitoring of tumor angiogenesis. The aim of this study was to explore and evaluate the feasibility of a novel68Ga-labeled RGD peptide for tumor angiogenesis imaging. [68Ga]Ga-NOTA-PEG3- β-Glu-RGD2, a cyclic RGD dimer with a symmetric β-glutamate linker, was successfully designed and radiolabeled in high radiochemical yields. A series of experiments in vivo and in vitro were investigated to perform a preliminary evaluation and confirm good target at integrin αvβ3-positive tumor cells. The results suggest that [68Ga]Ga-NOTA-PEG3- β-Glu-RGD2 may be a promising radiotracer for positron emission tomography imaging of tumor angiogenesis.
Source: Journal of Radioanalytical and Nuclear Chemistry - Category: Nuclear Medicine Source Type: research