Preliminary biological evaluation of Ga-68-labeled cyclic RGD dimer as an integrin alpha(v)beta(3)-targeting radiotracer for tumor PET imaging

摘要

Radiolabeled 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 novel Ga-68-labeled RGD peptide for tumor angiogenesis imaging. [Ga-68]Ga-NOTA-PEG(3)-beta-Glu-RGD(2), a cyclic RGD dimer with a symmetric beta-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 alpha(v)beta(3)-positive tumor cells. The results suggest that [Ga-68]Ga-NOTA-PEG(3)-beta-Glu-RGD(2) may be a promising radiotracer for positron emission tomography imaging of tumor angiogenesis.