Preliminary biological evaluation of 68Ga-labeled cyclic RGD dimer as an integrin αvβ3-targeting radiotracer for tumor PET imaging
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 68Ga-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.
Keywordsαvβ3 Integrin RGD peptides Angiogenesis Gallium-68 PET imaging
This study was funded in part by the Science and Technology Foundation of Guangdong Province (No. 2016B090920087), the Science and Technology Planning Project Foundation of Guangzhou (Nos. 201604020169 and 201510010145), the National Natural Science Foundation of China (Nos. 81571704, 81671719 and 81770505), the Natural Science Foundation of Guangdong Province (No. 2015A030313067), the Research Project of Shanghai Municipal Health and Family Planning Commission (No. 201740060), and China Postdoctoral Science Foundation (Nos. 2018M631029 and 2019T120775).
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