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Noninvasive imaging of c(RGD)29R as a potential delivery carrier for transfection of siRNA in malignant tumors

文献作者:Xue Qi Chen, Meng Liu, Rong Fu Wang, Ping Yan,  Chun Li Zhang, Chao Ma, Qian Zhao, Lei Yin, Guang Yu Zhao, Feng Qin Guo     《Journal of Labelled Compounds and Radiopharmaceuticals》 ABSTRACTS The purpose of our study was to develop and evaluate a novel integrin α v β 3 specific delivery carrier for transfection of siRNA in malignant tumors. We adopted arginineglycineaspartate  (RGD) motif as a tissue target for specific recognition of integrin α ν β 3 . A chimaeric peptide was synthesized by adding nonamer arginine residues (9arginine [9R]) at the carboxy terminus of cyclicRGD dimer, designated as c(RGD) 2 9R, to enable small interfering RNA (siRNA) binding. To test the applicability of the delivery carrier in vivo, c(RGD) 2 9R was labeled with radionuclide of technetium99m. Biodistribution and γcamera imaging studies were performed in HepG2 xenograftbearing nude mice. As results, an optimal 10:1 molar ratio of  99m Tcc(RGD) 2 9R to siRNA w...