18F-FP-PEG2-β-Glu-RGD2: A Symmetric Integrin αvβ3-Targeting Radiotracer for Tumor PET Imaging.

Radiolabeled cyclic arginine-glycine-aspartic (RGD) peptides can be used for noninvasive determination of integrin αvβ3 expression in tumors. In this study, we performed radiosynthesis and biological evaluation of a new 18F-labeled RGD homodimeric peptide with one 8-amino-3,6-dioxaoctanoic acid (PEG2) linker on the glutamate β-amino group (18F-FP-PEG2-β-Glu-RGD2) as a symmetric PET tracer for tumor imaging.

Biodistribution studies showed that radioactivity of 18F-FP-PEG2-β-Glu-RGD2 was rapidly cleared from blood by predominately renal excretion. MicroPET-CT imaging with 18F-FP-PEG2-β-Glu-RGD2 revealed high tumor contrast and low background in A549 human lung adenocarcinoma-bearing mouse models, PC-3 prostate cancer-bearing mouse models, and orthotopic transplanted C6 brain glioma models. 18F-FP-PEG2-β-Glu-RGD2 exhibited good stability in vitro and in vivo. The results suggest that this tracer is a potential PET tracer for tumor imaging.

PloS one. 2015 Sep 23*** epublish ***

Kongzhen Hu, Xiaolan Tang, Ganghua Tang, Shaobo Yao, Baoguo Yao, Hongliang Wang, Dahong Nie, Xiang Liang, Caihua Tang, Shanzhen He

Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , College of Materials and Energy, Southern China Agricultural University, Guangzhou, 510642, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China. , Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.

PubMed      Full Text Article

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