title: 18F-FP-PEG2-β-Glu-RGD2: A Symmetric Integrin αvβ3-Targeting Radiotracer for Tumor PET Imaging.
abstract: 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.
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Kongzhen
authors.initials: K
authors.lastname: Hu
authors.affiliation: College of Materials and Energy, Southern China Agricultural University, Guangzhou, 510642, China.
authors.forename: Xiaolan
authors.initials: X
authors.lastname: Tang
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Ganghua
authors.initials: G
authors.lastname: Tang
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Shaobo
authors.initials: S
authors.lastname: Yao
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Baoguo
authors.initials: B
authors.lastname: Yao
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Hongliang
authors.initials: H
authors.lastname: Wang
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Dahong
authors.initials: D
authors.lastname: Nie
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Liang
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Caihua
authors.initials: C
authors.lastname: Tang
authors.affiliation: Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, 510080, China.
authors.forename: Shanzhen
authors.initials: S
authors.lastname: He
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D019281:Dimerization; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism*; D008175:Lung Neoplasms / Q000000981:diagnostic imaging*; D051379:Mice; D008819:Mice, Nude; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000737:chemistry*; D014018:Tissue Distribution; D014057:Tomography, X-Ray Computed; D014183:Transplantation, Heterologous
chemical_list: D005462:Fluorine Radioisotopes; D039302:Integrin alphaVbeta3; D009842:Oligopeptides; D019275:Radiopharmaceuticals; C047981:arginyl-glycyl-aspartic acid