title: A direct comparison of tumor angiogenesis with ⁶⁸Ga-labeled NGR and RGD peptides in HT-1080 tumor xenografts using microPET imaging.
abstract: Peptides containing asparagine-glycine-arginine (NGR) and arginine-glycine-aspartic acid (RGD) sequence are being developed for tumor angiogenesis-targeted imaging and therapy. The aim of this study was to compare the efficacy of NGR- and RGD-based probes for imaging tumor angiogenesis in HT-1080 tumor xenografts. Two PET probes, (68)Ga-NOTA-G₃-NGR2 and ⁶⁸Ga-NOTA-G₃-RGD2, were successfully prepared. In vitro stability, partition coefficient, tumor cell binding, as well as in vivo biodistribution properties were also analyzed for both PET probes. The results revealed that the two probes were both hydrophilic and stable in vitro and in vivo, and they were excreted predominately and rapidly through the kidneys. For both probes, the higher tumor uptake and lower accumulation in vital organs were determined. No significant difference between two probes was observed in terms of tumor uptake and the in vivo biodistribution properties. We concluded that these two probes are promising in tumor angiogenesis imaging. ⁶⁸Ga-NOTA-G₃-NGR2 has the potential as an alternative for PET imaging in patients with fibrosarcoma, and it may offer an opportunity to noninvasively monitor CD13-targeted therapy.
authors.affiliation: Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, 15 Changle West Road, Xi'an, 710032, Shaanxi, China.
authors.forename: Yahui
authors.initials: Y
authors.lastname: Shao
authors.forename: Wansheng
authors.initials: W
authors.lastname: Liang
authors.forename: Fei
authors.initials: F
authors.lastname: Kang
authors.forename: Weidong
authors.initials: W
authors.lastname: Yang
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Ma
authors.forename: Guiyu
authors.initials: G
authors.lastname: Li
authors.forename: Shu
authors.initials: S
authors.lastname: Zong
authors.forename: Kai
authors.initials: K
authors.lastname: Chen
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
mesh_terms: D000230:Adenocarcinoma / Q000098:blood supply / Q000000981:diagnostic imaging; D000818:Animals; D001692:Biological Transport; D045744:Cell Line, Tumor; D004355:Drug Stability; D005260:Female; D005354:Fibrosarcoma / Q000098:blood supply* / Q000000981:diagnostic imaging; D005710:Gallium Radioisotopes; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008819:Mice, Nude; D057054:Molecular Imaging; D009389:Neovascularization, Pathologic / Q000000981:diagnostic imaging*; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics; D065667:Renal Elimination; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D005710:Gallium Radioisotopes; C526428:NGR peptide; D009842:Oligopeptides; D019275:Radiopharmaceuticals; C047981:arginyl-glycyl-aspartic acid