Journal
AMINO ACIDS
Volume 46, Issue 10, Pages 2355-2364Publisher
SPRINGER WIEN
DOI: 10.1007/s00726-014-1788-x
Keywords
MicroPET imaging; NGR; RGD; CD13; Integrin; Tumor angiogenesis; Ga-68 labeling
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Funding
- USC Department of Radiology
- National Natural Science Foundation of China [81230033, 81227901, 81090270, 81371594]
- National Basic Research Program of China (973 Program) [2011CB707704]
- International Cooperation Program of Xijing Hospital [XJZT13G02]
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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, Ga-68-NOTA-G(3)-NGR2 and Ga-68-NOTA-G(3)-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. Ga-68-NOTA-G(3)-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.
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