A direct comparison of tumor angiogenesis with 68Ga-labeled NGR and RGD peptides in HT-1080 tumor xenografts using microPET imaging
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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, 68Ga-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.
KeywordsMicroPET imaging NGR RGD CD13 Integrin Tumor angiogenesis 68Ga labeling
We thank Dr. Xiaoyuan Chen (National Institute of Biomedical Imaging and Bioengineering, Bethesda, MD, USA) for his generous gift of the NOTA-G3-RGD2 peptide. This work was supported by the USC Department of Radiology, the National Natural Science Foundation of China (Grant Nos. 81230033, 81227901, 81090270, 81371594), the National Basic Research Program of China (973 Program) (Grant No. 2011CB707704), and the International Cooperation Program of Xijing Hospital (Grant No. XJZT13G02).
Conflict of interest
The authors declare that they have no conflict of interest.
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