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- Title
One-step radiosynthesis of F-AlF-NOTA-RGD for tumor angiogenesis PET imaging.
- Authors
Shuanglong Liu; Hongguang Liu; Han Jiang; Yingding Xu; Hong Zhang; Zhen Cheng
- Abstract
Purpose: One of the major obstacles of the clinical translation of F-labeled arginine-glycine-aspartic acid (RGD) peptides has been the laborious multistep radiosynthesis. In order to facilitate the application of RGD-based positron emission tomography (PET) probes in the clinical setting we investigated in this study the feasibility of using the chelation reaction between AlF and a macrocyclic chelator-conjugated dimeric RGD peptide as a simple one-step F labeling strategy for development of a PET probe for tumor angiogenesis imaging. Methods: Dimeric cyclic peptide E[ c(RGDyK)] (RGD) was first conjugated with a macrocyclic chelator, 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), and the resulting bioconjugate NOTA-RGD was then radiofluorinated via AlF intermediate to synthesize F-AlF-NOTA-RGD. Integrin binding affinities of the peptides were assessed by a U87MG cell-based receptor binding assay using I-echistatin as the radioligand. The tumor targeting efficacy and in vivo profile of F-AlF-NOTA-RGD were further evaluated in a subcutaneous U87MG glioblastoma xenograft model by microPET and biodistribution. Results: NOTA-RGD was successfully F-fluorinated with good yield within 40 min using the AlF intermediate. The IC of F-AlF-NOTA-RGD was determined to be 46 ± 4.4 nM. Quantitative microPET studies demonstrated that F-AlF-NOTA-RGD showed high tumor uptake, fast clearance from the body, and good tumor to normal organ ratios. Conclusion: NOTA-RGD bioconjugate has been successfully prepared and labeled with AlF in one single step of radiosynthesis. The favorable in vivo performance and the short radiosynthetic route of F-AlF-NOTA-RGD warrant further optimization of the probe and the radiofluorination strategy to accelerate the clinical translation of F-labeled RGD peptides.
- Publication
European Journal of Nuclear Medicine & Molecular Imaging, 2011, Vol 38, Issue 9, p1732
- ISSN
1619-7070
- Publication type
Academic Journal
- DOI
10.1007/s00259-011-1847-4