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- W130774619 abstract "524 Objectives Clinical translation of 18F-labeled arginine-glycine-aspartate (RGD) peptides is partially hindered by the multi-step and laborious radiosynthesis. The goal of this study was to investigate the feasibility of one-step 18F-labeling of a dimeric RGD peptide for microPET imaging via a simple chelation reaction between Al18F and NOTA-RGD2. Methods Cyclic peptide E[c(RGDyK)]2 (RGD2) was conjugated with macrocyclic chelator 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) and labeled with Al18F to synthesize [18F]AlF-NOTA-RGD2. The petide conjugate’s affinity and specificity to integrin were assessed by cell-based receptor binding assay, and the tumor targeting efficacy of [18F]AlF-NOTA-RGD2 was evaluated in a subcutaneous U87MG glioblastoma xenograft mouse model. Results The NOTA-RGD2 conjugate could be radiofluorinated in good yield within 40 min via Al18F intermediate. The IC50 of [19F]AlF-NOTA-RGD2 determined by U87MG cell-based receptor binding assay was 46 ± 4.4 nM using 125I-echistatin as radioligand. Quantitative microPET imaging studies using [18F]AlF-NOTA-RGD2 demonstrated the high tumor uptake, fast clearance from body, and good tumor to normal organ ratios. Conclusions The NOTA-RGD2 conjugate has been successfully labeled with Al18F in one single step. The good in vivo behavior plus the short synthesis route for [18F]AlF-NOTA-RGD2 warrant further exploration for kit-like production of 18F-labeled RGD PET radiopharmaceutical for integrin αvβ3 imaging and potential clinical translation" @default.
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- W130774619 date "2011-05-01" @default.
- W130774619 modified "2023-09-24" @default.
- W130774619 title "Development of [18F]AlF-NOTA-RGD2 probe for microPET imaging in U87MG-tumor bearing mice" @default.
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