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• W2135200923 abstract "Radiolabeled bombesin (BBN) analogs that bind to the gastrin-releasing peptide receptor (GRPR) represent a topic of active investigation for the development of molecular probes for PET or SPECT of prostate cancer (PCa). RM1 and AMBA have been identified as the 2 most promising BBN peptides for GRPR-targeted cancer imaging and therapy. In this study, to develop a clinically translatable BBN-based PET probe, we synthesized and evaluated ¹⁸F-AlF- (aluminum-fluoride) and ⁶⁴Cu-radiolabeled RM1 and AMBA analogs for their potential application in PET imaging of PCa. <b>Methods:</b> 1,4,7-triazacyclononane, 1-glutaric acid-4,7 acetic acid (NODAGA)–conjugated RM1 and AMBA were synthesized and tested for their GRPR-binding affinities. The NODAGA-RM1 and NODAGA-AMBA probes were further radiolabeled with ⁶⁴Cu or ¹⁸F-AlF and then evaluated in a subcutaneous PCa xenograft model (PC3) by small-animal PET imaging and biodistribution studies. <b>Results:</b> NODAGA-RM1 and NODAGA-AMBA can be successfully synthesized and radiolabeled with ⁶⁴Cu and ¹⁸F-AlF. ⁶⁴Cu- and ¹⁸F-AlF-labeled NODAGA-RM1 demonstrated excellent serum stability and tumor-imaging properties in the in vitro stability assays and in vivo imaging studies. ⁶⁴Cu-NODAGA-RM1 exhibited tumor uptake values of 3.3 ± 0.38, 3.0 ± 0.76, and 3.5 ± 1.0 percentage injected dose per gram of tissue (%ID/g) at 0.5, 1.5, and 4 h after injection, respectively. ¹⁸F-AlF-NODAGA-RM1 exhibited tumor uptake values of 4.6 ± 1.5, 4.0 ± 0.87, and 3.9 ± 0.48 %ID/g at 0.5, 1, and 2 h, respectively. <b>Conclusion:</b> The high-stability, efficient tumor uptake and optimal pharmacokinetic properties highlight ¹⁸F-AlF-NODAGA-RM1 as a probe with great potential and clinical application for the PET imaging of prostate cancer." @default.
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• W2135200923 date "2013-11-06" @default.
• W2135200923 modified "2023-10-07" @default.
• W2135200923 title "A Comparative Study of Radiolabeled Bombesin Analogs for the PET Imaging of Prostate Cancer" @default.
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• W2135200923 doi "https://doi.org/10.2967/jnumed.113.121533" @default.
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