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2-Fluoropyridine prosthetic compounds for the 18F labeling of bombesin analogues |
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| Authors: | James Inkster Kuo-Shyan Lin Samia Ait-Mohand Simon Gosselin François Bénard Brigitte Guérin Maral Pourghiasian Thomas Ruth Paul Schaffer Tim Storr |
| Institution: | 1. TRIUMF, Nuclear Medicine Division, 4004 Wesbrook Mall, Vancouver, Canada BC V6T 2A3;2. Simon Fraser University, Dept. of Chemistry, 8888 University Drive, Burnaby, Canada BC V5A 1S6;3. BC Cancer Agency, Dept. of Molecular Oncology, 675 West 10th Avenue, Vancouver, Canada BC V5Z 1L3;4. Université de Sherbrooke, Department of Nuclear Medicine and Radiobiology, 3001 12e Avenue Nord, Sherbrooke, Canada QC J1H 5N4 |
| Abstract: | Acetylene-bearing 2-18F]fluoropyridines 18F]FPy5yne and PEG-18F]FPyKYNE were prepared via efficient nucleophilic heteroaromatic 18F]fluorination of their corresponding 2-trimethylammoniumpyrdinyl precursors. The prosthetic groups were conjugated to azide- and PEG3-modified bombesin(6–14) analogues via copper-catalyzed azide–alkyne cycloaddition couplings to yield mono- and di-mini-PEGylated ligands for PET imaging of the gastrin- releasing peptide receptor. The PEG3- and PEG2/PEG3-bearing 18F peptides showed decreased lipophilicity relative to an analogous non-mini-PEGylated 18F peptide. Assessment of water-soluble peptide pharmacokinetics and tumour-targeting capabilities in a mouse model of prostate cancer is currently underway. |
| Keywords: | Bombesin Positron emission tomography Fluorine-18 CuAAC chemistry Neuropeptides |
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