| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10595583 | Bioorganic & Medicinal Chemistry Letters | 2013 | 7 Pages |
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.
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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,