Angewandte Chemie International Edition · 2011 · 130 citations · 34 references
MedicineMedicinal ChemistryPharmaceuticsMolecular ImagingMolecular OncologyTherapeutic Nuclear MedicineNuclear Medicine ChemistryProstate Cancer ImagingRadiopharmaceuticalsTargeted Imaging AgentsTargeted RadiopharmaceuticalsTumor Receptor ImagingAzide-based LabelingPeptide RadiolabelingPeptide RadiopharmaceuticalsPeptide-based RadiopharmaceuticalsPeptide-based RadiotracersPet RadiopharmaceuticalsReceptor-targeted Imaging AgentsTargeted Radionuclide Imaging
Click for PET: The GRP-receptor-specific peptide bombesin, which is often used for nuclear imaging of tumors, can be labeled with 18F in a mild and rapid manner by using a copper-free azide–alkyne “click” reaction. A range of azides can be used to provide peptides with different hydrophobicities. The resulting 18F radiopharmaceutical tracers (see scheme) maintain their high affinity for the targeted receptor in vitro in human prostate cancer cells.
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