Kit like 18F labeling method for synthesis of RGD peptide-based PET probes

摘要

Positron Emission Tomography (PET) has become a popular imaging technique widely used for diagnostic purposes. To date, much attention has been devoted to ¹⁸F-fluoride because of the characteristics of its nuclear decay, as well as its relative ease of preparation from ¹⁸O-water. However, with a half-life of 110 minutes, swift and efficient incorporation of ¹⁸F-fluorine into biomolecules is necessary to minimize loss of activity. Therefore, the discovery of rapid and reliable incorporation of ¹⁸F-fluorine atoms into biomolecules would be highly beneficial, especially if these protocols can be carried out directly in irradiated 18O-water. In the study published in the American Journal of Nuclear Medicine and Molecular Imaging, cyclo-RGD-¹⁸F-aryltrifluoroborate conjugates were prepared based on one-step and one-pot-two-step methods. This paper represents recent efforts on the design and development of novel PET tracers based on the “Kit like” ¹⁸F labeling method.