Direct Cu-mediated aromatic ¹⁸F-labeling of highly reactive tetrazines for pretargeted bioorthogonal PET imaging.

ABSTRACT: Pretargeted imaging can be used to visualize and quantify slow-accumulating targeting vectors with short-lived radionuclides such as fluorine-18 - the most popular clinically applied Positron Emission Tomography (PET) radionuclide. Pretargeting results in higher target-to-background ratios compared to conventional imaging approaches using long-lived radionuclides. Currently, the tetrazine ligation is the most popular bioorthogonal reaction for pretargeted imaging, but a direct ¹⁸F-labeling strategy for highly reactive tetrazines, which would be highly beneficial if not essential for clinical translation, has thus far not been reported. In this work, a simple, scalable and reliable direct ¹⁸F-labeling procedure has been developed. We initially studied the applicability

SUBMITTER: Garcia-Vazquez R 

PROVIDER: S-EPMC8442695 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature