ChemRxiv
These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
Direct Aromatic 18 F-Labeling of Highly Reactive Tetrazines for Pretargeted Bioorthogonal PET Imaging.pdf (2.55 MB)

Direct Aromatic 18F-Labeling of Highly Reactive Tetrazines for Pretargeted Bioorthogonal PET Imaging

preprint
submitted on 20.02.2021, 14:34 and posted on 22.02.2021, 13:29 by Rocio Garcia-Vazquez, Umberto Maria Battisti, Jesper Tranekjær Jørgensen, Vladimir Shalgunov, Lars Hvass, Daniel L. Stares, Ida Nymann Petersen, François Crestey, Andreas Löffler, Dennis Svatunek, Jesper Langgaard Kristensen, Hannes Mikula, Andreas Kjaer, Matthias Herth
Pretargeted bioorthogonal imaging can be used to visualize and quantify slow accumulating targeting vectors with short-lived radionuclides such as fluorine-18 - the most 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 direct18 F-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 18 F-labeling procedure has been developed and applied to obtain a pretargeting tetrazine-based imaging agent with favorable characteristics (target-to-background ratios and clearance) that may qualify it for future clinical translation.

History

Email Address of Submitting Author

matthias.herth@sund.ku.dk

Institution

University of Copenhagen

Country

Denmark

ORCID For Submitting Author

0000-0002-7788-513X

Declaration of Conflict of Interest

No conflict of interest

Exports