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Pretargeted PET Imaging Using a Bioorthogonal 18 F-Labeled trans-Cyclooctene in an Ovarian Carcinoma Model

In cancer research, pretargeted positron emission tomography (PET) imaging has emerged as an effective two-step approach that combines the excellent target affinity and selectivity of antibodies with the advantages of using short-lived radionuclides such as fluorine-18. One possible approach is base...

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Bibliographic Details
Published in:Bioconjugate chemistry 2017-12, Vol.28 (12), p.2915-2920
Main Authors: Billaud, Emilie M F, Belderbos, Sarah, Cleeren, Frederik, Maes, Wim, Van de Wouwer, Marlies, Koole, Michel, Verbruggen, Alfons, Himmelreich, Uwe, Geukens, Nick, Bormans, Guy
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Language:English
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Summary:In cancer research, pretargeted positron emission tomography (PET) imaging has emerged as an effective two-step approach that combines the excellent target affinity and selectivity of antibodies with the advantages of using short-lived radionuclides such as fluorine-18. One possible approach is based on the bioorthogonal inverse-electron-demand Diels-Alder (IEDDA) reaction between tetrazines and trans-cyclooctene (TCO) derivatives. Here, we report the first successful use of an F-labeled small TCO compound, [ F]1 recently developed in our laboratory, to perform pretargeted immuno-PET imaging. The study was performed in an ovarian carcinoma mouse model, using a trastuzumab-tetrazine conjugate.
ISSN:1043-1802
1520-4812
DOI:10.1021/acs.bioconjchem.7b00635