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

Bioconjug Chem

Laboratory for Radiopharmaceutical Research, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven , Campus Gasthuisberg, O&N2, Herestraat 49, Box 821, 3000 Leuven, Belgium.

Published: December 2017


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Article Abstract

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.

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http://dx.doi.org/10.1021/acs.bioconjchem.7b00635DOI Listing

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