Billaud Emilie M F, Belderbos Sarah, Cleeren Frederik, Maes Wim, Van de Wouwer Marlies, Koole Michel, Verbruggen Alfons, Himmelreich Uwe, Geukens Nick, Bormans Guy
Laboratory for Radiopharmaceutical Research, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven , Campus Gasthuisberg, O&N2, Herestraat 49, Box 821, 3000 Leuven, Belgium.
Biomedical MRI/MoSAIC, Department of Imaging and Pathology, KU Leuven , Campus Gasthuisberg, O&N1, Herestraat 49, Box 505, 3000 Leuven, Belgium.
Bioconjug Chem. 2017 Dec 20;28(12):2915-2920. doi: 10.1021/acs.bioconjchem.7b00635. Epub 2017 Dec 11.
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.
在癌症研究中，预靶向正电子发射断层扫描（PET）成像已成为一种有效的两步法，该方法将抗体出色的靶标亲和力和选择性与使用诸如氟-18等短寿命放射性核素的优势相结合。一种可能的方法是基于四嗪与反式环辛烯（TCO）衍生物之间的生物正交逆电子需求狄尔斯-阿尔德（IEDDA）反应。在此，我们报告了首次成功使用我们实验室最近开发的一种F标记的小TCO化合物[F]1进行预靶向免疫PET成像。该研究在卵巢癌小鼠模型中进行，使用了曲妥珠单抗-四嗪偶联物。
