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 ¹⁸F-labeled small TCO compound, [¹⁸F]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.

中文翻译：

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在卵巢癌模型中使用生物正交¹⁸ F标签的反式-环辛烯进行预靶向PET成像

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方法，该方法结合了抗体的出色靶亲和力和选择性以及使用短寿命放射性核素（例如氟18）的优势。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的狄尔斯-阿尔德（IEDDA）反应。在这里，我们报道了我们实验室最近开发的¹⁸ F标记的小TCO化合物[ ¹⁸ F] 1的首次成功使用，以进行预先靶向的免疫PET成像。该研究是在卵巢癌小鼠模型中使用曲妥珠单抗-四嗪偶联物进行的。