一种新型 F 标记的点击底物，可通过 PET 对表达 SNAP 标签的细胞进行靶向成像。

A novel F-labeled clickable substrate for targeted imaging of SNAP-tag expressing cells by PET .

机构信息

European Institute for Molecular Imaging (EIMI), University of Münster, Germany.

Department of Nuclear Medicine, University Hospital Münster, Germany.

出版信息

Chem Commun (Camb). 2021 Sep 28;57(77):9850-9853. doi: 10.1039/d1cc03871k.

DOI:10.1039/d1cc03871k

PMID:34490435

Abstract

Bioorthogonal covalent labeling with self-labeling enzymes like SNAP-tag bears a high potential for specific targeting of cells for imaging and also . To this end, fluorescent SNAP substrates have been established and used in microscopy and fluorescence imaging while radioactive substrates for the highly sensitive and whole-body positron emission tomography (PET) have been lacking. Here, we show for the first time successful and high-contrast PET imaging of subcutaneous SNAP-tag expressing tumor xenografts by bioorthogonal covalent targeting with a novel F-based radioligand .

摘要

生物正交的共价标记与自标记酶（如 SNAP 标签）相结合，具有对细胞进行特异性成像和靶向的巨大潜力。为此，已经建立了荧光 SNAP 底物，并在显微镜和荧光成像中得到了应用，而对于高度敏感的全身正电子发射断层扫描（PET），则缺乏放射性底物。在这里，我们首次展示了通过新型 F 基放射性配体的生物正交共价靶向，成功地对皮下表达 SNAP 标签的肿瘤异种移植进行了高对比度的 PET 成像。