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RXH-Reactive 18F-Vinyl Sulfones as Versatile Agents for PET Probe Construction
Bioconjugate Chemistry ( IF 4.7 ) Pub Date : 2020-10-25 , DOI: 10.1021/acs.bioconjchem.0c00487
Tao Zhang 1 , Jianhua Cai 1, 2 , Hui Wang 1 , Mengzhe Wang 1 , Hong Yuan 1 , Zhanhong Wu 1 , Xiaofen Ma 1, 3 , Zibo Li 1
Affiliation  

Efficient radiolabeling reactions are important chemical tools in biomedical research especially in probe construction. Herein, three 18F-labeled vinyl sulfones were prepared. In particular, 18F-PEG1-VS (((2-(2-(fluoro-18F)ethoxy)ethyl)sulfonyl)ethane) could not only allow chemoselective labeling of bioactive molecules containing −XH (X = S, NH) groups, but also react with red blood cells both in vitro and in living mice for potential cell tracking applications. In addition, these hydrophilic agents were found to cross the blood brain barrier (BBB) efficiently and localize at the cerebellum region. In summary, 18F-labeled vinyl sulfones provide a versatile platform for PET probe construction.

中文翻译:

RXH反应性18 F-乙烯基砜可作为PET探针构建的多功能试剂

高效的放射性标记反应是生物医学研究中重要的化学工具,尤其是在探针构建中。在此,制备了三个18 F-标记的乙烯基砜。特别地,18 F-PEG1-VS((((2-(2-(fluoro- 18 F)乙氧基)乙基)磺酰基)乙烷)不仅可以对含有-XH(X = S,NH)的生物活性分子进行化学选择性标记,但在体外和活体小鼠中也会与红细胞发生反应,从而具有潜在的细胞追踪应用。另外,发现这些亲水剂有效地穿过血脑屏障(BBB)并位于小脑区域。总之,18 F标记的乙烯基砜为PET探针的构建提供了一个多功能的平台。
更新日期:2020-11-18
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