F-标记的亲水性环辛烯的开发作为 PET 探针构建的生物正交工具。
Development of F-Labeled hydrophilic -cyclooctene as a bioorthogonal tool for PET probe construction.
机构信息
Department of Radiology, Biomedical Research Imaging Center, and Lineberger Comprehensive Cancer Center, the University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, 27599, USA.
Department of Chemistry, the University of Delaware, Newark, Delaware, 19716, USA.
出版信息
Chem Commun (Camb). 2023 Dec 5;59(97):14387-14390. doi: 10.1039/d3cc04212j.
Abstract
We report the development of a hydrophilic F-labeled a-TCO derivative [F]3 (log = 0.28) through a readily available precursor and a single-step radiofluorination reaction (RCY up to 52%). We demonstrated that [F]3 can be used to construct not only multiple small molecule/peptide-based PET agents, but protein/diabody-based imaging probes in parallel.
摘要
我们报道了一种亲水性 F 标记的 a-TCO 衍生物 [F]3（logD = 0.28）的开发，该衍生物通过易得的前体和单步放射性氟化反应（RCY 高达 52%）得到。我们证明了 [F]3 不仅可以用于构建多种小分子/肽基 PET 试剂，还可以用于同时构建基于蛋白质/双抗体的成像探针。
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