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Development of 18F-Labeled hydrophilic trans-cyclooctene as a bioorthogonal tool for PET probe construction. 2023
Muyun Xu, and
Xinrui Ma, and
Jessica E Pigga, and
He Zhang, and
Shuli Wang, and
Weiling Zhao, and
Huaifu Deng, and
Anna M Wu, and
Rihe Liu, and
Zhanhong Wu, and
Joseph M Fox, and
Zibo Li
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. zhanhong_wu@med.unc.edu.
We report the development of a hydrophilic 18F-labeled a-TCO derivative [18F]3 (log P = 0.28) through a readily available precursor and a single-step radiofluorination reaction (RCY up to 52%). We demonstrated that [18F]3 can be used to construct not only multiple small molecule/peptide-based PET agents, but protein/diabody-based imaging probes in parallel.
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