Design of Novel ¹⁸F-Labeled Amino Acid Tracers Using Sulfur ¹⁸F-Fluoride Exchange Click Chemistry.

ABSTRACT: [¹⁸F]Gln-OSO₂F, [¹⁸F]Arg-OSO₂F, and [¹⁸F]FSY-OSO₂F were designed by introducing sulfonyl ¹⁸F-fluoride onto glutamine, arginine, and tyrosine, respectively. [¹⁸F]FSY-OSO₂F can be prepared directly by sulfur ¹⁸F-fluoride exchange, while [¹⁸F]Gln-OSO₂F and [¹⁸F]Arg-OSO₂F require a two-step labeling method. Those tracers retain their typical transport characteristics for unmodified amino acids. Both PET imaging and biodistribution confirmed that [¹⁸F]FSY-OSO₂F visualized MCF-7 and 22Rv1 subcutaneous tumors with high contrast, and its tumor-to-muscle ratio was better than that of [¹⁸F]FET. However, [¹⁸

SUBMITTER: Huang Y 

PROVIDER: S-EPMC10860173 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature