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• W4311863231 abstract "Rationale: Conventional 18F-labeling methods that demand substrate pre-modification or lengthy radiosynthesis procedures have impeded the visualization and translation of numerous biomolecules, as biomarkers or ligands, using modern positron emission tomography techniques in vivo. Moreover, 18F-labeled biomolecules in high molar activity (Am) that are indispensable for sensitive imaging could be only achieved under strict labeling conditions. Methods: Herein, 18F-labeled fluorothiophosphate (FTP) synthons in high Am have been generated rapidly in situ in reaction solutions with < 5% water via nucleophilic substitution by wet [18F]F-, which required minimal processing from cyclotron target water. Results: Various 18F-labeled FTP synthons have been prepared in 30 sec at room temperature with high radiochemical yields > 75% (isolated, non-decay-corrected). FTP synthons with unsaturated hydrocarbon or activated ester group can conjugate with typical small molecules, peptides, proteins, and metallic nanoparticles. 337-517 GBq μmol-1 Am has been achieved for 18F-labeled c(RGDyK) peptide using an automatic module with 37-74 GBq initial activity. Conclusion: The combination of high 18F-fluorination efficiency of FTP synthons and following mild conjugation condition provides a universal simplified one-pot 18F-labeling method for broad unmodified biomolecular substrates." @default.
• W4311863231 created "2023-01-01" @default.
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• W4311863231 date "2023-01-01" @default.
• W4311863231 modified "2023-09-25" @default.
• W4311863231 title "Simplified one-pot ¹⁸F-labeling of biomolecules with <i>in situ</i> generated fluorothiophosphate synthons in high molar activity" @default.
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• W4311863231 doi "https://doi.org/10.7150/thno.79452" @default.
• W4311863231 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36632226" @default.
• W4311863231 hasPublicationYear "2023" @default.
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