Covalent protein conjugation facilitates the study of biological processes and the synthesis of therapeutic biomacromolecules. A method that uses vinyl thianthrenium reagents for the site-selective formation of highly reactive episulfonium species on proteins is demonstrated. These in situ-formed intermediates react with diverse nucleophiles, providing access to protein conjugates in one step without purification.
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This is a summary of: Hartmann, P. et al. Chemoselective umpolung of thiols to episulfoniums for cysteine bioconjugation. Nat. Chem. https://doi.org/10.1038/s41557-023-01388-7 (2023).
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Site-selective episulfonium formation on protein surfaces. Nat. Chem. 16, 312–313 (2024). https://doi.org/10.1038/s41557-024-01445-9
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DOI: https://doi.org/10.1038/s41557-024-01445-9
