Serine-Selective Bioconjugation Vantourout, Julien C Rao Adusumalli, Srinivasa Knouse, Kyle W. Flood, Dillon Ramirez, Antonio Muñoz Padial, Natalia Israte, Alena Maziarz, Katarzyna deGruyter, Justine N. Merchant, Rohan R. Qiao, Jennifer X. Schmidt, Michael A. Deery, Michael J. Eastgate, Martin D. Dawson, Philip E. Bernardes, Gonçalo J. L. Baran, Phil S. This Communication reports the first general method for rapid, chemoselective, and modular functionalization of serine residues in native polypeptides, which uses a reagent platform based on the P(V) oxidation state. This redox-economical approach can be used to append nearly any kind of cargo onto serine, generating a stable, benign, and hydrophilic phosphorothioate linkage. The method tolerates all other known nucleophilic functional groups of naturally occurring proteinogenic amino acids. A variety of applications can be envisaged by this expansion of the toolbox of site-selective bioconjugation methods. 2021-03-16T13:24:24Z 2021-03-16T13:24:24Z 2020-09-23 info:eu-repo/semantics/article J. Am. Chem. Soc. 2020, 142, 41, 17236–17242 http://hdl.handle.net/10481/67274 https://pubs.acs.org/doi/10.1021/jacs.0c05595 eng http://creativecommons.org/licenses/by-nc-nd/3.0/es/ info:eu-repo/semantics/openAccess Creative Commons Attribution-NonCommercial-NoDerivs 3.0 License Atribución-NoComercial-SinDerivadas 3.0 España American Chemical Society