1. Serine-Selective Bioconjugation
- Author
-
Vantourout, Julien C., Rao Adusumalli, Srinivasa, Knouse, Kyle W., Flood, Dillon, Ramirez, Antonio, M. 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., and Baran, Phil S.
- Subjects
3. Good health - Abstract
The first general method for the rapid, chemoselective, and modular functionalization of serine residues in native polypeptides is reported. Using a reagent platform based on P(V) oxidation state, this redox-economic 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 enabled by this expansion of the toolbox of site-selective bioconjugation methods.