at Peking University School of Pharmaceutical Sciences
​​​​the dong research group
8. α-Selective Lysine Ligation and Application in Chemical Synthesis of Interferon Gamma
Org. Lett. 2019, 21, 3265–3270
Yuankun Dao, Lin Han, Hanxuan Wang, and Suwei Dong*

A traceless β-mercaptan-assisted α-selective ligation of N-terminal lysine-containing peptides has been developed. In this ligation–desulfurization-based protocol, the ε-amine of lysine is free of protection, thus improving the overall synthetic efficiency and avoiding harsh reactions in preparing large peptides and proteins. The applicability of this methodology has been demonstrated in the synthesis of an acid-labile therapeutic protein, interferon gamma, and the anticancer activity of synthetic protein has also been evaluated.