Solid phase diversity-oriented lysine modification of cyclic peptides

Abstract

Herein, we report a novel strategy for diversity-oriented lysine modification of cyclic peptides based on the orthogonal alkylation of the lysine residues. All steps can be achieved in the solid phase with satisfying conversions. Notably, we demonstrated that the tether modification could help to improve the cellular uptake of peptides.

Keywords: cyclic peptides; diversity oriented; lysine modification.