Synthesis of N-Linked glycopeptides using convergent enzymatic glycosylation combined with SPPS

Abstract

Glycosylation of peptides and proteins has emerged as a promising strategy to improve the pharmacokinetic profile of peptide-and protein-based therapeutics. The synthesis of pure homogeneous N-linked glycopeptides and glycoproteins is a challenging task, and efficient routes to access them are in high demand. Endo-b-N-acetylglucosaminidise catalysed glycosylation of N-acetylglucosaminetagged peptides, using activated oligosaccharide oxazolines as donors, has recently attracted attention due to the relative simplicity by which the process convergently affords glycoconjugates with complete control of stereo- and regioselectivity. Herein, a brief review of some examples of recent enzyme-mediated N-glycosylation used to synthesise glycopeptides with therapetic potential is provided.