Synthesis and biological evaluation of a multiantigenic Tn/TF-containing glycopeptide mimic of the tumor-related MUC1 glycoprotein

The glycopeptide construct shown was synthesized using a convergent strategy based on oxime chemical ligation. It is composed of a universal T-helper and three tumor-related epitopes from the human mucin MUC1, an non-glycosylated repeat unit, and two units glycosylated with the Tn and TF epitopes, respectively. In association with a mild adjuvant suitable for human therapy, this construct elicited a strong specific immune response in mice, directed against natural tumor-associated structures.