Synthesis of Tn/T Antigen MUC1 Glycopeptide BSA Conjugates and Their Evaluation as Vaccines

The tumor‐associated mucin MUC1 over‐expressed in most epithelial tumor tissues is considered a promising target for immunotherapy. The extracellular part of MUC1 contains a domain of numerous tandem repeats of the amino acid sequence HGVTSAPDTRPAPGSTAPPA, including five potential O‐glycosylation sites. In this study, T9 and S15 have been chosen as the positions of glycosylation. The glycopeptides N‐terminally equipped with a triethylene glycol spacer were synthesized by microwave‐assisted Fmoc solid‐phase peptide synthesis. After detachment from the resin and deprotection, the MUC1 glycopeptides were conjugated to bovine serum albumin (BSA). To evaluate the immunological properties, balb/c mice were immunized with these BSA vaccines. Tumor‐associated MUC1 glycopeptides are attractive targets for antitumor immunotherapy. MUC1 glycopeptides containing the Tn and T antigen side chain were conjugated with bovine serum albumin. Thesevaccines were used for immunization of balb/c mice, and the immune responses were evaluated by enzyme‐linked immunoabsorbent assay.