Mucin Glycopeptide-Protein Conjugates - Promising Antitumor Vaccine Candidates

作者：Palitzsch Boejrn^*; Glaffig Markus; Kunz Horst

来源：Israel Journal of Chemistry, 2015, 55(3-4): 256-267.

DOI：10.1002/ijch.201400131

• antitumor vaccines
• glycopeptides
• solid-phase synthesis
• tetanus toxoid conjugates
• tumor-associated MUC1

Recent efforts towards the development of synthetic glycopeptide vaccines, which aim at the active immunization of patients against their own tumor tissues, are outlined. To achieve sufficient tumor selectivity, glycopeptides of the tandem repeat region of tumor-associated mucin, MUC1, have been synthesized. Since the endogenous structures usually exert low immunogenicity, these glycopeptide antigens, as B-cell epitopes, were conjugated with immunostimulating components. In the present short review, work is outlined in which the MUC1 B-cell epitope peptides are conjugated with bovine serum albumin ( BSA), keyhole limpet hemocyanin ( KLH), or tetanus toxoid ( TTox). In particular, the synthetic vaccines based on tetanus toxoid induce very strong tolerance-breaking immune responses in mice. The induced antibodies of the IgG type indicate the installation of an immunological memory. In addition, these antibodies strongly bind to human breast tumor cells in culture, demonstrated by flow cytometry experiments, and also to the tumor cells in mammary carcinoma tissues.

• 出版日期2015-4