Synthetic Multivalent Glycopeptide‐Lipopeptide Antitumor Vaccines: Impact of the Cluster Effect on the Killing of Tumor Cells |
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| Authors: | Dr Hui Cai Zhan‐Yi Sun Mei‐Sha Chen Prof Dr Yu‐Fen Zhao Prof Dr Horst Kunz Prof Dr Yan‐Mei Li |
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| Affiliation: | 1. Key Lab of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing 100084 (P.R. China);2. Institute of organic Chemistry, Johannes Gutenberg‐University of Mainz, Duesbergweg 10‐14, 55128 Mainz (Germany) |
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| Abstract: | Multivalent synthetic vaccines were obtained by solid‐phase synthesis of tumor‐associated MUC1 glycopeptide antigens and their coupling to a Pam3Cys lipopeptide through click reactions. These vaccines elicited immune responses in mice without the use of any external adjuvant. The vaccine containing four copies of a MUC1 sialyl‐TN antigen showed a significant cluster effect. It induced in mice prevailing IgG2a antibodies, which bind to MCF‐7 breast tumor cells and initiate the killing of these tumor cells by activation of the complement‐dependent cytotoxicity complex. |
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| Keywords: | antigens antitumor agents cytotoxicity multivalent glycopeptides vaccines |
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