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Synthetic Multivalent Glycopeptide‐Lipopeptide Antitumor Vaccines: Impact of the Cluster Effect on the Killing of Tumor Cells
Author(s) -
Cai Hui,
Sun ZhanYi,
Chen MeiSha,
Zhao YuFen,
Kunz Horst,
Li YanMei
Publication year - 2014
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201308875
Subject(s) - lipopeptide , glycopeptide , adjuvant , antigen , muc1 , epitope , immune system , antibody , chemistry , cytotoxicity , cancer research , immunology , biology , in vitro , biochemistry , antibiotics , bacteria , genetics
Multivalent synthetic vaccines were obtained by solid‐phase synthesis of tumor‐associated MUC1 glycopeptide antigens and their coupling to a Pam 3 Cys 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‐T N antigen showed a significant cluster effect. It induced in mice prevailing IgG 2a 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.