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Synthetic MUC1 Antitumor Vaccine Candidates with Varied Glycosylation Pattern Bearing R/S‐configured Pam3CysSerLys4
Authors:Lei Shi  Dr. Hui Cai  Dr. Zhi‐Hua Huang  Zhan‐Yi Sun  Prof. Dr. Yong‐Xiang Chen  Prof. Dr. Yu‐Fen Zhao  Prof. Dr. Horst Kunz  Prof. Dr. Yan‐Mei Li
Affiliation:1. Key Laboratory of Bioorganic Phosphorus Chemistry and, Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing, China;2. Institute of Organic Chemistry, Johannes Gutenberg University of Mainz, Mainz, Germany
Abstract:The Toll‐like receptor 2 ligand Pam3CysSer is of particular interest for the construction synthetic vaccines because of its ability to stimulate of the innate immune system. Such vaccines usually comprise Pam3CysSer with the natural R‐configuration at the glycerol 2‐position. Pam3CysSer peptide vaccines with natural configuration have been shown to be more efficient than the corresponding R/S diastereomers. In order to clarify whether the effect of the configuration of Pam3Cys on the immune response also applies to glycopeptide vaccines, MUC1 glycopeptide–lipopeptide vaccines bearing either R‐ or R/S‐configured Pam3CysSerLys4 were compared for their immunological effects. In order to find out whether glycosylated MUC1 tandem repeat domains comprise not only B‐cell epitopes but also T‐cell epitopes, two‐component vaccines containing the Pam3CysSerLys4 lipopeptide and MUC1 glycopeptides with various glycosylation patterns were synthesized, and their immune reactions in mice were studied.
Keywords:antibodies  antitumor agents  MUC1 glycopeptides  toll-like receptor   2 ligand  tumor-associated carbohydrate antigens
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