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i Pr 2 EtN in
Scheme 13 Active ester coupling of the three-component vaccine: a) HOBt,
DMF, b) subsequent removal of the protecting groups.
51
Scheme 14 Three-component vaccine containing a MUC1 partial sequence, a T-cell
epitope from polio virus and a lipopeptide ligand of toll-like receptor 2.
cysteine was coupled. This N-terminal cysteine was then used for a native
chemical ligation (NCL) 67 with a Pam 3 Cys lipopeptide in a liposome
preparation to give the three-component vaccine 51 (Scheme 14).
The vaccine 51 was administered in form of liposomes to transgenic
mice which express human MUC1. The mice reacted with strong immune
responses. The immunised mice after
challenging with murine
 
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