Synthesis and immunological evaluation of N-acyl modified Tn analogues as anticancer vaccine candidates.

Tumor-associated carbohydrate antigens (TACAs), which are aberrantly expressed on the surface of tumor cells, are important targets for anticancer vaccine development. Herein, several N-acyl modified Tn analogues were synthesized and conjugated with carrier protein CRM197. The immunological results of these glycoconjugates indicated that 6-CRM197 elicited higher titers of antibodies which cross-reacted with native Tn antigen than the unmodified 2-CRM197 did. The IFN-γ-producing frequency of lymphocytes in mice treated with 6-CRM197 was obviously increased, compared to that of mice vaccinated with 2-CRM197 (p=0.016), which was typically associated with the Th1 response. Moreover, the elicited antisera against antigen 6-CRM197 reacted strongly with the Tn-positive tumor cells, implying the potential of this glycoconjugate as an anticancer vaccine.