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

Abstract 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 proteinCRM197. The immunological results of these glycoconjugatesindicated that 6 –CRM197 elicited higher titers of antibodies which cross-reacted with native Tn antigenthan 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 glycoconjugateas an anticancer vaccine.