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

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• 作者：Chengcheng Song^a ; ^b ; ^&dagger ; ; Shuang Sun^b ; ^&dagger ; ; Chang-Xin Huo^b ; Qin Li^b ; Xiu-Jing Zheng^b ; Guihua Tai^a ; Yifa Zhou^a ; ^{zhouyf383@nenu.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Xin-Shan Ye^b ; ^{xinshan@bjmu.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Carbohydrate ; Vaccine ; Tn antigen ; Glycoconjugate ; Anticancer
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：24
• 期：4
• 页码：915-920
• 全文大小：842 K

文摘

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.