Globo H is a tumor-associated carbohydrate antigen (TACA), which serves as a valuable target for antitumor vaccine or cancer immunotherapies. However, most TACAs are T-cell-independent, and they cannot induce powerful immune response due to their poor immunogenicity. To address this problem, herein, several Globo H analogues with modification on the N-acyl group were prepared through a preactivation-based glycosylation strategy from the non-reducing end to the reducing end. These modified Globo H derivatives were then conjugated with carrier protein CRM197 to form glycoconjugates as anticancer vaccine candidates, which were used in combination with adjuvant glycolipid C34 for immunological studies. The immunological effects of these synthetic vaccine candidates were evaluated on Balb/c mice. The results showed that the fluorine-modified N-acyl Globo H conjugates can induce higher titers of IgG antibodies that can recognize the naturally occurring Globo H antigen on the surface of cancer cells and can eliminate cancer cells in the presence of a complement, indicating the potential of these synthetic glycoconjugates as anticancer vaccine candidates.

中文翻译：

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N-酰基修饰的 Globo H 衍生物作为抗癌疫苗候选物的合成和免疫学评价

Globo H 是一种肿瘤相关碳水化合物抗原 (TACA)，可作为抗肿瘤疫苗或癌症免疫疗法的重要靶标。然而，大多数 TACA 不依赖于 T 细胞，并且由于其免疫原性差，它们不能诱导强大的免疫反应。为了解决这个问题，在此，对N进行了修改的几个 Globo H 类似物-酰基通过基于预活化的糖基化策略从非还原端到还原端制备。然后将这些修饰的 Globo H 衍生物与载体蛋白 CRM197 缀合以形成糖缀合物作为抗癌疫苗候选物，其与佐剂糖脂 C34 组合用于免疫学研究。在 Balb/c 小鼠身上评估了这些合成候选疫苗的免疫学效果。结果表明，氟修饰的N-酰基 Globo H 偶联物可以诱导更高滴度的 IgG 抗体，该抗体可以识别癌细胞表面天然存在的 Globo H 抗原，并且可以在补体存在的情况下消除癌细胞，表明这些合成糖缀合物作为抗癌疫苗候选物的潜力。