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肿瘤相关糖抗原是肿瘤细胞表面重要的分子标志物之一,也是抗肿瘤糖疫苗研发的主要靶标。然而,由于其作为自身抗原的免疫耐受以及较弱的免疫原性,天然的肿瘤相关糖抗原通常无法激发有效的免疫反应,而非天然的氮苷抗原类似物可能会成为解决该问题的有效途径之一。目前氮苷类似物用于肿瘤疫苗的研究未见文献报道。因此,在本篇文章中,我们以半乳糖溴代糖为供体、甲氧基胺取代的单糖为受体通过偶联反应成功合成了肿瘤相关二糖抗原TF的氮苷类似物。
Tumor-associated carbohydrate antigen is one of the important molecular markers on the surface of tumor cells, and is also the main target for antitumor sugar vaccine research and development. However, native tumor-associated carbohydrate antigens are often unable to elicit an effective immune response due to their immune tolerance as a self-antigen and weak immunogenicity, whereas non-natural alanoside analogs may be effective in solving this problem One of the ways. At present, the research on the use of alanosine analogue for tumor vaccine has not been reported in the literature. Therefore, in this paper, we have successfully synthesized the alanine analogs of tumor-associated disaccharide antigen TF by coupling reaction using galactose bromide as donor and methoxyamine substituted monosaccharide as acceptor.