摘要
Tumor-associated carbohydrate antigens （TACAs）, important molecular markers on tumor cells, are major targets for the development of anti-cancer vaccines. However, due to the immunotolerance and weak immunogenicity, native TACAs cannot induce powerful immune response. The use of modified TACAs such as N-glycosides could be an alternative strategy to overcome this problem. Herein, the synthesis of N（OMe）-linked analogue of tumor-associated disaccharide antigen Thomsen-Friedenreich （TF） by the glycosylation reaction is described.
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。
基金
Grant from the Ministry of Science and Technology of China(Grant No.2012ZX09502001-001)
the National Natural Science Foundation of China(Grant No.81172916)
