论文部分内容阅读
目的 为获得精确定位糖基化糖肽 ,合成O 乙酰氨基半乳糖基化氨基酸 ,作为糖肽固相合成的原料。方法 利用环状糖结构的半缩醛羟基可与含侧链羟基氨基酸的羟基形成糖苷键 ,用化学方法 ,使过乙酰化GalNAc与氨基被 9 Fluorenylmethoxycarbonyl (N α Fmoc)保护的丝氨酸或苏氨酸连接。结果 反应产物通过反相制备HPLC纯化后 ,可作为O 连接糖肽合成构建单位 (Buildingblocks)在固相多肽合成仪上合成所需的病毒或肿瘤相关糖肽 ,并可进一步研究其生物学活性。结论 本法相对易操作 ,重复性好 ,收益率也较高 ,更重要的是糖基化的均一性好 ,对推动糖肽研究具有重要意义
OBJECTIVE To obtain the precise positioning of glycosylated glycopeptides, O-acetylamino galactosylated amino acids were synthesized and used as raw materials for glycopeptide solid-phase synthesis. Methods The hemiacetal hydroxyl groups of the cyclic sugar structure can form glycosidic bonds with the hydroxyl groups of the side chain hydroxyl amino acids and the chemical reaction of the peracetylated GalNAc with the serine or threonine whose amino group is protected by 9 Fluorenylmethoxycarbonyl (N α Fmoc) connection. Results The reaction products were purified by reverse-phase preparative HPLC and used as O-linked glycopeptide building blocks (Building blocks) to synthesize the desired virus or tumor-associated glycopeptides on a solid-phase peptide synthesizer and to further investigate their biological activity. Conclusion This method is relatively easy to operate with good repeatability and high yield, and more importantly, the glycosylation is of good homogeneity, which is of great significance for the promotion of glycopeptide research