Synthesis of Heavily Glycosylated Peptide Thioester
Synthesis of Heavily Glycosylated Peptide Thioester
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DOI：
10.1080/07328301003743640
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发表时间：
2010-01-01
影响因子：
1
通讯作者：
Kajihara, Yasuhiro
中科院分区：
文献类型：
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作者：
Hirano, Kiriko;Kajihara, Yasuhiro
促红细胞生成素（EPO）需要高度糖基化才能在体内发挥其生物活性。为了合成高度糖基化的EPO类似物，相应的糖基化肽硫酯对于通过天然化学连接制备糖基化的整个EPO肽骨架是必需的。在构建了对应于EPO中1-32个氨基酸序列的肽硫酯后，我们的目标是通过卤代乙酰胺方法将三种复合型双触角唾液酸寡糖掺入该肽硫酯。反应得到所需的高度糖基化的肽硫酯。
Erythropoietin (EPO) needs to be heavily glycosylated to exhibit its bioactivity in vivo. In order to synthesize heavily glycosylated EPO analogues, corresponding glycosylated peptide thioesters are essential to prepare glycosylated whole EPO peptide backbones through native chemical ligation. After construction of the peptide thioester corresponding to the 1-32 amino acid sequence in EPO, we aimed to incorporate three complex-type biantennary sialyloligosaccharides to this peptide thioester by the haloacetamide method. The reaction afforded the desired heavily glycosylated peptide thioester.