Graduate School of Life Science, Hokkaido University, N22, W11 Kita-ku, Sapporo, Japan.
Org Biomol Chem. 2012 Feb 28;10(8):1612-7. doi: 10.1039/c2ob06532k. Epub 2012 Jan 11.
A standardized and smooth protocol for solid-phase glycopeptides synthesis under microwave irradiation was developed. Double activation system was proved to allow for highly efficient coupling of Tn-Ser/Thr and bulky core 2-Ser/Thr derivatives. Versatility and robustness of the present strategy was demonstrated by constructing a Mucine-1 (MUC1) fragment and glycosylated fragments of tau protein. The success of this approach relies on the combination of microwave energy, a resin consisting totally of polyethylene glycol, a low excess of sugar amino acid and the "double activation" method.
开发了一种在微波辐射下固相糖肽合成的标准化和流畅的方案。双激活系统被证明可以有效地偶联 Tn-Ser/Thr 和大体积核心 2-Ser/Thr 衍生物。通过构建粘蛋白-1（MUC1）片段和tau 蛋白的糖基化片段，证明了本策略的多功能性和稳健性。这种方法的成功依赖于微波能量、完全由聚乙二醇组成的树脂、糖氨基酸的低过量和“双激活”方法的结合。
