alpha-Selective Lysine Ligation and Application in Chemical Synthesis of Interferon Gamma
alpha-Selective Lysine Ligation and Application in Chemical Synthesis of Interferon Gamma
复制标题
α-选择性赖氨酸连接及其在干扰素γ化学合成中的应用
DOI：
10.1021/acs.orglett.9b00980
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发表时间：
2019
期刊：
影响因子：
5.2
通讯作者：
Dong Suwei
中科院分区：
文献类型：
--
作者：
Dao Yuankun;Han Lin;Wang Hamann;Dong Suwei
本文报道了一种无痕β-巯基辅助的N-端赖氨酸肽的α-选择性连接反应。在这种基于连接-脱硫的方案中，赖氨酸的ε-胺不受保护，从而提高了整体合成效率，避免了制备大肽和蛋白质时的苛刻反应。这种方法的适用性已被证明在酸不稳定的治疗性蛋白质，干扰素γ的合成，合成蛋白质的抗癌活性也进行了评估。
A traceless β-mercaptan-assisted α-selective ligation ofN-terminal lysine-containing peptides has been developed. In this ligation–desulfurization-based protocol, the ε-amine of lysine is free of protection, thus improving the overall synthetic efficiency and avoiding harsh reactions in preparing large peptides and proteins. The applicability of this methodology has been demonstrated in the synthesis of an acid-labile therapeutic protein, interferon gamma, and the anticancer activity of synthetic protein has also been evaluated.