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Modification of Oligopeptides on Aspartic Acid or Lysine Residues by Solid-Phase Synthesis through On-Resin Side-Chain Conjugation
Synlett ( IF 1.7 ) Pub Date : 2018-10-24 , DOI: 10.1055/s-0037-1611060 Hongyan Shen 1 , Xibo Ning 1 , Di Liu 1 , Shimiao Liu 1 , Mingjie Zhang 2
Synlett ( IF 1.7 ) Pub Date : 2018-10-24 , DOI: 10.1055/s-0037-1611060 Hongyan Shen 1 , Xibo Ning 1 , Di Liu 1 , Shimiao Liu 1 , Mingjie Zhang 2
Affiliation
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On-resin side-chain conjugations of various moieties to oligopeptides were performed through an orthogonal protecting protocol using side-chain-protecting groups for aspartic acid or lysine that could be selectively removed on-resin. Various types of modification, such as PEGylation, biotinylation, glycosylation, or fluorophore-labeling of peptides, were realized by using this strategy. The formation of ester, amide, hydrazide, and thiourea bonds was accomplished through the on-resin conjugation. Our work provides an improved and convenient solid-phase synthetic protocol for the modification of oligopeptides on their aspartic acid or lysine residues. This is a universal and practical method that is expected to increase the potential application of peptide-related drugs.
中文翻译：
通过树脂上侧链共轭固相合成修饰天冬氨酸或赖氨酸残基上的寡肽
各种部分与寡肽的树脂侧链缀合是通过正交保护协议进行的，使用侧链保护基团可以在树脂上选择性去除天冬氨酸或赖氨酸。使用该策略实现了各种类型的修饰，例如肽的聚乙二醇化、生物素化、糖基化或荧光团标记。酯、酰胺、酰肼和硫脲键的形成是通过树脂上的共轭作用完成的。我们的工作为寡肽在其天冬氨酸或赖氨酸残基上的修饰提供了一种改进且方便的固相合成方案。这是一种通用且实用的方法，有望增加肽相关药物的潜在应用。
更新日期：2018-10-24
中文翻译：
通过树脂上侧链共轭固相合成修饰天冬氨酸或赖氨酸残基上的寡肽
各种部分与寡肽的树脂侧链缀合是通过正交保护协议进行的，使用侧链保护基团可以在树脂上选择性去除天冬氨酸或赖氨酸。使用该策略实现了各种类型的修饰，例如肽的聚乙二醇化、生物素化、糖基化或荧光团标记。酯、酰胺、酰肼和硫脲键的形成是通过树脂上的共轭作用完成的。我们的工作为寡肽在其天冬氨酸或赖氨酸残基上的修饰提供了一种改进且方便的固相合成方案。这是一种通用且实用的方法，有望增加肽相关药物的潜在应用。
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