Tuning of protease resistance in oligopeptides through N-alkylation.
Tuning of protease resistance in oligopeptides through N-alkylation.
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通过 N-烷基化调节寡肽的蛋白酶抗性。
DOI：
10.1039/c8cc04407d
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发表时间：
2018
期刊：
影响因子：
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通讯作者：
Hawker,CraigJ
中科院分区：
文献类型：
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作者：
Kaminker,Revital;Anastasaki,Athina;Gutekunst,WillR;Luo,Yingdong;Lee,Sang-Ho;Hawker,CraigJ
氨基酸的N-甲基化是在天然和合成肽中产生蛋白酶抗性的有效方法。然而，除N-甲基以外的烷基取代基尚未被广泛研究。在这里，我们准备和检查一系列的N-取代的肽，其中的烷基基团的大小和长度进行调制。这些设计见解为调节寡肽中的蛋白水解提供了独特的模块化手柄。
N-Methylation of amino acids is an effective way to create protease resistance in both natural and synthetic peptides. However, alkyl substituents other than N-methyl have not been extensively studied. Here, we prepare and examine a series of N-substituted peptides in which the size and length of the alkyl group is modulated. These design insights provide a unique and modular handle for tuning proteolysis in oligopeptides.