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通过在树脂上引入取代基,在主链酰胺氮上带有甲基及更大取代基的肽的固相合成。

Solid-Phase Synthesis of Peptides with Methyl and Larger Substituents on Backbone Amide Nitrogens via On-Resin Incorporation of the Substituents.

作者信息

Morimoto Jumpei, Yokomine Marin, Yamazaki Takaya, Sando Shinsuke

机构信息

Department of Chemistry and Biotechnology, Graduate School of Engineering, The University of Tokyo, Tokyo, Japan.

Department of Bioengineering, Graduate School of Engineering, The University of Tokyo, Tokyo, Japan.

出版信息

Methods Mol Biol. 2025;2931:61-73. doi: 10.1007/978-1-0716-4562-8_6.

Abstract

Introducing substituents on backbone amide nitrogens of peptides is an attractive strategy to improve the pharmacological properties of peptides. Here, we describe a solid-phase synthetic method for peptides with various substituents on backbone amide nitrogens. The method utilizes the procedures for introducing substituents on resin, which facilitates introducing diverse functional groups on backbone amide nitrogens.

摘要

在肽的主链酰胺氮上引入取代基是改善肽类药物性质的一种有吸引力的策略。在此,我们描述了一种用于在主链酰胺氮上带有各种取代基的肽的固相合成方法。该方法利用了在树脂上引入取代基的步骤,这有助于在主链酰胺氮上引入多种官能团。

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