Ribosomal incorporation of N-acetyl-3,5-bis(chloromethyl)benzylthio-L-alanine for developing an mRNA-displayed bicyclic peptide library cyclized via 1,3,5-tris(methyl)benzene.

IF 2.9 3区化学 Q1 CHEMISTRY, ORGANIC

Organic & Biomolecular Chemistry Pub Date : 2025-05-27 DOI:10.1039/d5ob00693g

Maolin Li, Haipeng Yu, Jie Cheng, Wenfeng Cai, Youming Zhang, Yizhen Yin

引用次数: 0

Abstract

We report a novel method for constructing an mRNA-displayed bicyclic peptide library cyclized through 1,3,5-tris(methyl)benzene by ribosomally incorporating N-acetyl-3,5-bis(chloromethyl)benzylthio-L-alanine, enabling the selection of bicyclic peptides against specific targets. Using this method, we successfully identified bicyclic peptides that bind to human Trop2 and VEGF165, providing a new strategy for selecting bicyclic peptides cyclized by trimethylbenzene.

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核糖体结合n -乙酰-3,5-二（氯甲基）苄基硫代- l-丙氨酸，形成经1,3,5-三（甲基）苯环化的mrna双环肽文库。

我们报道了一种新的方法，通过核糖体结合n -乙酰基-3,5-二（氯甲基）苄基硫代- l-丙氨酸，构建一个通过1,3,5-三（甲基）苯环化的mrna展示双环肽文库，使双环肽能够针对特定靶点进行选择。利用该方法，我们成功地鉴定了与人Trop2和VEGF165结合的双环肽，为三甲基苯环化双环肽的选择提供了一种新的策略。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Organic & Biomolecular Chemistry 化学-有机化学

CiteScore

5.50

自引率

9.40%

发文量

1056

审稿时长

1.3 months

期刊介绍： Organic & Biomolecular Chemistry is an international journal using integrated research in chemistry-organic chemistry. Founded in 2003 by the Royal Society of Chemistry, the journal is published in Semimonthly issues and has been indexed by SCIE, a leading international database. The journal focuses on the key research and cutting-edge progress in the field of chemistry-organic chemistry, publishes and reports the research results in this field in a timely manner, and is committed to becoming a window and platform for rapid academic exchanges among peers in this field. The journal's impact factor in 2023 is 2.9, and its CiteScore is 5.5.