{"title":"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。","authors":"Maolin Li, Haipeng Yu, Jie Cheng, Wenfeng Cai, Youming Zhang, Yizhen Yin","doi":"10.1039/d5ob00693g","DOIUrl":null,"url":null,"abstract":"<p><p>We report a novel method for constructing an mRNA-displayed bicyclic peptide library cyclized through 1,3,5-tris(methyl)benzene by ribosomally incorporating <i>N</i>-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.</p>","PeriodicalId":96,"journal":{"name":"Organic & Biomolecular Chemistry","volume":" ","pages":""},"PeriodicalIF":2.9000,"publicationDate":"2025-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Ribosomal incorporation of <i>N</i>-acetyl-3,5-bis(chloromethyl)benzylthio-L-alanine for developing an mRNA-displayed bicyclic peptide library cyclized <i>via</i> 1,3,5-tris(methyl)benzene.\",\"authors\":\"Maolin Li, Haipeng Yu, Jie Cheng, Wenfeng Cai, Youming Zhang, Yizhen Yin\",\"doi\":\"10.1039/d5ob00693g\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>We report a novel method for constructing an mRNA-displayed bicyclic peptide library cyclized through 1,3,5-tris(methyl)benzene by ribosomally incorporating <i>N</i>-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.</p>\",\"PeriodicalId\":96,\"journal\":{\"name\":\"Organic & Biomolecular Chemistry\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":2.9000,\"publicationDate\":\"2025-05-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Organic & Biomolecular Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1039/d5ob00693g\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Organic & Biomolecular Chemistry","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1039/d5ob00693g","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
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.
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.
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.