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In this study, we report (1) a scalable, systematic, and general synthetic approach for the supply of ribosomally synthesized and post-translationally modified peptides (RiPPs) bearing Tyr–Trp cross-linkages, and (2) the comprehensive expansion of novel chemical space through their skeletal diversification. In recent years, numerous biaryl-containing peptides have been discovered, and some of these RiPPs exhibit potent biological activities. However, despite the high metabolic stability and strong target protein binding generally attributed to biaryl RiPPs, their significant strain and rigidity have limited the availability of general synthetic methods. Here, we demonstrate the high versatility of modular synthetic strategies for the construction of RiPPs and achieve the synthesis of a variety of RiPPs containing Tyr–Trp cross-linkages. Furthermore, skeletal diversification via scaffold hopping enables access to artificial RiPP scaffolds incorporating quinazoline and quinoline motifs, whose preparation has previously been challenging.

権利情報:

• Creative Commons BY Attribution 4.0 International
  

キーワード: Ribosomally Synthesized and Post-translationally Modified Peptides, Skeletal Editing, Scaffold Hopping, Larock Macrocyclization, C–H Arylation

刊行年月日: 2026-05-26

出版者: Royal Society of Chemistry (RSC)

掲載誌:

• Chemical Science (ISSN: 20416520) vol. 17 issue. 28 p. 13835-13849

研究助成金:

• National Natural Science Foundation of China NSFC25SC26
• Research Grants Council, University Grants Committee 26302024
• Research Grants Council, University Grants Committee 16306525
• Hong Kong University of Science and Technology R9820
• Japan Society for the Promotion of Science JP23H03810
• Japan Science and Technology Corporation JPMJER1903
• Shenzhen Research Institute, City University of Hong Kong 7020157

原稿種別: 出版者版 (Version of record)

MDR DOI:

公開URL: https://doi.org/10.1039/d6sc03088b

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更新時刻: 2026-11-02 14:32:55 +0900

MDRでの公開時刻: 2026-11-02 16:34:13 +0900