{
  "abstract": "Non-symmetric stapling of native peptides that crosslinking two distinct residues is a valuable tool for enriching diversity of peptide macrocycles, yet it is less achieved due to the high demand for chemo- and siteselectivity control, as well as the competitive intermolecular peptide crosslinking. Herein, we reported a noncovalent interaction activation strategy for non-symmetric stapling of tyrosine-containing peptides by employing ethenesulfonyl fluoride (ESF) as a bifunctional crosslinker. Once covalently anchored to peptide, the sulfonyl fluoride motif is activated by non-covalent interactions, which triggers an intramolecular SuFEx click reaction with tyrosine to afford peptide macrocycles. This approach efficiently crosslinks diverse residue pairs, including Cys–Tyr, His–Tyr and Pro–Tyr. Notably, the protocol is scalable and can be performed in solid-phase synthesis, providing a robust access to tyrosine-bridged peptide macrocycles with excellent diversity.",
  "abstract_shown": true,
  "affiliations": [
    "Engineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry",
    "Fudan University",
    "Shanghai Engineering Research Center of Industrial Asymmetric Catalysis of Chiral Drugs"
  ],
  "article_type": null,
  "arxiv": null,
  "author_total": 11,
  "authors": [
    {
      "name": "Junwei Han"
    },
    {
      "name": "Yi-Chi Lu"
    },
    {
      "name": "Shangli Ding"
    },
    {
      "name": "Qiu-Shuo Zheng"
    },
    {
      "name": "Yu-Qin Wen"
    },
    {
      "name": "Neng-Rong Chen"
    },
    {
      "name": "Chen-Xiao Fu"
    },
    {
      "name": "Longguang Jiang"
    },
    {
      "name": "Fa-Jie Chen",
      "orcid": "0000-0002-0421-3885"
    },
    {
      "name": "Wan-Zhen Lin"
    },
    {
      "affs": [
        0,
        1,
        2
      ],
      "name": "Fen-Er Chen"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/5ysrjg456rcba.bib",
  "cited_by": 0,
  "doi": "10.26434/chemrxiv.15003320/v2",
  "fulltext_url": null,
  "id": "5ysrjg456rcba",
  "issns": [],
  "landing_url": "https://chemrxiv.org/doi/full/10.26434/chemrxiv.15003320/v2",
  "language": null,
  "licence": "CC-BY",
  "licence_label": "CC BY",
  "licence_source": "journal",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "openalex",
      "1312|Chemical Synthesis and Analysis"
    ]
  ],
  "openalex": "W7222999455",
  "pdf_url": "https://chemrxiv.org/doi/pdf/10.26434/chemrxiv.15003320/v2",
  "pmcid": null,
  "pmid": null,
  "published": "2026-10-20",
  "publisher": "American Chemical Society (ACS)",
  "ris": "https://research.draconitic.com/paper/5ysrjg456rcba.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T12:17:24Z",
      "native_id": "10.26434/chemrxiv.15003320",
      "source": "chemrxiv",
      "url": "https://chemrxiv.org/doi/full/10.26434/chemrxiv.15003320/v2"
    }
  ],
  "subjects": [
    {
      "field": "biochemistry",
      "origin": "openalex:1312|Chemical Synthesis and Analysis",
      "subfield": "molecular-biology"
    }
  ],
  "title": "Non-Symmetric Stapling of Tyrosine-Containing Peptides Driven by Intramolecular Non-Covalent Interactions",
  "title_text": "Non-Symmetric Stapling of Tyrosine-Containing Peptides Driven by Intramolecular Non-Covalent Interactions",
  "type": "preprint",
  "updated_at": "2026-10-30T12:17:24Z",
  "url": "https://research.draconitic.com/paper/5ysrjg456rcba",
  "venue": "ChemRxiv",
  "versions": []
}