{"title":"肽-寡核苷酸缀合物：水溶液或柱上催化制备","authors":"Marion Gras, Michael Smietana, Pauline Adler","doi":"10.1002/cpz1.70154","DOIUrl":null,"url":null,"abstract":"<p>Peptide–oligonucleotide conjugates (POCs) are synthesized through a novel catalytic and sustainable approach. The amide coupling between peptide and oligonucleotide is facilitated by 1,4-diazabicyclo[2.2.2]octane (DABCO) as catalyst and 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) as a stoichiometric activating agent. Two distinct methods are described for the POC synthesis: the first involves an on-column conjugation in an anhydrous environment, while the second enables a post-synthetic conjugation in an aqueous buffer. This last approach has been successfully extended to an iterative process, offering significant potential for the development of DNA-encoded libraries.© 2025 The Author(s). Current Protocols published by Wiley Periodicals LLC.</p><p><b>Basic Protocol 1</b>: On-column conjugation of an amino acid or of a peptide to an oligonucleotide</p><p><b>Support Protocol</b>: Deprotection of the Boc-protected amine of the lysine</p><p><b>Basic Protocol 2</b>: In-solution conjugation of an amino acid or of a peptide on an oligonucleotide</p><p><b>Basic Protocol 3</b>: Iterative process for the preparation of a peptide–oligonucleotide conjugate</p>","PeriodicalId":93970,"journal":{"name":"Current protocols","volume":"5 6","pages":""},"PeriodicalIF":2.2000,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/cpz1.70154","citationCount":"0","resultStr":"{\"title\":\"Peptide–Oligonucleotide Conjugates: Catalytic Preparation in Aqueous Solution or On-Column\",\"authors\":\"Marion Gras, Michael Smietana, Pauline Adler\",\"doi\":\"10.1002/cpz1.70154\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>Peptide–oligonucleotide conjugates (POCs) are synthesized through a novel catalytic and sustainable approach. The amide coupling between peptide and oligonucleotide is facilitated by 1,4-diazabicyclo[2.2.2]octane (DABCO) as catalyst and 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) as a stoichiometric activating agent. Two distinct methods are described for the POC synthesis: the first involves an on-column conjugation in an anhydrous environment, while the second enables a post-synthetic conjugation in an aqueous buffer. This last approach has been successfully extended to an iterative process, offering significant potential for the development of DNA-encoded libraries.© 2025 The Author(s). Current Protocols published by Wiley Periodicals LLC.</p><p><b>Basic Protocol 1</b>: On-column conjugation of an amino acid or of a peptide to an oligonucleotide</p><p><b>Support Protocol</b>: Deprotection of the Boc-protected amine of the lysine</p><p><b>Basic Protocol 2</b>: In-solution conjugation of an amino acid or of a peptide on an oligonucleotide</p><p><b>Basic Protocol 3</b>: Iterative process for the preparation of a peptide–oligonucleotide conjugate</p>\",\"PeriodicalId\":93970,\"journal\":{\"name\":\"Current protocols\",\"volume\":\"5 6\",\"pages\":\"\"},\"PeriodicalIF\":2.2000,\"publicationDate\":\"2025-06-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://onlinelibrary.wiley.com/doi/epdf/10.1002/cpz1.70154\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current protocols\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://currentprotocols.onlinelibrary.wiley.com/doi/10.1002/cpz1.70154\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current protocols","FirstCategoryId":"1085","ListUrlMain":"https://currentprotocols.onlinelibrary.wiley.com/doi/10.1002/cpz1.70154","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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Peptide–Oligonucleotide Conjugates: Catalytic Preparation in Aqueous Solution or On-Column
Peptide–oligonucleotide conjugates (POCs) are synthesized through a novel catalytic and sustainable approach. The amide coupling between peptide and oligonucleotide is facilitated by 1,4-diazabicyclo[2.2.2]octane (DABCO) as catalyst and 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) as a stoichiometric activating agent. Two distinct methods are described for the POC synthesis: the first involves an on-column conjugation in an anhydrous environment, while the second enables a post-synthetic conjugation in an aqueous buffer. This last approach has been successfully extended to an iterative process, offering significant potential for the development of DNA-encoded libraries.© 2025 The Author(s). Current Protocols published by Wiley Periodicals LLC.
Basic Protocol 1: On-column conjugation of an amino acid or of a peptide to an oligonucleotide
Support Protocol: Deprotection of the Boc-protected amine of the lysine
Basic Protocol 2: In-solution conjugation of an amino acid or of a peptide on an oligonucleotide
Basic Protocol 3: Iterative process for the preparation of a peptide–oligonucleotide conjugate
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