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• W2944006961 endingPage "1628" @default.
• W2944006961 startingPage "1622" @default.
• W2944006961 abstract "Improving oligonucleotide delivery is critical for the further development of oligonucleotide-based therapeutics. Covalent attachment of reporter molecules is one of the most promising approaches toward efficient oligonucleotide-based therapies. An efficient methods for the attachment of a variety of reporter groups is Cu(I)-catalyzed Huisgen azide-alkyne 1,3-dipolar cycloaddition. However, the majority of potential oligonucleotide (ON) therapeutics in clinical trials are carrying phosphorothioate (PS) linkages, and this robust conjugation method is not yet established for these ONs due to a general concern of Cu-S interaction. Here, we developed a method allowing for efficient conjugation of peptides to PS oligonucleotides. The method utilizes solid supported oligonucleotides that can be readily transformed into clickable ONs by simple linker conjugation and further reacted with an azido containing moiety (e.g., a peptide) using the CuBr × Me2S complex as a superior catalyst in that reaction. This study opens the way for further development of PS oligonucleotide-conjugates by means of efficient Cu(I)-catalyzed Huisgen azide-alkyne 1,3-dipolar cycloaddition." @default.
• W2944006961 created "2019-05-16" @default.
• W2944006961 creator A5010094521 @default.
• W2944006961 creator A5050524016 @default.
• W2944006961 creator A5051602267 @default.
• W2944006961 date "2019-05-08" @default.
• W2944006961 modified "2023-10-16" @default.
• W2944006961 title "Efficient Conjugation to Phosphorothioate Oligonucleotides by Cu-Catalyzed Huisgen 1,3-Dipolar Cycloaddition" @default.
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• W2944006961 doi "https://doi.org/10.1021/acs.bioconjchem.9b00217" @default.
• W2944006961 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31067031" @default.
• W2944006961 hasPublicationYear "2019" @default.
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