Synthesis and Properties of Oligonucleotides Containing LNA-Sulfamate and Sulfamide Backbone Linkages

ZENGİN KURT B., Dhara D., El-Sagheer A. H., Brown T.

ORGANIC LETTERS, vol.26, pp.4137-4141, 2024 (SCI-Expanded, Scopus) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 26
  • Publication Date: 2024
  • Doi Number: 10.1021/acs.orglett.4c01232
  • Journal Name: ORGANIC LETTERS
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, Chemical Abstracts Core, Chimica, MEDLINE
  • Page Numbers: pp.4137-4141
  • Bezmialem Vakıf University Affiliated: Yes

Abstract

Oligonucleotides hold great promise as therapeutic agents but poor bioavailability limits their utility. Hence, new analogues with improved cell uptake are urgently needed. Here, we report the synthesis and physical study of reduced-charge oligonucleotides containing artificial LNA-sulfamate and sulfamide linkages combined with 2 '-O-methyl sugars and phosphorothioate backbones. These oligonucleotides have high affinity for RNA and excellent nuclease resistance.