Synthesis and biophysical properties of 5’-thio-2’,4’-BNA/LNA oligonucleotide

Publication date: Available online 23 May 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Md Ariful Islam, Aki Fujisaka, Shohei Mori, Kosuke Ramon Ito, Takao Yamaguchi, Satoshi Obika
Phophorothioate modification of oligonucleotides is one of the most promising chemical modifications in nucleic acid therapeutics. Structurally similar 5'-thio or phosphorothiolate-modified nucleotides, in which the 5'-bridging oxygen atom is replaced with a sulfur atom, are attracting attention and gaining importance in oligonucleotide-based research. In our present study, we synthesized 5'-thio-2',4'-BNA/LNA monomers bearing thymine or 5-methylcytosine nucleobase. The 5'-thio-2',4'-BNA/LNA monomers were successfully incorporated into target oligonucleotides, and their nuclease stability and binding affinity with complementary strands were evaluated.

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