We recently designed guanidine-bridged nucleic acids (GuNA), and GuNA bearing a thymine (T) nucleobase was synthesized and successfully incorporateed into oligonucleotides. The GuNA-T-modified oligonucleotides possessed high duplex-forming ability towards their...

Anti-microRNA oligonucleotides (AMOs) are valuable tools for the treatment of diseases caused by the dysregulation of microRNA expression. However, the correlation between chemical modifications in AMO sequences and the microRNA-inhibitory activity has not been fully elucidated. In this study, we synthesized a series of AMOs containing cationic guanidine-bridged nucleic acids (GuNA) and evaluated their activities using a dual luciferase assay. We also optimized the site of GuNA substitution and found an effective design for the inhibition of microRNA-21, which was partially different from that of conventional nucleic acid derivatives. This study showed that GuNA-substituted AMOs are effective in inhibiting the function of microRNA.

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2ʹ-amino-locked nucleic acid (ALNA), maintains excellent duplex stability, and the nitrogen at the 2ʹ-position is an attractive scaffold for functionalization. Herein, a facile and efficient method for the synthesis of...