Biol. Pharm. Bull., 27(4),453-456, April 2004

Current Topics

2′-O,4′-C-Ethylene-Bridged Nucleic Acids (ENA^TM) as Next-Generation Antisense and Antigene Agents

Makoto KOIZUMI

Lead Discovery Research Laboratories, Sankyo Co., Ltd.; 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. * To whom correspondence should be addressed. e-mail: koizum@sankyo.co.jp

Novel 2′-O,4′-C-ethylene nucleosides have been synthesized as building blocks for antisense and antigene oligonucleotides. 2′-O,4′-C-Ethylene-bridged nucleic acids (ENA^TM) comprising 2′-O,4′-C-ethylene nucleosides have considerable affinity to complementary RNA and double-stranded DNA. Incorporation of 2′-O,4′-C-ethylene nucleosides into oligonucleotides dramatically increase their resistance against exonucleases. In this review, the properties of ENA oligonucleotides and some of their applications as antisense and antigene oligonucleotides are described.

Key words 2′-O,4′-C-ethylene-bridged nucleic acid; antisense oligonucleotide; antigene; exon-skipping