2′-O,4′-C-Ethylene-bridged nucleic acids (ENATM) as next-generation antisense and antigene agents

Abstract

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™) 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. © 2004 Pharmaceutical Society of Japan.