2'-O,4'-C-ethylene-bridged nucleic acids (ENA) as next-generation antisense and antigene agents.
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.
Koizumi
Makoto
M
Lead Discovery Research Laboratories, Sankyo Co. Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. koizum@sankyuo.co.jp
D001952:Bridged-Ring Compounds / Q000138:chemical synthesis / Q000737:chemistry; D004355:Drug Stability; D005030:Ethylenes / Q000138:chemical synthesis / Q000737:chemistry*; D005092:Exonucleases / Q000737:chemistry; D008968:Molecular Conformation; D009696:Nucleic Acids / Q000138:chemical synthesis / Q000737:chemistry*; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis / Q000737:chemistry*
D001952:Bridged-Ring Compounds; D005030:Ethylenes; D009696:Nucleic Acids; D016376:Oligonucleotides, Antisense; D005092:Exonucleases