Synthesis of double-headed 2-5A-antisense chimeras and their ability to activate human RNase L.
The synthesis of a novel 2-5A-antisense chimera having two molecules of a 2-5A tetramer at the 5'-terminus of the antisense moiety with a 2-(hydroxymethyl)-1,3-propanediol linker is described. The ability of the synthesized 2-5A antisense chimeras to activate RNase L was estimated by monitoring the cleavage of a target RNA by the activated RNase L. The double-headed 2-5A-antisense chimera linked with two molecules of a butanediol linker more efficiently cleaved the target RNA as compared with the single-headed 2-5A-antisense chimera and the double-headed 2-5A-antisense chimera linked with a molecule of the butanediol linker.
Department of Biomolecular Science, Faculty of Engineering, Gifu University, Yanagido, Gifu 501-1193, Japan.
Yoshihito
Y
Ueno
Shusaku
S
Okatani
Yuuki
Y
Yamada
Yukio
Y
Kitade
D000227:Adenine Nucleotides / Q000138:chemical synthesis* / Q000494:pharmacology*; D001483:Base Sequence; D002678:Chimera; D016373:DNA, Antisense / Q000737:chemistry; D004789:Enzyme Activation; D006801:Humans; D009843:Oligoribonucleotides / Q000138:chemical synthesis* / Q000494:pharmacology*; D012259:Ribonuclease, Pancreatic / Q000378:metabolism*
D000227:Adenine Nucleotides; D016373:DNA, Antisense; D009843:Oligoribonucleotides; C023505:2',5'-oligoadenylate; D012259:Ribonuclease, Pancreatic