OLIGONUCLEOTIDE PRODRUGS

摘要

Disclosed is an oligonucleotide prodrug comprising at least six covalently linked nucleotides, at least one of which is derivatized with a lipophilic chemical group reversibly and covalently attached to the nucleotide at a 5' phosphate, a 3' phosphate, or an internucleotidic phosphate linkage. The prodrug is reactive with a cellular or tissue enzyme which cleaves the lipophilic group from the derivatized nucleotide, thereby regenerating the parent oligonucleotide.