TRPM-2 ANTISENSE THERAPY USING AN OLIGONUCLEOTIDE HAVING 2'-O-2-METHOXYLETHYL MODIFICATIONS

摘要

A compound consisting of an oligonucleotide of sequence CAGCAGCAGAGTCTTCATCAT, where the oligonucleotide has a phosphorothioate backbone throughout, the sugar moieties of nucleotides 1-4 and 18-21 bear 2'-O-methoxyethyl modifications, and the remaining nucleotides nucleotides 5-17 are 2'-deoxynucleotides, and where the cytosines of nucleotides 1, 4 and 19 are 5-methylcytosines. The compound has increased stability in vivo and improved in vitro and in vivo antitumor activity.