发明名称 MODIFICATION OF NUCLEIC ACID
摘要 PROBLEM TO BE SOLVED: To provide a method for reinforcing the mismatch-recognizing ability of a specific antisense nucleic acid by introducing a polyamine to the C-5 position of the pyrimidine base of the antisense nucleic acid, capable of giving nucleic acid medicines having high double strand-forming abilities with perfectly complementary chains and useful for treating infectious diseases such as HIV, etc. SOLUTION: This method for reinforcing the mismatch-recognizing ability of an antisense nucleic acid comprises introducing a polyamine to the C-5 position of the pyrimidine base (preferably expressed by formula I) of an antisense nucleic acid comprising a phosphorothioate oligomer DNA. The polyamine is preferably introduced by treating a phosphorothioate oligomer DNA having a pyrimidine base having a methoxycarbonylmethyl group at the C-5 position as a constituent with an excessive amount of tris(2-aminoethyl)amine, and a polyamine-modified phosphorothioate oligomer DNA of formula II or III (Acr is a compound of formula-IV; U* is a compound of formula V) is used for anti-HIV preparations.
申请公布号 JPH11322784(A) 申请公布日期 1999.11.24
申请号 JP19980145175 申请日期 1998.05.12
申请人 TOAGOSEI CO LTD 发明人 SHINOZUKA KAZUO;OKAMOTO TAKESHI;MATSUKURA MAKOTO;SAWAI HIROAKI
分类号 C12N15/09;A61K31/70;A61K48/00;A61P31/12;A61P37/04;C07H21/04 主分类号 C12N15/09
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