申请人:Shudo, Koichi, Prof. Dr.
公开号:EP0540742A1
公开(公告)日:1993-05-12
An oligodeoxynucleotide including an oligonucleotide comprising 5' - phosphates of a nucleoside, formed by combining 2 - deoxy - L - erythro- pentose with a nucleic acid base in the form of a β- anomer, linked with each other through 3'-5' phosphodiester linkages; and another oligodeoxynucleotide including an oligonucleotide comprising 5'-phosphates of a nucleoside, formed by combining 2 - deoxy - D - ribose with a nucleic acid base in the form of a β- anomer, and 5' - phosphates of another nucleoside, formed by combining 2 - deoxy - L - erythro- pentose with a nucleic acid base in the form of a β- anomer, linked with each other alternatingly through 3'-5' phosphodiester linkages. Each of the oligodeoxynucleotides combines specifically with a natural oligonucleotide having a complementary base sequence and is useful as an antisense DNA having an activity of inhibiting gene expression. These oligodeoxynucleotides can be efficiently produced by the solid phase method using a phosphoramidite derivative containing a 2-deoxy-β- L-erythro-pentofuranosyl moiety.
一种寡核苷酸,包括包含5'-核苷酸磷酸的寡核苷酸,由将2'-去氧-L-赤霉糖与以β-异构体形式的核酸碱基结合而成,通过3'-5'磷酸二酯键连接在一起;另一种寡核苷酸,包括包含5'-核苷酸磷酸的寡核苷酸,由将2'-去氧-D-核糖与以β-异构体形式的核酸碱基结合而成,并且由将2'-去氧-L-赤霉糖与以β-异构体形式的核酸碱基结合而成的另一个核苷酸磷酸连接在一起,通过3'-5'磷酸二酯键交替连接在一起。这些寡核苷酸分别与具有互补碱基序列的天然寡核苷酸特异结合,并可用作具有抑制基因表达活性的反义DNA。这些寡核苷酸可以通过使用含有2'-去氧-β-L-赤霉糖基团的磷酰胺酰胺衍生物的固相法高效制备。