Oligonucleotides including pyrazolo[3,4-D]pyrimidine bases, bound in
double stranded nucleic acids
    1.
    发明授权
    Oligonucleotides including pyrazolo[3,4-D]pyrimidine bases, bound in double stranded nucleic acids 失效
    寡核苷酸包括双链核酸结合的吡唑并[3,4-D]嘧啶碱基

    公开(公告)号:US6143877A

    公开(公告)日:2000-11-07

    申请号:US848373

    申请日:1997-04-30

    CPC分类号: C07H21/00 C12Q1/6813

    摘要: A triplex forming oligonucleotide is complementary pursuant to the G/T or A/G recognition motif to a homopurine, or substantially homopurine target sequence in double stranded nucleic acids, and at least one and preferably all of the guanine bases are replaced by their pyrazolo[3,4-d]pyrimidine analog, namely by 6-amino-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one. The oliginucleotides containing the pyrazolo[3,4-d]pyrimidine analog of guanine exhibit a lesser degree of self-association, and lack the nucleophilic nitrogen atom in the 7 position of guanine. The latter feature results in a diminished extent of self-crosslinking in ODNs which also have a covalently attached cross-linking agent.

    摘要翻译: 三链体形成寡核苷酸是根据G / T或A / G识别基序与双链核酸中的均嘌呤或基本上均嘌呤靶序列互补的,并且至少一个并优选全部鸟嘌呤碱基被其吡唑并[ 3,4-d]嘧啶类似物,即6-氨基-1H-吡唑并[3,4-d]嘧啶-4(5H) - 酮。 含有鸟嘌呤的吡唑并[3,4-d]嘧啶类似物的寡核苷酸表现出较小程度的自身结合,并且在鸟嘌呤的7位缺乏亲核氮原子。 后一个特征导致ODN中的自交联程度减小,其也具有共价连接的交联剂。