Enhanced triple-helix and double-helix formation with oligomers
containing modified purines
    35.
    发明授权
    Enhanced triple-helix and double-helix formation with oligomers containing modified purines 失效
    增强的三螺旋和双螺旋形成与含有修饰嘌呤的低聚物

    公开(公告)号:US5594121A

    公开(公告)日:1997-01-14

    申请号:US479248

    申请日:1995-06-07

    摘要: Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain 7-deaza-7-substituted purines or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used for diagnostic purposes in order to detect viruses or disease conditions.

    摘要翻译: 公开了与仅含有常规碱的低聚物相比,具有增强形成双链体或三链体的能力的新型低聚物。 寡聚体包含7-脱氮-7-取代的嘌呤或相关类似物。 本发明的寡聚体能够(i)通过在生理pH下偶联到目标DNA双链体的主要沟槽中或(ii)通过结合单链DNA形成双链体,形成具有各种靶序列的病毒或致癌基因序列的三链体 或由靶基因编码的RNA。 本发明的低聚物可被构建成具有任何所需的序列,条件是序列通常包括用本发明的类似物代替的一个或多个碱基。 本发明的组合物可用于诊断目的以检测病毒或疾病状况。

    Non-nucleoside linkers for convenient attachment of labels to
oligonucleotides using standard synthetic methods
    37.
    发明授权
    Non-nucleoside linkers for convenient attachment of labels to oligonucleotides using standard synthetic methods 失效
    用于使用标准合成方法方便地将标记连接到寡核苷酸的非核苷连接子

    公开(公告)号:US5414077A

    公开(公告)日:1995-05-09

    申请号:US237233

    申请日:1994-05-02

    摘要: Pseudonucleosides and pseudonucleotides are useful in the synthesis of oligomers which contain these components as a means to derivatize the resulting oligonucleotide to useful substituents such as chelators, intercalators, or lipophilic compounds. In general, these pseudonucleotide components are of the formula: ##STR1## wherein each Y is independently O or S; each X is independently H, PO.sub.3.sup.-2, an activated nucleotide synthesis coupling moiety, a protecting group, a nucleoside, a nucleotide or a nucleotide sequence, or comprises a solid support;F is a functional group capable of linking an additional moiety or said group already reacted to effect the binding of said additional moiety;.quadrature. is an organic backbone which does not contain additional F or Y-X substituents and which is either achiral even when the Y-X substituents are different, or is a single enantiomer of a chiral compound;with the proviso that at least one X is a nucleoside, nucleotide, nucleotide sequence, an activated nucleotide synthesis coupling moiety, or comprises a solid support, or F represents said functional group already reacted with an additional group. Oligonucleotides having the pseudonucleoside at the 3' terminus are particularly stable in vivo.

    摘要翻译: 伪核苷和伪核苷酸可用于合成含有这些组分的寡聚体,作为将所得寡核苷酸衍生为有用的取代基如螯合剂,嵌入剂或亲脂性化合物的手段。 通常,这些假核苷酸组分具有下式:其中每个Y独立地为O或S; 每个X独立地是H,PO3-2,活化的核苷酸合成偶联部分,保护基,核苷,核苷酸或核苷酸序列,或包含固体支持物; F是能够连接另外的部分或所述已经反应的基团以实现所述另外部分的结合的官能团; 并且不含有额外的F或Y-X取代基的有机主链,即使Y-X取代基不同也是非手性的,或是手性化合物的单一对映异构体; 条件是至少一个X是核苷,核苷酸,核苷酸序列,活化的核苷酸合成偶联部分,或包含固体支持物,或F表示已经与另外的基团反应的所述官能团。 在3'末端具有假核苷的寡核苷酸在体内特别稳定。

    Oligonucleotide analogs with novel linkages

    公开(公告)号:US5264562A

    公开(公告)日:1993-11-23

    申请号:US690786

    申请日:1991-04-24

    申请人: Mark Matteucci

    发明人: Mark Matteucci

    CPC分类号: C07H19/06 C07H19/16 C07H21/00

    摘要: Oligonucleotide analogs wherein one or more phosphodiester linkages between adjacent nucleotides are replaced by an formacetal/ketal type linkage are resistant to nucleases and do not need to exhibit the diastereomerism characteristic of many other oligonucleotide analogs, and thus are capable of strong hybridization to target RNA or DNA. These oligonucleotide analogs are useful in therapies which modulate gene expression using "antisense" or other specifically binding oligomers.