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    OLIGONUCLEOTIDES HAVING A-DNA FORM AND B-DNA FORM CONFORMATIONAL GEOMETRY
    3.
    发明公开
    OLIGONUCLEOTIDES HAVING A-DNA FORM AND B-DNA FORM CONFORMATIONAL GEOMETRY 审中-公开
    OLIGONKLEOTIDE DIE EINE KONFORMATIONSGEOMETRIE DER A-DNS UND B-DNS FORM HABEN

    公开(公告)号：EP1180113A4

    公开(公告)日：2002-09-18

    申请号：EP00928716

    申请日：2000-05-03

    申请人： ISIS PHARMACEUTICALS INC

    发明人： MANOHARAN MUTHIAH ,  MOHAN VENKATRAMAN

    IPC分类号： C12N15/09 ,  A61K48/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04

    CPC分类号： C07H21/00

    摘要： Modified oligonucleotides containing both A-form conformation geometry and B-form conformation geometry nucleotides are disclosed. The B-form geometry allows the oligonucleotide to serve as substrates for RNase H when bound to a target nucleic acid strand. The A-form geometry imparts properties to the oligonucleotide that modulate binding affinity and nuclease resistance. By utilizing C2' endo sugars or O4' endo sugars, the B-form characteristics are imparted to a portion of the oligonucleotide. The A-form characteristics are imparted via use of either 2'-O-modified nucleotides that have 3' endo geometries or use of end caps having particular nuclease stability or by use of both of these in conjunction with each other.

    摘要翻译： 公开了含有A型构象几何和B型构象几何核苷酸的修饰的寡核苷酸。 B型几何结构允许寡核苷酸在与靶核酸链结合时充当RNA酶H的底物。 A型几何形状赋予调节结合亲和力和核酸酶抗性的寡核苷酸的特性。 通过利用C2'内切糖或O4'内切糖，将B型特征赋予寡核苷酸的一部分。 A型特征通过使用具有3'内部几何结构的2'-O-修饰的核苷酸或使用具有特定核酸酶稳定性的端帽或通过使用这两者相互结合而赋予。