Derivatized oligonucleotides having improved uptake and other properties
    34.
    发明授权
    Derivatized oligonucleotides having improved uptake and other properties 失效
    具有改善摄取和其他性质的衍生寡核苷酸

    公开(公告)号:US06831166B2

    公开(公告)日:2004-12-14

    申请号:US10073718

    申请日:2002-02-11

    Abstract: Linked nucleosides having at least one functionalized nucleoside that bears a substituent such as a steroid molecule, a reporter molecule, a non-aromatic lipophilic molecule, a reporter enzyme, a peptide, a protein, a water soluble vitamin, a lipid soluble vitamin, an RNA cleaving complex, a metal chelator, a porphyrin, an alkylator, a pyrene, a hybrid photonuclease/intercalator, or an aryl azide photo-crosslinking agent exhibit increased cellular uptake and other properties. The substituent can be attached at the 2′-position of the functionalized nucleoside via a linking group. If at least a portion of the remaining liked nucleosides are 2′-deoxy-2′-fluoro, 2′-O-methoxy, 2′-O-ethoxy, 2′-O-propoxy, 2′-O-aminoalkoxy or 2′-O-allyloxy nucleosides, the substituent can be attached via a linking group at any of the 3′ or the 5′ positions of the nucleoside or on the heterocyclic base of the nucleoside or on the inter-nucleotide linkage linking the nucleoside to an adjacent nucleoside.

    Abstract translation: 具有至少一个具有取代基的官能化核苷的连接核苷,例如类固醇分子,报道分子,非芳族亲脂性分子,报道酶,肽,蛋白质,水溶性维生素,脂溶性维生素, RNA切割复合物,金属螯合剂,卟啉,烷基化剂,芘,混合光子核酸酶/嵌入剂或芳基叠氮化物光交联剂表现出增加的细胞摄取和其它性质。 取代基可以通过连接基团连接在官能化核苷的2'-位上。 如果至少一部分剩余的核苷类为2'-脱氧-2'-氟,则2'-O-甲氧基,2'-O-乙氧基,2'-O-丙氧基,2'-O-氨基烷氧基或2 '-O-烯丙氧基核苷,取代基可以通过连接基团在核苷的3'或5'位置或核苷的杂环碱基上或连接核苷与核苷酸之间的核苷酸间连接 相邻核苷。

    Chemical modification of DNA using peptide nucleic acid conjugates
    36.
    发明授权
    Chemical modification of DNA using peptide nucleic acid conjugates 失效
    使用肽核酸缀合物进行DNA的化学修饰

    公开(公告)号:US06746868B1

    公开(公告)日:2004-06-08

    申请号:US09705365

    申请日:2000-11-03

    Abstract: Complexes comprising a nucleic acid molecule and a conjugated peptide nucleic acid (PNA). The PNA may be labeled or conjugated to a protein, peptide, carbohydrate moiety or receptor ligand. These complexes are used to transfect cells to monitoring plasmid biodistribution, promote nuclear localization, induce transcriptional activation, lyse the endosomal compartment and facilitate transfection. These complexes increase the efficiency of expression of a particular gene.

    Abstract translation: 包含核酸分子和缀合肽核酸(PNA)的复合物。 PNA可以标记或缀合到蛋白质,肽,碳水化合物部分或受体配体。 这些复合物用于转染细胞以监测质粒生物分布,促进核定位,诱导转录激活,裂解内体室并促进转染。 这些复合物增加特定基因的表达效率。

    Chimeric oligonucleotides for modulating gene expression
    37.
    发明授权
    Chimeric oligonucleotides for modulating gene expression 失效
    用于调节基因表达的嵌合寡核苷酸

    公开(公告)号:US06713621B1

    公开(公告)日:2004-03-30

    申请号:US08401192

    申请日:1995-03-09

    CPC classification number: C07K14/70542 A61K38/00 A61K48/00

    Abstract: Genes coding for vascular cell adhesion molecules, particularly VCAM-1, are modulated through interaction of oligonucleotides with transcriptional regulatory factors which bind to the genes. Specific and effective oligonucleotides are provided which interact with the transcriptional regulatory factors to diminish their interaction with the genes and downregulate their function. Multi-modal oligonucleotides are also provided which interact both with a transcriptional regulatory factor and with another aspect of gene function.

    Abstract translation: 编码血管细胞粘附分子,特别是VCAM-1的基因通过寡核苷酸与结合基因的转录调节因子的相互作用来调节。 提供具体和有效的寡核苷酸,其与转录调节因子相互作用以减少它们与基因的相互作用并下调其功能。 还提供了多模态寡核苷酸,其与转录调节因子和基因功能的另一方面相互作用。

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