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公开(公告)号：US07422861B2
公开(公告)日：2008-09-09
申请号：US10025423
申请日：2001-12-18
CPC分类号： A61K51/0491 , C07K14/001 , C12N15/87 , C12N15/88 , Y02P20/582
摘要： Different-sequence peptoids, including lipid- and sterol-conjugated peptoids, are found to be effective in transfection of cells with oligonucleotides. Combinatorial libraries of such peptoids can be screened efficiently in a high-throughput format, and selected peptoids are identified post-screening.
摘要翻译： 发现不同序列的拟肽，包括脂质和固醇共轭的拟肽，在用寡核苷酸转染细胞中是有效的。 可以以高通量格式有效筛选此类拟肽的组合库，筛选后鉴定选择的拟肽。
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2.发明授权公开(公告)号：US06677445B1
公开(公告)日：2004-01-13
申请号：US09648254
申请日：2000-08-25
IPC分类号： C07H2104
CPC分类号： C12N15/113 , A61K38/00 , A61K47/54 , A61K47/554 , A61K47/6949 , B82Y5/00 , C12N2310/315 , C12N2310/317 , C12N2310/321 , C12N2310/346 , C12N2310/3515 , C12N2310/3521
摘要： Chimeric oligonucleotide of the formula 5′-W-X1-Y-X2-Z-3′, where W represents a 5′-O-alkyl nucleotide, each of X1 and X2 represents a block of seven to twelve phosphodiester-linked 2′-O-alkyl ribonucleotides, Y represents a block of five to twelve phosphorothioate-linked deoxyribonucleotides, and Z represents a blocking group effective to block nuclease activity at the 3′ end of the oligonucleotide, are described. These compounds exhibit high resistance to endo- and exonucleases, high sequence specificity, and the ability to activate RNAse H, as evidenced by efficient and long-lasting suppression of target mRNA. The oligonucleotides are preferably transfected into cells in formulations containing a lipid-peptoid conjugate carrier molecule of the formula L-linker-[N(CH2CH2NH2)CH2(C═O)—N(CH2CH2R)CH2(C═O)—N(CH2CH2R)CH2(C═O)]3—NH2, where L is a lipid moiety, including a steroid, and each group R is independently selected from alkyl, aminoalkyl, and aralkyl.
摘要翻译： 式5-WX 1 -YX 2 -Z-3'的嵌合寡核苷酸，其中W代表5'-O-烷基核苷酸，X 1和X 2各自表示 7至12个磷酸二酯连接的2'-O-烷基核糖核苷酸，Y表示5至12个硫代磷酸酯连接的脱氧核糖核苷酸的嵌段，Z表示有效阻断寡核苷酸3'端的核酸酶活性的封闭基团。 这些化合物表现出对内切核酸酶和外切核酸酶的高抗性，高序列特异性和激活RNA酶H的能力，如靶mRNA的有效和持久的抑制所证明的。 优选将寡核苷酸转染到含有脂质 - 拟肽结合物载体分子的制剂中，其中L是包含类固醇的脂质部分，每个基团R独立地选自烷基，氨基烷基和芳烷基。
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3.发明授权公开(公告)号：US06846921B2
公开(公告)日：2005-01-25
申请号：US09826519
申请日：2001-04-03
IPC分类号： A61K38/00 , A61K47/48 , C12N15/113 , C07H21/04
CPC分类号： C12N15/113 , A61K38/00 , A61K47/54 , A61K47/554 , A61K47/6949 , B82Y5/00 , C12N2310/315 , C12N2310/317 , C12N2310/321 , C12N2310/346 , C12N2310/3515 , C12N2310/3521
摘要： Chimeric oligonucleotide of the formula 5′-W—X1—Y—X2—Z-3′, where W represents a 5′-O-alkyl nucleotide, each of X1 and X2 represents a block of seven to twelve phosphodiester-linked 2′-O-alkyl ribonucleotides, Y represents a block of five to twelve phosphorothioate-linked deoxyribonucleotides, and Z represents a blocking group effective to block nuclease activity at the 3′ end of the oligonucleotide, are described. These compounds exhibit high resistance to endo- and exonucleases, high sequence specificity, and the ability to activate RNAse H, as evidenced by efficient and long-lasting suppression of target mRNA. The oligonucleotides are preferably transfected into cells in formulations containing a lipid-peptoid conjugate carrier molecule of the formula L-linker-[N(CH2CH2NH2)CH2(C═O)—N(CH2CH2R)CH2(C═O)—N(CH2CH2R)CH2(C═O)]3—NH2, where L is a lipid moiety, including a steroid, and each group R is independently selected from alkyl, aminoalkyl, and aralkyl.
摘要翻译： 式5-WX 1 -YX 2 -Z-3'的嵌合寡核苷酸，其中W代表5'-O-烷基核苷酸，X 1和X 2各自表示 7至12个磷酸二酯连接的2'-O-烷基核糖核苷酸，Y表示5至12个硫代磷酸酯连接的脱氧核糖核苷酸的嵌段，Z表示有效阻断寡核苷酸3'末端核酸酶活性的封闭基团。 这些化合物表现出对内切核酸酶和外切核酸酶的高抗性，高序列特异性和激活RNA酶H的能力，如靶mRNA的有效和持久的抑制所证明的。 优选将寡核苷酸转染到含有脂质 - 拟肽结合物载体分子的制剂中，其中L是包含类固醇的脂质部分，每个基团R独立地选自烷基，氨基烷基和芳烷基。
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4.发明授权公开(公告)号：US06586244B2
公开(公告)日：2003-07-01
申请号：US09876176
申请日：2001-06-06
IPC分类号： C07H2104
CPC分类号： C12N15/113 , A61K38/00 , C07K14/78 , C12Q1/6886 , C12Q2600/136
摘要： Inhibitors of laminin5beta3 are provided that reduce the expression or biological activities of laminin5beta3 or the expression of laminin5beta3 mRNA in a mammalian cell. Laminin5beta3 inhibitors include antisense molecules, ribozymes, antibodies and antibody fragments, proteins and polypeptides as well as small molecules. Laminin5beta3 inhibitors find use in compositions and methods for decreasing laminin5beta3 gene expression as well as methods for inhibiting the proliferation of mammalian cells, including tumor cells of epithelial origin, and methods for treating neoplastic diseases.
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