发明授权
US08410071B2 Potent LNA oligonucleotides for the inhibition of HIF-1A expression
有权
用于抑制HIF-1A表达的强效LNA寡核苷酸
- 专利标题： Potent LNA oligonucleotides for the inhibition of HIF-1A expression
- 专利标题（中）： 用于抑制HIF-1A表达的强效LNA寡核苷酸
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申请号： US13079525申请日： 2011-04-04
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公开(公告)号： US08410071B2公开(公告)日： 2013-04-02
- 发明人: Majken Westergaard , Charlotte Albaek Thrue , Frank Winther Rasmussen , Henrik Frydenlund Hansen
- 申请人： Majken Westergaard , Charlotte Albaek Thrue , Frank Winther Rasmussen , Henrik Frydenlund Hansen
- 申请人地址： DK Hersholm US NJ Piscataway
- 专利权人： Santaris Pharma a/s,Enzon Pharmaceuticals, Inc.
- 当前专利权人： Santaris Pharma a/s,Enzon Pharmaceuticals, Inc.
- 当前专利权人地址： DK Hersholm US NJ Piscataway
- 代理机构： Stoel Rives, LLP
- 主分类号： C12Q1/68
- IPC分类号： C12Q1/68 ; C12P19/34 ; C12N15/63 ; A01N43/04 ; C07H21/04
摘要：
The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5′-(Tx)GxGxcsasasgscsastscscsTxGxT-3′ and 5′-(Gx)TxTxascstsgscscststscsTxTxA-3′, wherein capital letters designate a beta-D-oxy-LNA nucleotide analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighboring nucleotides/LNA nucleotide analogues, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighboring nucleotides/LNA nucleotide analogues, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-1a (HIF-1a), e.g. in the treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g. diabetic retinopathy, macular degeneration (ARMD), psoriasis, rheumatoid arthritis and other inflammatory diseases.
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