- Novel anthraquinone conjugate of 2,2-bis(hydroxymethyl)propionic acid incorporated to a TFO with phosphodiester linkage facilitates triplex formation with dsDNA bearing a pyrimidine-gapped polypurine sequence
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An anthraquinone derivative conjugated with 2,2-bis(hydroxymethyl) propionic acid as a novel non-nucleosidic component was synthesized and successfully incorporated into an internal region of 14-mer triplex-forming oligonucleotide (TFO) via the phosphoramidite method. The resulted novel TFO exhibits remarkable enhancement effect on the thermal stability of a DNA triplex upon binding to a pyrimidine-gap containing polyprurine sequence.
- Sato, Megumi,Moriguchi, Tomohisa,Shinozuka, Kazuo
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Read Online
- Synthesis of 2-deoxy ribose related disaccharide nucleoside and its phosphoramidite
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Synthesis of impurity reference compound of anti-tumor drug ISIS 183750 was achieved. In this process, a general method for synthesis of 2-deoxy ribosyl disaccharide nucleosides was established for the first time.
- Ding, Yili,Deng, Rilie,Wang, Bingyun
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p. 3848 - 3852
(2017/06/13)
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- Efficient large-scale synthesis of 5′-O-dimethoxytrityl-N 4-benzoyl-5-methyl-2′-deoxycytidine
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An efficient process to synthesize 5′- O -dimethoxytrityl-N 4 -benzoyl-5-methyl-2 ′-deoxycytidine in high yield and quality is described. Final benzoylation was improved by developing a method to selectively hydrolyze benzoyl ester impurities. This inexpensive approach was scaled up to multi-kilogram quantities for routine use in oligonucleotide therapeutics. Copyright Taylor & Francis Group, LLC.
- Ross, Bruce,Han, Mingming,Ravikumar, Vasulinga
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p. 765 - 770
(2007/10/03)
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- Antisense inhibition via RNAse H-independent reduction in mRNA
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The present invention provides compositions and methods for reducing levels of a preselected mRNA, using antisense compounds targeted to a splice site or a region up to 50 nucleobases upstream of an exon/intron junction on said mRNA. Preferably, said antisense compounds do not elicit RNAse H cleavage of the mRNA.
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Page/Page column 20
(2010/02/12)
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- Metallic salt of N4-acylcytidine derivatives, and a method for producing N4-acylcytidine derivatives using the same
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The present invention provides a method for producing a high purity N4-acylcytidine derivative. More specially, the invention provides a compound represented by the formula (1): wherein R1 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms, a perfluoroalkyl group having 1 to 4 carbon atoms, or a halogen atom; R2 is a hydrogen atom, an alkoxyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms with a substituent, or a halogen atom; R3 represents a methyl group or a phenyl group; and M represents a positive ion of an alkali metal or an alkaline earth metal, and a compound represented by the formula (2): wherein R1, R2, and R3 are as defined above, produced by using the compound represented by the formula (1).
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Page/Page column 5
(2010/02/13)
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- Modulation of DC-SIGN expression
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Compounds, compositions and methods are provided for modulating the expression of DC-SIGN. The compositions comprise oligonucleotides, targeted to nucleic acid encoding DC-SIGN. Methods of using these compounds for modulation of DC-SIGN expression and for diagnosis and treatment of diseases and conditions associated with expression of DC-SIGN are provided.
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Page/Page column 12
(2008/06/13)
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- Antisense modulation of polo-like kinase expression
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Antisense compounds, compositions and methods are provided for modulating the expression of polo-like kinase. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding polo-like kinase. Methods of using these compounds for modulation of polo-like kinase expression and for treatment of diseases associated with expression of polo-like kinase are provided.
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Page/Page column 17-18
(2008/06/13)
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- Antisense modulation of resistin expression
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Antisense compounds, compositions and methods are provided for modulating the expression of resistin. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding resistin. Methods of using these compounds for modulation of resistin expression and for treatment of diseases associated with expression of resistin are provided.
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Page/Page column 17-18
(2010/02/05)
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- Modulation of forkhead box O1A expression
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Antisense compounds, compositions and methods are provided for modulating the expression of forkhead box O1A. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding forkhead box O1A. Methods of using these compounds for modulation of forkhead box O1A expression and for treatment of diseases associated with expression of forkhead box O1A are provided, in particular, for methods of treating diabetes.
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Page/Page column 20
(2010/02/06)
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- Antisense modulation of phosphotyrosyl phosphatase activator expression
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Antisense compounds, compositions and methods are provided for modulating the expression of phosphotyrosyl phosphatase activator. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding phosphotyrosyl phosphatase activator. Methods of using these compounds for modulation of phosphotyrosyl phosphatase activator expression and for treatment of diseases associated with expression of phosphotyrosyl phosphatase activator are provided.
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Page/Page column 17-18
(2008/06/13)
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- Antisense modulation of PPP2R1A expression
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Antisense compounds, compositions and methods are provided for modulating the expression of PPP2R1A. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PPP2R1A. Methods of using these compounds for modulation of PPP2R1A expression and for treatment of diseases associated with expression of PPP2R1A are provided.
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Page/Page column 17-18
(2010/02/05)
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- Antisense modulation of requiem expression
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Antisense compounds, compositions and methods are provided for modulating the expression of requiem. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding requiem. Methods of using these compounds for modulation of requiem expression and for treatment of diseases associated with expression of requiem are provided.
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Page/Page column 17-18
(2010/02/05)
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- Antisense modulation of hepatoma-derived growth factor expression
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Antisense compounds, compositions and methods are provided for modulating the expression of hepatoma-derived growth factor. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding hepatoma-derived growth factor. Methods of using these compounds for modulation of hepatoma-derived growth factor expression and for treatment of diseases associated with expression of hepatoma-derived growth factor are provided.
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Page/Page column 17-18
(2010/11/30)
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- Antisense modulation of PTPRA expression
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Antisense compounds, compositions and methods are provided for modulating the expression of PTPRA. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTPRA. Methods of using these compounds for modulation of PTPRA expression and for treatment of diseases associated with expression of PTPRA are provided.
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Page/Page column 18
(2008/06/13)
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- Antisense modulation of Ran GTPase activating protein 1 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of Ran GTPase activating protein 1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding Ran GTPase activating protein 1. Methods of using these compounds for modulation of Ran GTPase activating protein 1 expression and for treatment of diseases associated with expression of Ran GTPase activating protein 1 are provided.
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Page/Page column 18
(2010/02/05)
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- Antisense modulation of KIAA1531 protein expression
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Antisense compounds, compositions and methods are provided for modulating the expression of KIAA1531 protein. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding KIAA1531 protein. Methods of using these compounds for modulation of KIAA1531 protein expression and for treatment of diseases associated with expression of KIAA1531 protein are provided.
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Page/Page column 18
(2010/02/05)
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- Antisense modulation of G protein-coupled receptor 6 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of G protein-coupled receptor 6. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding G protein-coupled receptor 6. Methods of using these compounds for modulation of G protein-coupled receptor 6 expression and for treatment of diseases associated with expression of G protein-coupled receptor 6 are provided.
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Page/Page column 18
(2010/02/05)
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- Antisense modulation of LAR expression
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Antisense compounds, compositions and methods are provided for modulating the expression of LAR. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding LAR. Methods of using these compounds for modulation of LAR expression and for treatment of diseases associated with expression of LAR are provided.
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Page/Page column 18
(2010/02/05)
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- Antisense modulation of G protein-coupled receptor 12 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of G protein-coupled receptor 12. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding G protein-coupled receptor 12. Methods of using these compounds for modulation of G protein-coupled receptor 12 expression and for treatment of diseases associated with expression of G protein-coupled receptor 12 are provided.
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Page/Page column 18
(2010/11/30)
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- Oligonucleotides having modified nucleoside units
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Disclosed are oligonucleotide that include one or more modified nucleoside units. The oligonucleotides are particularly useful as antisense agents, ribozymes, aptamer, siRNA agents, probes and primers or, when hybridized to an RNA, as a substrate for RNA cleaving enzymes including RNase H and dsRNase.
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- Oligonucleotides having modified nucleoside units
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Disclosed are oligonucleotides and oligonucleosides that include one or more modified nucleoside units. The oligonucleotides and oligonucleosides are particularly useful as antisense agents, ribozymes, aptamer, siRNA agents, probes and primers or, when hybridized to an RNA, as a substrate for RNA cleaving enzymes including RNase H and dsRNase.
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- Antisense modulation of PPP3CB expression
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Antisense compounds, compositions and methods are provided for modulating the expression of PPP3CB. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PPP3CB. Methods of using these compounds for modulation of PPP3CB expression and for treatment of diseases associated with expression of PPP3CB are provided.
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Page/Page column 18
(2008/06/13)
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- Antisense modulation of perilipin expression
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Antisense compounds, compositions and methods are provided for modulating the expression of perilipin. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding perilipin. Methods of using these compounds for modulation of perilipin expression and for treatment of diseases associated with expression of perilipin are provided.
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Page/Page column 17-18
(2008/06/13)
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- Modulation of diacylglycerol acyltransferase 1 expression
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Compounds, compositions and methods are provided for modulating the expression of diacylglycerol acyltransferase 1. The compositions comprise oligonucleotides, targeted to nucleic acid encoding diacylglycerol acyltransferase 1. Methods of using these compounds for modulation of diacylglycerol acyltransferase 1 expression and for diagnosis and treatment of disease associated with expression of diacylglycerol acyltransferase 1 are provided.
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Page/Page column 12
(2008/06/13)
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- Antisense modulation of fatty acid synthase expression
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Antisense compounds, compositions and methods are provided for modulating the expression of fatty acid synthase. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding fatty acid synthase. Methods of using these compounds for modulation of fatty acid synthase expression and for treatment of diseases associated with expression of fatty acid synthase are provided.
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Page/Page column 17-18
(2010/02/06)
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- Antisense modulation of DEXRAS1 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of DEXRAS1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding DEXRAS1. Methods of using these compounds for modulation of DEXRAS1 expression and for treatment of diseases associated with expression of DEXRAS1 are provided.
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Page/Page column 17
(2008/06/13)
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- Antisense modulation of EDG5 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of EDG5. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding EDG5. Methods of using these compounds for modulation of EDG5 expression and for treatment of diseases associated with expression of EDG5 are provided.
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Page/Page column 17-18
(2008/06/13)
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- ANTISENSE MODULATION OF EDG1 EXPRESSION
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Antisense compounds, compositions and methods are provided for modulating the expression of EDG1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding EDG1. Methods of using these compounds for modulation of EDG1 expression and for treatment of diseases associated with expression of EDG1 are provided.
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Page/Page column 17-18
(2008/06/13)
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- Antisense modulation of cyclin-dependent kinase 6 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of cyclin-dependent kinase 6. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding cyclin-dependent kinase 6. Methods of using these compounds for modulation of cyclin-dependent kinase 6 expression and for treatment of diseases associated with expression of cyclin-dependent kinase 6 are provided.
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Page/Page column 19-20
(2008/06/13)
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- Antisense modulation of hypothetical protein LOC51249 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of hypothetical protein LOC51249. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding hypothetical protein LOC51249. Methods of using these compounds for modulation of hypothetical protein LOC51249 expression and for treatment of diseases associated with expression of hypothetical protein LOC51249 are provided.
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Page/Page column 17-18
(2008/06/13)
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- Antisense modulation of selenophosphate synthetase 2 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of selenophosphate synthetase 2. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding selenophosphate synthetase 2. Methods of using these compounds for modulation of selenophosphate synthetase 2 expression and for treatment of diseases associated with expression of selenophosphate synthetase 2 are provided.
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Page/Page column 17-18
(2008/06/13)
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- Antisense modulation of ADAM12 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of ADAM12. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding ADAM12. Methods of using these compounds for modulation of ADAM12 expression and for treatment of diseases associated with expression of ADAM12 are provided.
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Page/Page column 18
(2008/06/13)
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- Antisense modulation of SMRT expression
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Antisense compounds, compositions and methods are provided for modulating the expression of SMRT. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding SMRT. Methods of using these compounds for modulation of SMRT expression and for treatment of diseases associated with expression of SMRT are provided.
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Page/Page column 18-19
(2008/06/13)
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- Antisense modulation of cyclin-dependent kinase 4 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of cyclin-dependent kinase 4. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding cyclin-dependent kinase 4. Methods of using these compounds for modulation of cyclin-dependent kinase 4 expression and for treatment of diseases associated with expression of cyclin-dependent kinase 4 are provided.
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Page/Page column 21
(2008/06/13)
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- Antisense modulation of insulin-like growth factor 2 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of insulin-like growth factor 2. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding insulin-like growth factor 2. Methods of using these compounds for modulation of insulin-like growth factor 2 expression and for treatment of diseases associated with expression of insulin-like growth factor 2 are provided.
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Page/Page column 20
(2008/06/13)
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- Antisense modulation of PTPRM expression
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Antisense compounds, compositions and methods are provided for modulating the expression of PTPRM. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTPRM. Methods of using these compounds for modulation of PTPRM expression and for treatment of diseases associated with expression of PTPRM are provided.
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Page/Page column 17-18
(2008/06/13)
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- Antisense modulation of HMG-CoA reductase expression
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Antisense compounds, compositions and methods are provided for modulating the expression of HMG-CoA reductase. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding HMG-CoA reductase. Methods of using these compounds for modulation of HMG-CoA reductase expression and for treatment of diseases associated with expression of HMG-CoA reductase are provided.
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Page/Page column 18-19
(2010/02/05)
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- Antisense modulation of P2X4 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of P2X4. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding P2X4. Methods of using these compounds for modulation of P2X4 expression and for treatment of diseases associated with expression of P2X4 are provided.
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Page/Page column 17-18
(2008/06/13)
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- Antisense modulation of phospholipase D2 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of phospholipase D2. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding phospholipase D2. Methods of using these compounds for modulation of phospholipase D2 expression and for treatment of diseases associated with expression of phospholipase D2 are provided.
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Page/Page column 18
(2008/06/13)
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- Antisense modulation of phosphatidylinositol-4-phosphate 5-kinase, type II beta expression
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Antisense compounds, compositions and methods are provided for modulating the expression of phosphatidylinositol-4-phosphate 5-kinase, type II beta. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding phosphatidylinositol-4-phosphate 5-kinase, type II beta. Methods of using these compounds for modulation of phosphatidylinositol-4-phosphate 5-kinase, type II beta expression and for treatment of diseases associated with expression of phosphatidylinositol-4-phosphate 5-kinase, type II beta are provided.
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- Antisense modulation of hypothetical tumor endothelial marker expression
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Antisense compounds, compositions and methods are provided for modulating the expression of hypothetical tumor endothelial marker. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding hypothetical tumor endothelial marker. Methods of using these compounds for modulation of hypothetical tumor endothelial marker expression and for treatment of diseases associated with expression of hypothetical tumor endothelial marker are provided.
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- Antisense modulation of PTPN12 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of PTPN12. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTPN12. Methods of using these compounds for modulation of PTPN12 expression and for treatment of diseases associated with expression of PTPN12 are provided.
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- Phosphatidylinositol-4-phosphate 5-kinase, type II beta inhibitors for inhibiting angiogenesis
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Compounds, compositions and methods are provided for modulating the expression of phosphatidylinositol-4-phosphate 5-kinase, type II beta. The compositions comprise oligonucleotides, targeted to nucleic acid encoding phosphatidylinositol-4-phosphate 5-kinase, type II beta. Methods of using these compounds for modulation of phosphatidylinositol-4-phosphate 5-kinase, type II beta expression and for diagnosis and treatment of disease associated with expression of phosphatidylinositol-4-phosphate 5-kinase, type II beta are provided.
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- Antisense modulation of PRL-3 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of PRL-3. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PRL-3. Methods of using these compounds for modulation of PRL-3 expression and for treatment of diseases associated with expression of PRL-3 are provided.
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- Antisense modulation of transcription factor DP-1 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of transcription factor Dp-1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding transcription factor Dp-1. Methods of using these compounds for modulation of transcription factor Dp-1 expression and for treatment of diseases associated with expression of transcription factor Dp-1 are provided.
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- Antisense modulation of DRAK1 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of DRAK1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding DRAK1. Methods of using these compounds for modulation of DRAK1 expression and for treatment of diseases associated with expression of DRAK1 are provided.
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- Extracellular-signal-regulated kinase-6 inhibitors for inhibiting angiogenesis
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Compounds, compositions and methods are provided for modulating the expression of extracellular-signal-regulated kinase-6. The compositions comprise oligonucleotides, targeted to nucleic acid encoding extracellular-signal-regulated kinase-6. Methods of using these compounds for modulation of extracellular-signal-regulated kinase-6 expression and for diagnosis and treatment of disease associated with expression extracellular-signal-regulated kinase-6 are provided.
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- Antisense modulation of splicing factor R/S-rich 10 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of splicing factor R/S-rich 10. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding splicing factor R/S-rich 10. Methods of using these compounds for modulation of splicing factor R/S-rich 10 expression and for treatment of diseases associated with expression of splicing factor R/S-rich 10 are provided.
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Page column 18-19
(2010/02/03)
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- Antisense modulation of G protein-coupled receptor 49 expression
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Antisense compounds, compositions and methods are provided for modulating the expression of G protein-coupled receptor 49. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding G protein-coupled receptor 49. Methods of using these compounds for modulation of G protein-coupled receptor 49 expression and for treatment of diseases associated with expression of G protein-coupled receptor 49 are provided.
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- OLIGONUCLEOTIDES HAVING MODIFIED NUCLEOSIDE UNITS
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Disclosed are oligonucleotides and oligonucleosides that include one or more modified nucleoside units. The oligonucleotides and oligonucleosides are particularly useful as antisense agents, ribozymes, aptamer, siRNA agents, probes and primers or, when hybridized to an RNA, as a substrate for RNA cleaving enzymes including RNase H and dsRNase.
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Page 219-221
(2010/02/04)
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