WO2003070912A3 - RNA INTERFERENCE MEDIATED INHIBITION OF EPIDERMAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) - Google Patents

RNA INTERFERENCE MEDIATED INHIBITION OF EPIDERMAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) Download PDF

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Publication number
WO2003070912A3
WO2003070912A3 PCT/US2003/005045 US0305045W WO03070912A3 WO 2003070912 A3 WO2003070912 A3 WO 2003070912A3 US 0305045 W US0305045 W US 0305045W WO 03070912 A3 WO03070912 A3 WO 03070912A3
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WO
WIPO (PCT)
Prior art keywords
nucleic acid
short interfering
sina
rna
gene expression
Prior art date
Application number
PCT/US2003/005045
Other languages
French (fr)
Other versions
WO2003070912A2 (en
Inventor
James Mcswiggen
Pamela Pavco
Leonid Beigelman
Kathy Fosnaugh
Sharon Jamison
Original Assignee
Sirna Therapeutics Inc
James Mcswiggen
Pamela Pavco
Leonid Beigelman
Kathy Fosnaugh
Sharon Jamison
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US09/916,466 external-priority patent/US20030064945A1/en
Priority claimed from PCT/US2002/016840 external-priority patent/WO2002097114A2/en
Priority claimed from US10/251,117 external-priority patent/US20030170891A1/en
Priority claimed from US10/277,494 external-priority patent/US20030186909A1/en
Application filed by Sirna Therapeutics Inc, James Mcswiggen, Pamela Pavco, Leonid Beigelman, Kathy Fosnaugh, Sharon Jamison filed Critical Sirna Therapeutics Inc
Priority to JP2003569805A priority Critical patent/JP2005517437A/en
Priority to AU2003219818A priority patent/AU2003219818A1/en
Priority to EP03716093A priority patent/EP1501853A4/en
Publication of WO2003070912A2 publication Critical patent/WO2003070912A2/en
Priority to US10/923,354 priority patent/US20050176024A1/en
Publication of WO2003070912A3 publication Critical patent/WO2003070912A3/en

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C12N15/1138—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against receptors or cell surface proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/14—Type of nucleic acid interfering N.A.
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/315—Phosphorothioates
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/317—Chemical structure of the backbone with an inverted bond, e.g. a cap structure
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/318—Chemical structure of the backbone where the PO2 is completely replaced, e.g. MMI or formacetal
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/321—2'-O-R Modification
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    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/322—2'-R Modification
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/33—Chemical structure of the base
    • C12N2310/332—Abasic residue
    • C—CHEMISTRY; METALLURGY
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/50—Physical structure
    • C12N2310/53—Physical structure partially self-complementary or closed

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Genetics & Genomics (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
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  • Wood Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
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  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention concerns methods and reagents useful in modulating EGFR gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules capable of mediating RNA interference (RNAi) against HER1, HER2, HER3 and/or HER4. The small nucleic acid molecules are useful in the treatment and diagnosis of cancer.
PCT/US2003/005045 2001-05-18 2003-02-20 RNA INTERFERENCE MEDIATED INHIBITION OF EPIDERMAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) WO2003070912A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2003569805A JP2005517437A (en) 2002-02-20 2003-02-20 RNA interference-mediated inhibition of epidermal growth factor receptor gene expression using short interfering nucleic acids (siNa)
AU2003219818A AU2003219818A1 (en) 2002-02-20 2003-02-20 RNA INTERFERENCE MEDIATED INHIBITION OF EPIDERMAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
EP03716093A EP1501853A4 (en) 2002-02-20 2003-02-20 RNA INTERFERENCE MEDIATED INHIBITION OF EPIDERMAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US10/923,354 US20050176024A1 (en) 2001-05-18 2004-08-20 RNA interference mediated inhibition of epidermal growth factor receptor (EGFR) gene expression using short interfering nucleic acid (siNA)

Applications Claiming Priority (26)

Application Number Priority Date Filing Date Title
US29624901P 2001-06-06 2001-06-06
US09/916,466 US20030064945A1 (en) 1997-01-31 2001-07-25 Enzymatic nucleic acid treatment of diseases or conditions related to levels of epidermal growth factor receptors
US35858002P 2002-02-20 2002-02-20
US60/358,580 2002-02-20
US36312402P 2002-03-11 2002-03-11
US60/363,124 2002-03-11
USPCT/US02/16840 2002-05-29
PCT/US2002/016840 WO2002097114A2 (en) 2001-05-29 2002-05-29 Nucleic acid treatment of diseases or conditions related to levels of ras, her2 and hiv
US38678202P 2002-06-06 2002-06-06
US10/163,552 US20030105051A1 (en) 2001-05-29 2002-06-06 Nucleic acid treatment of diseases or conditions related to levels of HER2
US60/386,782 2002-06-06
US10/163,552 2002-06-06
US39392402P 2002-07-03 2002-07-03
US60/393,924 2002-07-03
US40678402P 2002-08-29 2002-08-29
US60/406,784 2002-08-29
US40837802P 2002-09-05 2002-09-05
US60/408,378 2002-09-05
US40929302P 2002-09-09 2002-09-09
US60/409,293 2002-09-09
US10/251,117 US20030170891A1 (en) 2001-06-06 2002-09-19 RNA interference mediated inhibition of epidermal growth factor receptor gene expression using short interfering nucleic acid (siNA)
US10/251,117 2002-09-19
US10/277,494 2002-10-21
US10/277,494 US20030186909A1 (en) 1997-01-27 2002-10-21 Nucleic acid treatment of diseases or conditions related to levels of epidermal growth factor receptors
US44012903P 2003-01-15 2003-01-15
US60/440,129 2003-01-15

Related Parent Applications (3)

Application Number Title Priority Date Filing Date
US10/163,552 Continuation-In-Part US20030105051A1 (en) 2001-05-18 2002-06-06 Nucleic acid treatment of diseases or conditions related to levels of HER2
US10/251,117 Continuation-In-Part US20030170891A1 (en) 2001-05-18 2002-09-19 RNA interference mediated inhibition of epidermal growth factor receptor gene expression using short interfering nucleic acid (siNA)
US10/277,494 Continuation-In-Part US20030186909A1 (en) 1997-01-27 2002-10-21 Nucleic acid treatment of diseases or conditions related to levels of epidermal growth factor receptors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US10/923,354 Continuation-In-Part US20050176024A1 (en) 2001-05-18 2004-08-20 RNA interference mediated inhibition of epidermal growth factor receptor (EGFR) gene expression using short interfering nucleic acid (siNA)

Publications (2)

Publication Number Publication Date
WO2003070912A2 WO2003070912A2 (en) 2003-08-28
WO2003070912A3 true WO2003070912A3 (en) 2004-11-11

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PCT/US2003/005045 WO2003070912A2 (en) 2001-05-18 2003-02-20 RNA INTERFERENCE MEDIATED INHIBITION OF EPIDERMAL GROWTH FACTOR RECEPTOR GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)

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WO (1) WO2003070912A2 (en)

Cited By (1)

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US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof

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US9181551B2 (en) 2002-02-20 2015-11-10 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA)
US9657294B2 (en) 2002-02-20 2017-05-23 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA)
AU2012216354B2 (en) * 2002-08-05 2016-01-14 Silence Therapeutics Gmbh Further novel forms of interfering RNA molecules
MXPA05001355A (en) 2002-08-05 2005-09-30 Atugen Ag Further novel forms of interfering rna molecules.
CA2546074A1 (en) * 2003-11-14 2005-06-02 Yale University Syk-targeted nucleic acid interference
US8815599B2 (en) 2004-06-01 2014-08-26 Pronai Therapeutics, Inc. Methods and compositions for the inhibition of gene expression
GB2424886A (en) * 2005-04-04 2006-10-11 Dxs Ltd Polynucleotide primers against epidermal growth factor receptor and method of detecting gene mutations
JP5242377B2 (en) * 2005-04-12 2013-07-24 ユニヴァルシテ リブレ デ ブリュッセル Use of RNAi-based approaches targeting galectin-1 to treat cancer
AU2006315099C1 (en) * 2005-11-21 2013-01-10 Johnson & Johnson Research Pty Limited Multitargeting interfering RNAs and methods of their use and design
EP1957044B1 (en) 2005-12-01 2013-03-13 Pronai Therapeutics, Inc. Amphoteric liposome formulation
ES2534430T3 (en) * 2006-08-28 2015-04-22 The University Of Western Australia Modulation method of epidermal growth factor receptor (EGFR) expression that involves miRNA
JP2010519906A (en) * 2007-03-02 2010-06-10 エムディーアールエヌエー，インコーポレイテッド NUCLEIC ACID COMPOUND AND USE THEREOF FOR SUPPRESSING EXPRESSION OF ERBB FAMILY GENE
WO2008109373A1 (en) * 2007-03-02 2008-09-12 Mdrna, Inc. Nucleic acid compounds for inhibiting erbb gene expression and uses thereof
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US8652787B2 (en) 2008-11-12 2014-02-18 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Use of ERBB4 as a prognostic and therapeutic marker for melanoma
JP2010263850A (en) * 2009-05-15 2010-11-25 Toyota Motor Corp Dna marker characteristic of plant of genus erianthus
US9168297B2 (en) 2010-06-23 2015-10-27 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Regulation of skin pigmentation by neuregulin-1 (NRG-1)
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WO2012027206A1 (en) 2010-08-24 2012-03-01 Merck Sharp & Dohme Corp. SINGLE-STRANDED RNAi AGENTS CONTAINING AN INTERNAL, NON-NUCLEIC ACID SPACER
WO2012040124A1 (en) 2010-09-22 2012-03-29 Alios Biopharma, Inc. Azido nucleosides and nucleotide analogs
EP3327125B1 (en) 2010-10-29 2020-08-05 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
EP2474617A1 (en) 2011-01-11 2012-07-11 InteRNA Technologies BV Mir for treating neo-angiogenesis
AP2014007796A0 (en) 2011-12-22 2014-07-31 Alios Biopharma Inc Substituted nucleosides, nucleotides and analogs thereof
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
SG10201804835VA (en) 2013-10-11 2018-07-30 Alios Biopharma Inc Substituted nucleosides, nucleotides and analogs thereof
MA45349A (en) * 2016-04-01 2019-02-06 Avidity Biosciences Llc EGFR NUCLEIC ACIDS AND THEIR USES
CN107881242A (en) * 2016-09-29 2018-04-06 广州康昕瑞基因健康科技有限公司 EGFR gene detection kit and detection method
EP3693465A1 (en) * 2019-02-05 2020-08-12 Pharmaq AS Novel fish coronavirus
CR20220316A (en) 2019-12-06 2022-10-07 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
US12014835B2 (en) 2020-02-19 2024-06-18 Vanderbilt University Methods for evaluating therapeutic benefit of combination therapies
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CN117794920A (en) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 N- (hydroxyalkyl (hetero) aryl) tetrahydrofurancarboxamides as sodium channel modulators

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