WO2003066885A3 - Method for screening for compounds having hdac inhibitory activity - Google Patents

Method for screening for compounds having hdac inhibitory activity Download PDF

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Publication number
WO2003066885A3
WO2003066885A3 PCT/EP2003/001228 EP0301228W WO03066885A3 WO 2003066885 A3 WO2003066885 A3 WO 2003066885A3 EP 0301228 W EP0301228 W EP 0301228W WO 03066885 A3 WO03066885 A3 WO 03066885A3
Authority
WO
WIPO (PCT)
Prior art keywords
screening
inhibitory activity
compounds
hdac
hdac inhibitory
Prior art date
Application number
PCT/EP2003/001228
Other languages
French (fr)
Other versions
WO2003066885A2 (en
Inventor
Fredericus Alphonsu Asselbergs
Peter Wisdom Atadja
Jonathan Hall
Bernd Kinzel
Original Assignee
Novartis Ag
Novartis Pharma Gmbh
Fredericus Alphonsu Asselbergs
Peter Wisdom Atadja
Jonathan Hall
Bernd Kinzel
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
Application filed by Novartis Ag, Novartis Pharma Gmbh, Fredericus Alphonsu Asselbergs, Peter Wisdom Atadja, Jonathan Hall, Bernd Kinzel filed Critical Novartis Ag
Priority to US10/503,186 priority Critical patent/US20050118596A1/en
Priority to EP03709701A priority patent/EP1476565A2/en
Priority to AU2003214055A priority patent/AU2003214055A1/en
Priority to JP2003566233A priority patent/JP2006505241A/en
Publication of WO2003066885A2 publication Critical patent/WO2003066885A2/en
Publication of WO2003066885A3 publication Critical patent/WO2003066885A3/en

Links

Classifications

    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57484—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, metabolites
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/44—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving esterase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value

Abstract

The invention relates to the use of Fra -1 levels as a marker for HDAC inhibition. Also disclosed are in vivo and in vitro methods for screening a compound for HDAC inhibitory activity, as well as methods for monitoring the therapeutic efficacy of an HDAC inhibitor in a subject in vivo and for determining resistance to an HDAC inhibitor in vitro or in vivo.
PCT/EP2003/001228 2002-02-08 2003-02-07 Method for screening for compounds having hdac inhibitory activity WO2003066885A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
US10/503,186 US20050118596A1 (en) 2002-02-08 2003-02-07 Method for screening for compounds having hdac inhibitory activity
EP03709701A EP1476565A2 (en) 2002-02-08 2003-02-07 Method for screening for compounds having hdac inhibitory activity
AU2003214055A AU2003214055A1 (en) 2002-02-08 2003-02-07 Method for screening for compounds having hdac inhibitory activity
JP2003566233A JP2006505241A (en) 2002-02-08 2003-02-07 Method for screening compound having HDAC inhibitory activity

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US35531102P 2002-02-08 2002-02-08
US60/355,311 2002-02-08

Publications (2)

Publication Number Publication Date
WO2003066885A2 WO2003066885A2 (en) 2003-08-14
WO2003066885A3 true WO2003066885A3 (en) 2003-12-11

Family

ID=27734500

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/001228 WO2003066885A2 (en) 2002-02-08 2003-02-07 Method for screening for compounds having hdac inhibitory activity

Country Status (5)

Country Link
US (1) US20050118596A1 (en)
EP (1) EP1476565A2 (en)
JP (1) JP2006505241A (en)
AU (1) AU2003214055A1 (en)
WO (1) WO2003066885A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7732475B2 (en) 2005-07-14 2010-06-08 Takeda San Diego, Inc. Histone deacetylase inhibitors
US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004074478A1 (en) * 2003-02-19 2004-09-02 Astellas Pharma Inc. Method of estimating antitumor effect of histone deacetylase inhibitor
WO2006042035A2 (en) * 2004-10-07 2006-04-20 Pharmacyclics, Inc. Method of monitoring anti-tumor activity of an hdac inhibitor
GB0606096D0 (en) * 2006-03-27 2006-05-03 Cbmm Sa Screening method
NZ617066A (en) 2008-12-23 2015-02-27 Gilead Pharmasset Llc Nucleoside analogs
CA2748057C (en) 2008-12-23 2018-07-03 Pharmasset, Inc. Nucleoside phosphoramidates
AU2010313255B2 (en) 2009-10-30 2015-04-30 Massachusetts Institute Of Technology The use of CI-994 and dinaline for the treatment of memory/cognition and anxiety disorders
CL2011000716A1 (en) 2010-03-31 2012-04-20 Gilead Pharmasset Llc Crystalline forms 1 6 of (s) -isopropyl-2 - (((s) - (((2r.3r.4r.5r) -5- (2,4-dioxo-3,4-dihydropyrimidin-1 (2h) -yl) -4-fluoro-3-hydroxy-4-methyl tetrahydrofuran-2-yl) methoxy) (phenoxy) phosphoryl) amino) propanoate; pharmaceutical composition and combination; and its use to treat a hepatitis c virus infection.
US20150141470A1 (en) 2012-05-08 2015-05-21 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
FR2993461B1 (en) 2012-07-19 2014-08-08 Genethon USE OF EPIGENOUS-MODIFYING COMPOUNDS FOR THE TREATMENT OF MUSCLE GENE DISEASES ASSOCIATED WITH AN ANOMALY OF PROTEIN CONFORMATION

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6068987A (en) * 1996-09-20 2000-05-30 Merck & Co., Inc. Histone deacetylase as target for antiprotozoal agents
WO2003035843A2 (en) * 2001-10-25 2003-05-01 Buck Institute For Age Research Screening system for modulators of her2 mediated transcription and her2 modulators identifed thereby

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050260649A1 (en) * 2001-02-12 2005-11-24 The Penn State Research Foundation Fra-1 expression in brain cancer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6068987A (en) * 1996-09-20 2000-05-30 Merck & Co., Inc. Histone deacetylase as target for antiprotozoal agents
WO2003035843A2 (en) * 2001-10-25 2003-05-01 Buck Institute For Age Research Screening system for modulators of her2 mediated transcription and her2 modulators identifed thereby

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
ABRAMOVA M V ET AL: "Selective repression of c-fos gene transcription in rat embryo fibroblasts transformed by oncogenes E1A and cHa-ras.", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS. UNITED STATES 27 JUN 2003, vol. 306, no. 2, 27 June 2003 (2003-06-27), pages 483 - 487, XP002257584, ISSN: 0006-291X *
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; January 2002 (2002-01-01), ABRAMOVA M V ET AL: "[Role of the TCF phosphorylation state and the chromatin structure in the negative transcription regulation of the c-fos proto-oncogene in E1A + c-Ha-ras transformed cells]", XP002257586, Database accession no. NLM11862715 *
KUKUSHKIN ALEXANDER N ET AL: "Downregulation of c-fos gene transcription in cells transformed by E1A and cHa-ras oncogenes: a role of sustained activation of MAP/ERK kinase cascade and of inactive chromatin structure at c-fos promoter.", ONCOGENE. ENGLAND 24 JAN 2002, vol. 21, no. 5, 24 January 2002 (2002-01-24), pages 719 - 730, XP002257585, ISSN: 0950-9232 *
MOLEKULIARNAIA BIOLOGIIA. RUSSIA 2002 JAN-FEB, vol. 36, no. 1, January 2002 (2002-01-01), pages 66 - 75, ISSN: 0026-8984 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7732475B2 (en) 2005-07-14 2010-06-08 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7741494B2 (en) 2005-07-14 2010-06-22 Takeda San Diego, Inc. Histone deacetylase inhibitors
US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides

Also Published As

Publication number Publication date
JP2006505241A (en) 2006-02-16
WO2003066885A2 (en) 2003-08-14
AU2003214055A8 (en) 2003-09-02
EP1476565A2 (en) 2004-11-17
US20050118596A1 (en) 2005-06-02
AU2003214055A1 (en) 2003-09-02

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