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WO2003008635A3 - η-SECRETASE IN VITRO SCREENING ASSAY - Google Patents

η-SECRETASE IN VITRO SCREENING ASSAY Download PDF

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Publication number
WO2003008635A3
WO2003008635A3 PCT/EP2002/007095 EP0207095W WO03008635A3 WO 2003008635 A3 WO2003008635 A3 WO 2003008635A3 EP 0207095 W EP0207095 W EP 0207095W WO 03008635 A3 WO03008635 A3 WO 03008635A3
Authority
WO
WIPO (PCT)
Prior art keywords
secretase
screening assay
vitro screening
substrate
secretase activity
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2002/007095
Other languages
French (fr)
Other versions
WO2003008635A8 (en
WO2003008635A2 (en
Inventor
Cornelia Dorner-Ciossek
Klaus Fuchs
Christian Haass
Markus Kostka
Harald Steiner
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Original Assignee
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
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 Boehringer Ingelheim Pharma GmbH and Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH and Co KG
Priority to MXPA03011898A priority Critical patent/MXPA03011898A/en
Priority to EP02745414A priority patent/EP1407043A2/en
Priority to CA002452832A priority patent/CA2452832A1/en
Priority to JP2003514950A priority patent/JP2004535206A/en
Publication of WO2003008635A2 publication Critical patent/WO2003008635A2/en
Publication of WO2003008635A8 publication Critical patent/WO2003008635A8/en
Anticipated expiration legal-status Critical
Publication of WO2003008635A3 publication Critical patent/WO2003008635A3/en
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

According to the screening method of the invention substances capable of modulating η-secretase activity are identified by incubating a source and a substrate of η-secretase activity with a test substance and detecting a C-terminal fragment released from said substrate.
PCT/EP2002/007095 2001-07-04 2002-06-27 η-SECRETASE IN VITRO SCREENING ASSAY Ceased WO2003008635A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
MXPA03011898A MXPA03011898A (en) 2001-07-04 2002-06-27 gamma-SECRETASE IN VITRO.
EP02745414A EP1407043A2 (en) 2001-07-04 2002-06-27 Gamma-secretase in vitro screening assay
CA002452832A CA2452832A1 (en) 2001-07-04 2002-06-27 .gamma.-secretase in vitro screening assay
JP2003514950A JP2004535206A (en) 2001-07-04 2002-06-27 In vitro screening assay for γ-secretase

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10131899A DE10131899A1 (en) 2001-07-04 2001-07-04 In Vitro Screening Assay for Gamma Secretase
DE10131899.5 2001-07-04

Publications (3)

Publication Number Publication Date
WO2003008635A2 WO2003008635A2 (en) 2003-01-30
WO2003008635A8 WO2003008635A8 (en) 2003-10-30
WO2003008635A3 true WO2003008635A3 (en) 2004-01-29

Family

ID=7690254

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/007095 Ceased WO2003008635A2 (en) 2001-07-04 2002-06-27 η-SECRETASE IN VITRO SCREENING ASSAY

Country Status (6)

Country Link
EP (1) EP1407043A2 (en)
JP (1) JP2004535206A (en)
CA (1) CA2452832A1 (en)
DE (1) DE10131899A1 (en)
MX (1) MXPA03011898A (en)
WO (1) WO2003008635A2 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0229582D0 (en) * 2002-12-19 2003-01-22 Merck Sharp & Dohme Novel assay
DE602006007810D1 (en) 2006-04-21 2009-08-27 Cellzome Ltd Substituted biphenylcarboxylic acids and their derivatives
JP2010520308A (en) 2007-03-07 2010-06-10 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Substituted phenoxyaminothiazolone as an estrogen-related receptor-alpha modulator
TW200902507A (en) 2007-03-07 2009-01-16 Janssen Pharmaceutica Nv Substituted phenoxy n-alkylated thiazolidinediones as estrogen related receptor-α modulators
US20090023158A1 (en) * 2007-07-13 2009-01-22 Elan Pharmaceuticals, Inc. Compositions and Methods for Identifying Substrate Specificity of Inhibitors of Gamma Secretase
WO2009051948A1 (en) 2007-10-17 2009-04-23 Janssen Pharmaceutica, N.V. Biphenyl carboxylic acids and derivatives thereof
AU2008312612B2 (en) 2007-10-19 2013-11-28 Janssen Pharmaceutica, N.V. Piperidinyl and piperazinyl modulators of gamma-secretase
MX2010004310A (en) 2007-10-19 2010-05-03 Janssen Pharmaceutica Nv Carbon linked modulators of y-secretase.
CN101888990B (en) 2007-10-19 2014-01-29 詹森药业有限公司 Amide-linked gamma-secretase modulator
MX2010004318A (en) 2007-10-19 2010-04-30 Janssen Pharmaceutica Nv Amine linked modulators of y-secretase.
US7968725B2 (en) 2008-07-22 2011-06-28 Janssen Pharmaceutica N.V. Pyridinyl modulators of γ-secretase
US9023767B2 (en) 2009-05-07 2015-05-05 Memorial Sloan-Kettering Cancer Center γ-Secretase substrates and methods of use
US9632088B2 (en) 2010-09-07 2017-04-25 Memorial Sloan-Kettering Cancer Center Methods and compositions for gamma-secretase assay
US10030260B2 (en) 2012-10-16 2018-07-24 The Johns Hopkins University Inducible reconstitution and real-time quantitative kinetic system for the study of intramembrane enzymes

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998015828A1 (en) * 1996-10-07 1998-04-16 Scios Inc. Method to identify direct inhibitors of the beta-amyloid forming enzyme gamma-secretase
DE19941039A1 (en) * 1999-08-28 2001-03-01 Boehringer Ingelheim Pharma gamma-secretase in vitro test system

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998015828A1 (en) * 1996-10-07 1998-04-16 Scios Inc. Method to identify direct inhibitors of the beta-amyloid forming enzyme gamma-secretase
DE19941039A1 (en) * 1999-08-28 2001-03-01 Boehringer Ingelheim Pharma gamma-secretase in vitro test system

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
DOVEY H F ET AL: "FUNCTIONAL GAMMA-SECRETASE INHIBITORS REDUCE BETA-AMYLOID PEPTIDE LEVELS IN BRAIN", JOURNAL OF NEUROCHEMISTRY, NEW YORK, NY, US, vol. 76, no. 1, 2001, pages 173 - 181, XP001147446, ISSN: 0022-3042 *
HIGAKI JEFFREY N ET AL: "A combinatorial approach to the identification of dipeptide aldehyde inhibitors of beta-amyloid production", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 19, 1999, pages 3889 - 3898, XP002185434, ISSN: 0022-2623 *
JO DONG-GYU ET AL: "Contribution of presenilin/gamma-secretase to calsenilin-mediated apoptosis.", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 305, no. 1, 23 May 2003 (2003-05-23), pages 62 - 66, XP009016709, ISSN: 0006-291X *
MCLENDON C ET AL: "Cell-free assays for gamma-secretase activity", FASEB JOURNAL, FED. OF AMERICAN SOC. FOR EXPERIMENTAL BIOLOGY, BETHESDA, MD, US, vol. 14, no. 15, December 2000 (2000-12-01), pages 2383 - 2386, XP002217636, ISSN: 0892-6638 *
NISHIMOTO I ET AL: "Alzheimer amyloid protein precursor complexes with brain GTP-binding protein G(o)", NATURE. ENGLAND 4 MAR 1993, vol. 362, no. 6415, 4 March 1993 (1993-03-04), pages 75 - 79, XP001155314, ISSN: 0028-0836 *
PINNIX I ET AL: "A novel gamma -secretase assay based on detection of the putative C-terminal fragment-gamma of amyloid beta protein precursor", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, US, vol. 276, no. 1, 5 January 2001 (2001-01-05), pages 481 - 487, XP002217635, ISSN: 0021-9258 *
ZAIN S B ET AL: "Molecular cloning of amyloid cDNA derived from mRNA of the Alzheimer disease brain: coding and noncoding regions of the fetal precursor mRNA are expressed in the cortex.", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA. UNITED STATES FEB 1988, vol. 85, no. 3, February 1988 (1988-02-01), pages 929 - 933, XP001155313, ISSN: 0027-8424 *

Also Published As

Publication number Publication date
WO2003008635A8 (en) 2003-10-30
EP1407043A2 (en) 2004-04-14
MXPA03011898A (en) 2004-03-26
JP2004535206A (en) 2004-11-25
WO2003008635A2 (en) 2003-01-30
DE10131899A1 (en) 2003-02-27
CA2452832A1 (en) 2003-01-30

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