ATE292801T1 - Verfahren zum screening von inhibitoren von asp2 - Google Patents

Verfahren zum screening von inhibitoren von asp2

Info

Publication number
ATE292801T1
ATE292801T1 AT00969693T AT00969693T ATE292801T1 AT E292801 T1 ATE292801 T1 AT E292801T1 AT 00969693 T AT00969693 T AT 00969693T AT 00969693 T AT00969693 T AT 00969693T AT E292801 T1 ATE292801 T1 AT E292801T1
Authority
AT
Austria
Prior art keywords
cleavage
asp
compounds
substrate
asp2
Prior art date
Application number
AT00969693T
Other languages
English (en)
Inventor
Gary Christie
Ishrut Hussain
David Powell
Original Assignee
Smithkline Beecham Plc
Smithkline Beecham Corp
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 Smithkline Beecham Plc, Smithkline Beecham Corp filed Critical Smithkline Beecham Plc
Application granted granted Critical
Publication of ATE292801T1 publication Critical patent/ATE292801T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4711Alzheimer's disease; Amyloid plaque core protein
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING 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
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6893Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
    • G01N33/6896Neurological disorders, e.g. Alzheimer's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/46Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
    • G01N2333/47Assays involving proteins of known structure or function as defined in the subgroups
    • G01N2333/4701Details
    • G01N2333/4709Amyloid plaque core protein
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/914Hydrolases (3)
    • G01N2333/948Hydrolases (3) acting on peptide bonds (3.4)
    • G01N2333/95Proteinases, i.e. endopeptidases (3.4.21-3.4.99)
    • G01N2333/964Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue
    • G01N2333/96425Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals
    • G01N2333/96427Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general
    • G01N2333/9643Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general with EC number
    • G01N2333/96472Aspartic endopeptidases (3.4.23)
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00Screening for compounds of potential therapeutic value
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00Screening for compounds of potential therapeutic value
    • G01N2500/02Screening involving studying the effect of compounds C on the interaction between interacting molecules A and B (e.g. A = enzyme and B = substrate for A, or A = receptor and B = ligand for the receptor)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Microbiology (AREA)
  • Wood Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Urology & Nephrology (AREA)
  • Public Health (AREA)
  • Toxicology (AREA)
  • Pathology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Physics & Mathematics (AREA)
  • Veterinary Medicine (AREA)
  • Cell Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • General Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Hospice & Palliative Care (AREA)
AT00969693T 1999-10-21 2000-10-19 Verfahren zum screening von inhibitoren von asp2 ATE292801T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9924957.5A GB9924957D0 (en) 1999-10-21 1999-10-21 Novel treatment
PCT/GB2000/004039 WO2001029563A1 (en) 1999-10-21 2000-10-19 Method of screening for inhibitors of asp2

Publications (1)

Publication Number Publication Date
ATE292801T1 true ATE292801T1 (de) 2005-04-15

Family

ID=10863153

Family Applications (1)

Application Number Title Priority Date Filing Date
AT00969693T ATE292801T1 (de) 1999-10-21 2000-10-19 Verfahren zum screening von inhibitoren von asp2

Country Status (9)

Country Link
US (2) US20050277165A1 (de)
EP (1) EP1224469B1 (de)
JP (1) JP2003512043A (de)
AT (1) ATE292801T1 (de)
AU (1) AU7934900A (de)
DE (1) DE60019321T2 (de)
ES (1) ES2240183T3 (de)
GB (1) GB9924957D0 (de)
WO (1) WO2001029563A1 (de)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9701684D0 (en) 1997-01-28 1997-03-19 Smithkline Beecham Plc Novel compounds
US6844148B1 (en) 1998-09-24 2005-01-18 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
PL205294B1 (pl) 1998-09-24 2010-03-31 Upjohn Co Izolowany lub oczyszczony polipeptyd, oczyszczony lub izolowany polinukleotyd, wektor, wektor ekspresyjny, komórka gospodarza, sposób wytwarzania polipeptydu, sposoby identyfikowania czynnika obniżającego, modulującego lub hamującego aktywność, zastosowanie takiego czynnika, izolowany kwas nukleinowy, obejmujący go wektor i ich zastosowanie, sposoby zmniejszania komórkowego wytwarzania beta amyloidu i zastosowanie antysensownego reagenta
US6699671B1 (en) 1998-09-24 2004-03-02 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
US7456007B1 (en) 1998-12-31 2008-11-25 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
US7115410B1 (en) 1999-02-10 2006-10-03 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
GB2364059B (en) 1999-02-10 2004-01-14 Elan Pharm Inc Beta-Secretase enzyme compositions and methods
US7514408B1 (en) 1999-12-02 2009-04-07 Elan Pharmaceuticals, Inc. β-secretase enzyme compositions and methods
DE60124080T2 (de) 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
JP2004502664A (ja) 2000-06-30 2004-01-29 イーラン ファーマスーティカルズ、インコーポレイテッド アルツハイマー病処置用化合物
PE20020276A1 (es) 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
BR0210721A (pt) 2001-06-27 2004-07-20 Elan Pharm Inc Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição
JP4547152B2 (ja) * 2001-10-23 2010-09-22 オクラホマ メディカル リサーチ ファウンデーション β−セクレターゼ阻害剤および使用方法
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
EP2281824A1 (de) 2009-08-07 2011-02-09 Noscira, S.A. Furan-Imidazolon-Derivate zur Behandlung von kognitiven, neurodegenerativen oder neuronalen Erkrankungen oder Funktionsstörungen
WO2012064836A1 (en) 2010-11-10 2012-05-18 Genentech, Inc. Methods and compositions for neural disease immunotherapy
EP2643299B1 (de) 2010-11-22 2016-06-22 Noscira, S.A. Bipyridinsulfonamidderivate zur behandlung von neurodegenerativen erkrankungen oder zuständen
JP2013158281A (ja) * 2012-02-03 2013-08-19 Shionogi & Co Ltd 新規bace1活性測定方法
CN105263900B (zh) * 2013-06-12 2020-09-22 默克专利股份公司 用于治疗关节病的羟基亚乙基衍生物
JP6859259B2 (ja) 2014-11-19 2021-04-14 ジェネンテック, インコーポレイテッド BACElに対する抗体及び神経疾患免疫療法のためのその使用
WO2016081640A1 (en) 2014-11-19 2016-05-26 Genentech, Inc. Anti-transferrin receptor / anti-bace1 multispecific antibodies and methods of use

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5187153A (en) * 1986-11-17 1993-02-16 Scios Nova Inc. Methods of treatment using Alzheimer's amyloid polypeptide derivatives
US4963654A (en) * 1989-02-13 1990-10-16 Taisho Pharmaceutical Co., Ltd. Peptide serine protease inhibitor
US5292652A (en) * 1990-10-05 1994-03-08 Athena Neurosciences, Inc. Amyloidin protease and uses thereof
WO1995013084A1 (en) * 1992-05-11 1995-05-18 Miles Inc. Cathepsin d is an amyloidogenic protease in alzheimer's disease
JPH11507538A (ja) * 1995-06-07 1999-07-06 アテナ ニューロサイエンシズ インコーポレイティド β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ
WO1998015828A1 (en) * 1996-10-07 1998-04-16 Scios Inc. Method to identify direct inhibitors of the beta-amyloid forming enzyme gamma-secretase
GB9701684D0 (en) * 1997-01-28 1997-03-19 Smithkline Beecham Plc Novel compounds
US6699671B1 (en) * 1998-09-24 2004-03-02 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
US6313268B1 (en) * 1998-10-16 2001-11-06 Vivian Y. H. Hook Secretases related to Alzheimer's dementia
CA2374610A1 (en) * 1999-06-28 2001-01-04 Jordan J. N. Tang Catalytically active recombinant memapsin and methods of use thereof

Also Published As

Publication number Publication date
JP2003512043A (ja) 2003-04-02
WO2001029563A1 (en) 2001-04-26
GB9924957D0 (en) 1999-12-22
AU7934900A (en) 2001-04-30
DE60019321D1 (de) 2005-05-12
EP1224469B1 (de) 2005-04-06
ES2240183T3 (es) 2005-10-16
US20070021348A1 (en) 2007-01-25
DE60019321T2 (de) 2005-09-08
US20050277165A1 (en) 2005-12-15
EP1224469A1 (de) 2002-07-24

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