CA2301201A1 - Procede d'inhibition de la cathepsine k - Google Patents

Procede d'inhibition de la cathepsine k Download PDF

Info

Publication number
CA2301201A1
CA2301201A1 CA002301201A CA2301201A CA2301201A1 CA 2301201 A1 CA2301201 A1 CA 2301201A1 CA 002301201 A CA002301201 A CA 002301201A CA 2301201 A CA2301201 A CA 2301201A CA 2301201 A1 CA2301201 A1 CA 2301201A1
Authority
CA
Canada
Prior art keywords
active site
procathepsin
cathepsin
lys
asn
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.)
Abandoned
Application number
CA002301201A
Other languages
English (en)
Inventor
Sherin S. Abdel-Meguid
Ward W. Smith
Cheryl Janson
Baoquang Zhao
Judith Lalonde
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.)
SmithKline Beecham Corp
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2301201A1 publication Critical patent/CA2301201A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6402—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from non-mammals
    • C12N9/6405—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from non-mammals not being snakes
    • C12N9/641—Cysteine endopeptidases (3.4.22)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/08—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81—Protease inhibitors
    • C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/8139—Cysteine protease (E.C. 3.4.22) inhibitors, e.g. cystatin

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

On a identifié une nouvelle structure cristalline de cathepsine K. La présente invention concerne également des procédés qui permettent d'identifier des inhibiteurs de cathepsine K et des procédés qui permettent de mettre au point des inhibiteurs de cathepsine K à l'aide de données structurelles et physiques fondées sur la structure cristallographique de la procathepsine K.
CA002301201A 1998-08-14 1998-08-14 Procede d'inhibition de la cathepsine k Abandoned CA2301201A1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1998/014634 WO2000009653A2 (fr) 1998-08-14 1998-08-14 Procede d'inhibition de la cathepsine k

Publications (1)

Publication Number Publication Date
CA2301201A1 true CA2301201A1 (fr) 2000-02-24

Family

ID=22267483

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002301201A Abandoned CA2301201A1 (fr) 1998-08-14 1998-08-14 Procede d'inhibition de la cathepsine k

Country Status (3)

Country Link
JP (1) JP2003527819A (fr)
CA (1) CA2301201A1 (fr)
WO (1) WO2000009653A2 (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
CN1416346A (zh) 2000-03-21 2003-05-07 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
EP1379634B1 (fr) * 2001-04-20 2017-12-13 The University Of Georgia Research Foundation, Inc. Inactivateurs de site actif
WO2007012180A1 (fr) * 2005-07-26 2007-02-01 Merck Frosst Canada Ltd. Inhibiteurs de la cystéine protéase de la famille de la papaïne pour le traitement des maladies parasitaires
EP2225196B1 (fr) 2007-11-29 2015-01-28 Merck Canada Inc. Inhibiteurs de cystéine-protéases pour le traitement de maladies parasitaires
WO2009087379A2 (fr) 2008-01-09 2009-07-16 Amura Therapeutics Limited Composés

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ132798A3 (cs) * 1995-10-30 1999-02-17 Smithkline Beecham Corporation Inhibitory proteázy
CZ206097A3 (cs) * 1995-10-30 1999-02-17 Smithkline Beecham Corporation Způsob inhibice kathepsinu K

Also Published As

Publication number Publication date
WO2000009653A2 (fr) 2000-02-24
JP2003527819A (ja) 2003-09-24
WO2000009653A3 (fr) 2007-05-24

Similar Documents

Publication Publication Date Title
US5856116A (en) Crystal structure and mutants of interleukin-1 beta converting enzyme
US6274336B1 (en) Method of inhibiting cathepsin K
Oefner et al. Structure of human neutral endopeptidase (Neprilysin) complexed with phosphoramidon
Orth et al. Crystal structure of the catalytic domain of human ADAM33
Harmat et al. The structure of MBL-associated serine protease-2 reveals that identical substrate specificities of C1s and MASP-2 are realized through different sets of enzyme–substrate interactions
Marquardt et al. The crystal structure of human α1-tryptase reveals a blocked substrate-binding region
WO2008109871A2 (fr) Structure cristalline de proprotéine convertase 9 (pcsk9) et utilisations de celle-ci
Medrano et al. Structure of proline iminopeptidase from Xanthomonas campestris pv. citri: a prototype for the prolyl oligopeptidase family
US20100030487A1 (en) THREE DIMENSIONAL COORDINATES OF HPTPbeta
Vath et al. The crystal structure of exfoliative toxin B: a superantigen with enzymatic activity
Tang et al. Crystal structure of earthworm fibrinolytic enzyme component a: revealing the structural determinants of its dual fibrinolytic activity
Ljunggren et al. Crystal structure of the parasite protease inhibitor chagasin in complex with a host target cysteine protease
Hasan et al. Mechanisms of Arg-Pro-Pro-Gly-Phe inhibition of thrombin
Dubin et al. Enzymatic activity of the Staphylococcus aureus SplB serine protease is induced by substrates containing the sequence Trp-Glu-Leu-Gln
Stec-Niemczyk et al. Structural and functional characterization of SplA, an exclusively specific protease of Staphylococcus aureus
Kagawa et al. Model for substrate interactions in C5a peptidase from Streptococcus pyogenes: A 1.9 Å crystal structure of the active form of ScpA
Symersky et al. High-resolution structure of the extracellular aspartic proteinase from Candida tropicalis yeast
CA2301201A1 (fr) Procede d'inhibition de la cathepsine k
Fischer et al. Structural mechanisms of inactivation in scabies mite serine protease paralogues
Shin et al. Crystal structure analyses of uncomplexed ecotin in two crystal forms: implications for its function and stability
EP1053304B1 (fr) Enzyme de conversion cristalline du facteur tnf alpha et ses utilisations
US6008033A (en) Proteases, compositions capable of binding to said site, and methods of use thereof
US6842704B2 (en) Crystalline TNF-α-converting enzyme and uses thereof
US20060014934A1 (en) Crystal structure of factor Vai and method for identifying blood factor Va modulators
WO2000077184A9 (fr) Cristaux de caspase-8 et modeles et procedes correspondants

Legal Events

Date Code Title Description
FZDE Dead