WO1996035788A3 - Peptides inhibiteurs de proteases de type kunitz - Google Patents

Peptides inhibiteurs de proteases de type kunitz Download PDF

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Publication number
WO1996035788A3
WO1996035788A3 PCT/US1996/006384 US9606384W WO9635788A3 WO 1996035788 A3 WO1996035788 A3 WO 1996035788A3 US 9606384 W US9606384 W US 9606384W WO 9635788 A3 WO9635788 A3 WO 9635788A3
Authority
WO
WIPO (PCT)
Prior art keywords
analogues
kpi
protease inhibitors
type protease
kunitz type
Prior art date
Application number
PCT/US1996/006384
Other languages
English (en)
Other versions
WO1996035788A2 (fr
Inventor
Tyler R White
Deborah Damm
David D Lesikar
Kethleen Mcfadden
Brett L Garrick
Original Assignee
Scios Inc
Tyler R White
Deborah Damm
David D Lesikar
Kethleen Mcfadden
Brett L Garrick
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 Scios Inc, Tyler R White, Deborah Damm, David D Lesikar, Kethleen Mcfadden, Brett L Garrick filed Critical Scios Inc
Priority to JP8534170A priority Critical patent/JPH11504938A/ja
Priority to AU58540/96A priority patent/AU5854096A/en
Priority to EP96920140A priority patent/EP0827539A2/fr
Publication of WO1996035788A2 publication Critical patent/WO1996035788A2/fr
Publication of WO1996035788A3 publication Critical patent/WO1996035788A3/fr

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    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81Protease inhibitors
    • C07K14/8107Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/811Serine protease (E.C. 3.4.21) inhibitors
    • C07K14/8114Kunitz type inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55Protease inhibitors
    • A61K38/57Protease inhibitors from animals; from humans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81Protease inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2319/00Fusion polypeptide
    • C07K2319/01Fusion polypeptide containing a localisation/targetting motif
    • C07K2319/02Fusion polypeptide containing a localisation/targetting motif containing a signal sequence

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Wood Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

L'invention se rapporte à des analogues du domaine des inhibiteurs de protéases de type Kunitz (KPI) d'une protéine précurseur amyloïde qui se lient et inhibent l'activité des sérine protéases, telles que la kallikréine, la plasmine, et des facteurs de coagulation tels que les facteurs VIIa, IXa, Xa, XIa et XIIa. Des compositions pharmaceutiques contenant les analogues de KPI, ainsi que les procédés d'utilisation de ces compositions, sont utiles pour améliorer et traiter des pathologies cliniques associées à l'activité de la sérine protéase, telles que des pertes de sang liées à des interventions chirurgicales impliquant une circulation extracorporelle. L'invention se rapporte également à des séquences nucléotidiques codant ces analogues et à des systèmes d'expression des peptides selon l'invention.
PCT/US1996/006384 1995-05-08 1996-05-08 Peptides inhibiteurs de proteases de type kunitz WO1996035788A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP8534170A JPH11504938A (ja) 1995-05-08 1996-05-08 クニッツ型プロテアーゼ阻害因子
AU58540/96A AU5854096A (en) 1995-05-08 1996-05-08 Kunitz type protease inhibitors
EP96920140A EP0827539A2 (fr) 1995-05-08 1996-05-08 Peptides inhibiteurs de proteases de type kunitz

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US43655595A 1995-05-08 1995-05-08
US64373196A 1996-05-06 1996-05-06
US08/436,555 1996-05-06
US08/643,731 1996-05-06

Publications (2)

Publication Number Publication Date
WO1996035788A2 WO1996035788A2 (fr) 1996-11-14
WO1996035788A3 true WO1996035788A3 (fr) 1996-12-12

Family

ID=27031013

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1996/006384 WO1996035788A2 (fr) 1995-05-08 1996-05-08 Peptides inhibiteurs de proteases de type kunitz

Country Status (6)

Country Link
EP (1) EP0827539A2 (fr)
JP (1) JPH11504938A (fr)
KR (1) KR19990008458A (fr)
AU (1) AU5854096A (fr)
CA (1) CA2220497A1 (fr)
WO (1) WO1996035788A2 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8921314B2 (en) 2008-10-15 2014-12-30 Angiochem, Inc. Conjugates of GLP-1 agonists and uses thereof
US9161988B2 (en) 2009-07-02 2015-10-20 Angiochem Inc. Multimeric peptide conjugates and uses thereof
US9173891B2 (en) 2009-04-20 2015-11-03 Angiochem, Inc. Treatment of ovarian cancer using an anticancer agent conjugated to an angiopep-2 analog
US9221867B2 (en) 2003-01-06 2015-12-29 Angiochem Inc. Method for transporting a compound across the blood-brain barrier
US9365634B2 (en) 2007-05-29 2016-06-14 Angiochem Inc. Aprotinin-like polypeptides for delivering agents conjugated thereto to tissues

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5663143A (en) * 1988-09-02 1997-09-02 Dyax Corp. Engineered human-derived kunitz domains that inhibit human neutrophil elastase
US6057287A (en) 1994-01-11 2000-05-02 Dyax Corp. Kallikrein-binding "Kunitz domain" proteins and analogues thereof
HU226419B1 (en) 1996-03-11 2008-12-29 Aerovance Human bikunin
AU4207499A (en) * 1998-05-28 1999-12-13 Zymogenetics Inc. Kunitz domain polypeptide and materials and methods for making it
JP2002517197A (ja) * 1998-06-03 2002-06-18 サイオス,インコーポレーテッド プロテアーゼインヒビターペプチド
US7153829B2 (en) 2002-06-07 2006-12-26 Dyax Corp. Kallikrein-inhibitor therapies
PT2311432E (pt) 2002-06-07 2015-02-09 Dyax Corp Polipeptídeos de domínio kunitz modificado e sua utilização para a redução de isquemia ou aparecimento de uma resposta inflamatória sistémica associada a um procedimento cirúrgico
US7235530B2 (en) 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
DK2360258T3 (en) 2005-02-18 2015-01-12 Angiochem Inc Aprotininpolypeptider to transport a compound of blood-brain-barrier
EP1907009A4 (fr) 2005-07-15 2009-09-02 Angiochem Inc Utilisation de polypeptides de l'aprotinine comme vehicules dans des conjugues pharmaceutiques
CN101952309A (zh) * 2007-12-21 2011-01-19 Ifxa有限公司 蛋白酶抑制剂
AU2009322043A1 (en) 2008-12-05 2011-07-07 Angiochem Inc. Conjugates of neurotensin or neurotensin analogs and uses thereof
AU2010203712A1 (en) 2009-01-06 2010-07-15 Dyax Corp. Treatment of mucositis with kallikrein inhibitors
LT2521568T (lt) 2010-01-06 2018-12-10 Dyax Corp. Plazmos kalikreiną surišantys baltymai
CN105713092B (zh) 2011-01-06 2019-09-10 戴埃克斯有限公司 血浆前激肽释放酶结合蛋白
EP2885318A4 (fr) 2012-08-14 2016-03-30 Angiochem Inc Conjugués peptides-dendrimères et leurs utilisations
DK3307326T3 (da) 2015-06-15 2020-10-19 Angiochem Inc Fremgangsmåder til behandling af leptomeningeal karcinomatose
CN108699134A (zh) * 2015-12-10 2018-10-23 国家生物技术研究所公司 淀粉样β-蛋白前体抑制剂结构域的变体
AU2016366557B2 (en) 2015-12-11 2024-01-25 Takeda Pharmaceutical Company Limited Plasma kallikrein inhibitors and uses thereof for treating hereditary angioedema attack
CN110051830A (zh) * 2019-03-14 2019-07-26 苏州新凝生物医药科技有限公司 一种protease nexin II\KPI蛋白突变体的应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0393431A1 (fr) * 1989-04-18 1990-10-24 Bayer Ag Homologues de l'inhibiteur de la protéase d'Alzheimer préparés de manière génétique, des souches hôtes et vecteurs d'expression pour leur préparation et leur utilisation comme médicament
WO1993014119A1 (fr) * 1992-01-07 1993-07-22 Novo Nordisk A/S Variants inhibiteurs de type kunitz de la protease humaine
WO1993014120A1 (fr) * 1992-01-07 1993-07-22 Novo Nordisk A/S Variant inhibiteur de la protease humaine de type kunitz
WO1995023860A2 (fr) * 1994-03-04 1995-09-08 Genentech, Inc. PROTEINES INHIBITRICES PROPRES AU DOMAINE DE KÜNITZ DERIVEES DE L'INHIBITEUR DU PRECURSEUR DE LA β-PROTEINE AMYLOIDE DE LA MALADIE D'ALZHEIMER

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0393431A1 (fr) * 1989-04-18 1990-10-24 Bayer Ag Homologues de l'inhibiteur de la protéase d'Alzheimer préparés de manière génétique, des souches hôtes et vecteurs d'expression pour leur préparation et leur utilisation comme médicament
WO1993014119A1 (fr) * 1992-01-07 1993-07-22 Novo Nordisk A/S Variants inhibiteurs de type kunitz de la protease humaine
WO1993014120A1 (fr) * 1992-01-07 1993-07-22 Novo Nordisk A/S Variant inhibiteur de la protease humaine de type kunitz
WO1995023860A2 (fr) * 1994-03-04 1995-09-08 Genentech, Inc. PROTEINES INHIBITRICES PROPRES AU DOMAINE DE KÜNITZ DERIVEES DE L'INHIBITEUR DU PRECURSEUR DE LA β-PROTEINE AMYLOIDE DE LA MALADIE D'ALZHEIMER

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
DENNIS M S ET AL: "Kunitz domain inhibitors of tissue factor-factor VIIa: I. Potent inhibitors selected from libraries by phage display.", JOURNAL OF BIOLOGICAL CHEMISTRY 269 (35). 1994. 22129-22136. ISSN: 0021-9258, XP002015893 *
DENNIS M S ET AL: "Kunitz domain inhibitors of tissue factor-factor VIIa: II. Potent and specific inhibitors by competitive phage selection.", JOURNAL OF BIOLOGICAL CHEMISTRY 269 (35). 1994. 22137-22144. ISSN: 0021-9258, XP002015892 *
DENNIS M S ET AL: "Potent and Selective Kunitz Domain Inhibitors of Plasma Kallikrein Designed by Phage Display.", JOURNAL OF BIOLOGICAL CHEMISTRY 270 (43). 1995. 25411-25417. ISSN: 0021-9258, XP002015896 *
HYNES T R ET AL: "X-RAY CRYSTAL STRUCTURE OF THE PROTEASE INHIBITOR DOMAIN OF ALZHEIMER 'S AMYLOID BETA-PROTEIN PRECURSOR.", BIOCHEMISTRY 29 (43). 1990. 10018-10022. CODEN: BICHAW ISSN: 0006-2960, XP002015891 *
J. PERONA ET AL: "Crystal structures of rat anionic trypsin complexed with the protein inhibitors APPI and BPTI", JOURNAL OF MOLECULAR BIOLOGY, vol. 230, 1993, pages 919 - 933, XP000608106 *
KIDO H ET AL: "PROTEASE-SPECIFICITY OF KUNITZ INHIBITOR DOMAIN OF ALZHEIMER 'S DISEASE AMYLOID PROTEIN PRECURSOR.", BIOCHEM BIOPHYS RES COMMUN 167 (2). 1990. 716-721. CODEN: BBRCA9 ISSN: 0006-291X, XP002015895 *
S. SINHA ET AL: "Conversion of the Alzheimer's beta-Amyloid precursor protein (APP) Kunitz domain into a potent human neutrophil elastase inhibitor", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 266, no. 31, 5 November 1991 (1991-11-05), MD US, pages 21011 - 21013, XP002015894 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9221867B2 (en) 2003-01-06 2015-12-29 Angiochem Inc. Method for transporting a compound across the blood-brain barrier
US9365634B2 (en) 2007-05-29 2016-06-14 Angiochem Inc. Aprotinin-like polypeptides for delivering agents conjugated thereto to tissues
US8921314B2 (en) 2008-10-15 2014-12-30 Angiochem, Inc. Conjugates of GLP-1 agonists and uses thereof
US9173891B2 (en) 2009-04-20 2015-11-03 Angiochem, Inc. Treatment of ovarian cancer using an anticancer agent conjugated to an angiopep-2 analog
US9161988B2 (en) 2009-07-02 2015-10-20 Angiochem Inc. Multimeric peptide conjugates and uses thereof

Also Published As

Publication number Publication date
CA2220497A1 (fr) 1996-11-14
EP0827539A2 (fr) 1998-03-11
KR19990008458A (ko) 1999-01-25
WO1996035788A2 (fr) 1996-11-14
JPH11504938A (ja) 1999-05-11
AU5854096A (en) 1996-11-29

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