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WO1996035788A3 - Kunitz type protease inhibitors - Google Patents

Kunitz type protease inhibitors 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
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/US1996/006384
Other languages
French (fr)
Other versions
WO1996035788A2 (en
Inventor
Tyler R White
Deborah Damm
David D Lesikar
Kethleen Mcfadden
Brett L Garrick
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.)
Scios LLC
Original Assignee
Scios LLC
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 LLC filed Critical Scios LLC
Priority to JP8534170A priority Critical patent/JPH11504938A/en
Priority to AU58540/96A priority patent/AU5854096A/en
Priority to EP96920140A priority patent/EP0827539A2/en
Publication of WO1996035788A2 publication Critical patent/WO1996035788A2/en
Publication of WO1996035788A3 publication Critical patent/WO1996035788A3/en
Anticipated expiration legal-status Critical
Ceased 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
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • 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
    • C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
    • C07K14/8114—Kunitz type inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • A61K38/57—Protease inhibitors from animals; from humans
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/01—Fusion polypeptide containing a localisation/targetting motif
    • C07K2319/02—Fusion polypeptide containing a localisation/targetting motif containing a signal sequence

Landscapes

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

Abstract

Analogues of the Kunitz Protease Inhibitor (KPI) domain of amyloid precursor protein bind to and inhibit activity of serine proteases, including kallikrein, plasmin and coagulation factors such as factors VIIa, IXa, Xa, XIa and XIIa. Pharmaceutical compositions containing the KPI analogues, along with methods for using such compositions, are useful for ameliorating and treating clinical conditions associated with increased serine protease activity, such as blood loss related to cardiopulmonary bypass surgery. Nucleic acid sequences encoding these analogues and systems for expression of the peptides of the invention are provided.
PCT/US1996/006384 1995-05-08 1996-05-08 Kunitz type protease inhibitors Ceased WO1996035788A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP8534170A JPH11504938A (en) 1995-05-08 1996-05-08 Kunitz-type protease inhibitor
AU58540/96A AU5854096A (en) 1995-05-08 1996-05-08 Kunitz type protease inhibitors
EP96920140A EP0827539A2 (en) 1995-05-08 1996-05-08 Kunitz type protease inhibitors

Applications Claiming Priority (4)

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

Publications (2)

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

Family

ID=27031013

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1996/006384 Ceased WO1996035788A2 (en) 1995-05-08 1996-05-08 Kunitz type protease inhibitors

Country Status (6)

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

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
KR100356956B1 (en) 1996-03-11 2003-03-15 베이어 코오포레이숀 Human bikunin
WO1999061615A1 (en) * 1998-05-28 1999-12-02 Zymogenetics, Inc. Kunitz domain polypeptide and materials and methods for making it
CA2330191A1 (en) * 1998-06-03 1999-12-09 Scios, Inc. Protease inhibitor peptides
ES2528254T3 (en) 2002-06-07 2015-02-05 Dyax Corp. Modified Kunitz domain polypeptides and their use to reduce ischemia or the onset of a systemic inflammatory response associated with a surgical procedure
US7153829B2 (en) 2002-06-07 2006-12-26 Dyax Corp. Kallikrein-inhibitor therapies
US7235530B2 (en) 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
EP2360258B1 (en) 2005-02-18 2014-10-08 Angiochem Inc. Aprotinin polypeptides for transporting a compound across the blood-brain barrier
DK2233156T3 (en) 2005-07-15 2013-08-05 Angiochem Inc Use of aprotinin polypeptides as carriers in pharmaceutical conjugates
US20110027337A1 (en) * 2007-12-21 2011-02-03 Ifxa A/S Protease inhibitor
JP5759379B2 (en) 2008-12-05 2015-08-05 アンジオケム インコーポレーテッド Neurotensin or neurotensin analog and use thereof
EP2385843A4 (en) 2009-01-06 2013-02-27 Dyax Corp Treatment of mucositis with kallikrein inhibitors
HRP20220107T1 (en) 2010-01-06 2022-04-15 Takeda Pharmaceutical Company Limited Plasma kallikrein binding proteins
CN105713092B (en) 2011-01-06 2019-09-10 戴埃克斯有限公司 Blood plasma prekallikrein binding protein
EP2885318A4 (en) 2012-08-14 2016-03-30 Angiochem Inc PEPTIDE-DENDRIMER CONJUGATES AND USES THEREOF
JP6823055B2 (en) 2015-06-15 2021-01-27 アンジオケム インコーポレーテッド How to treat soft meningeal carcinomatosis
US20180362616A1 (en) * 2015-12-10 2018-12-20 The National Institute for Biotechnology in the Negev Ltd. VARIANTS OF AMYLOID beta-PROTEIN PRECURSOR INHIBITOR DOMAIN
KR20250139401A (en) 2015-12-11 2025-09-23 다케다 파머수티컬 컴패니 리미티드 Plasma kallikrein inhibitors and uses thereof for treating hereditary angioedema attack
CN110051830A (en) * 2019-03-14 2019-07-26 苏州新凝生物医药科技有限公司 A kind of protease nexin II KPI protein mutant application

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0393431A1 (en) * 1989-04-18 1990-10-24 Bayer Ag Homologues of Alzheimer protease inhibitor prepared genetechnologically, host-strains and expression vectors for their preparation and use as a medicament
WO1993014120A1 (en) * 1992-01-07 1993-07-22 Novo Nordisk A/S A human kunitz-type protease inhibitor variant
WO1993014119A1 (en) * 1992-01-07 1993-07-22 Novo Nordisk A/S Human kunitz-type protease inhibitor variants
WO1995023860A2 (en) * 1994-03-04 1995-09-08 Genentech, Inc. KUNITZ DOMAIN INHIBITOR PROTEINS DERIVED FROM ALZHEIMER'S AMYLOID β-PROTEIN PRECURSOR INHIBITOR

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996039619A1 (en) * 1995-06-06 1996-12-12 Kla Instruments Corporation Optical inspection of a specimen using multi-channel responses from the specimen

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0393431A1 (en) * 1989-04-18 1990-10-24 Bayer Ag Homologues of Alzheimer protease inhibitor prepared genetechnologically, host-strains and expression vectors for their preparation and use as a medicament
WO1993014120A1 (en) * 1992-01-07 1993-07-22 Novo Nordisk A/S A human kunitz-type protease inhibitor variant
WO1993014119A1 (en) * 1992-01-07 1993-07-22 Novo Nordisk A/S Human kunitz-type protease inhibitor variants
WO1995023860A2 (en) * 1994-03-04 1995-09-08 Genentech, Inc. KUNITZ DOMAIN INHIBITOR PROTEINS DERIVED FROM ALZHEIMER'S AMYLOID β-PROTEIN PRECURSOR INHIBITOR

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
KR19990008458A (en) 1999-01-25
WO1996035788A2 (en) 1996-11-14
JPH11504938A (en) 1999-05-11
CA2220497A1 (en) 1996-11-14
AU5854096A (en) 1996-11-29
EP0827539A2 (en) 1998-03-11

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