[go: up one dir, main page]

WO2000068363A3 - Elastase variants and substrates - Google Patents

Elastase variants and substrates Download PDF

Info

Publication number
WO2000068363A3
WO2000068363A3 PCT/US2000/006692 US0006692W WO0068363A3 WO 2000068363 A3 WO2000068363 A3 WO 2000068363A3 US 0006692 W US0006692 W US 0006692W WO 0068363 A3 WO0068363 A3 WO 0068363A3
Authority
WO
WIPO (PCT)
Prior art keywords
elastase
variants
substrates
histidine
amino acid
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/US2000/006692
Other languages
French (fr)
Other versions
WO2000068363A2 (en
Inventor
Paul J Carter
Acqua William Dall
Maria Rodriques
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.)
Genentech Inc
Original Assignee
Genentech 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 Genentech Inc filed Critical Genentech Inc
Priority to AU49709/00A priority Critical patent/AU4970900A/en
Publication of WO2000068363A2 publication Critical patent/WO2000068363A2/en
Publication of WO2000068363A3 publication Critical patent/WO2000068363A3/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
    • 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
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6448—Elastases, e.g. pancreatic elastase (3.4.21.36); leukocyte elastase (3.4.31.37)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention provides elastase variants having one or more amino acid substitutions at selected positions relative to a precursor elastase. In particular, an active-site histidine residue corresponding to histidine number 43 in human neutrophil elastase can be substituted with an amino acid having a volume smaller than that of histidine. In preferred embodiments, elastase variants of the invention have distinctive substrate specificity for substrates containing histidine residues at the position two amino acid residues to the N-terminal side of the site of cleavage. Preferred substrates for the elastase variants are also provided. The elastase variants and substrates of the invention are useful for a variety of therapeutic and non therapeutic applications.
PCT/US2000/006692 1999-05-05 2000-05-04 Elastase variants and substrates Ceased WO2000068363A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU49709/00A AU4970900A (en) 1999-05-05 2000-05-04 Elastase variants and substrates

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13264099P 1999-05-05 1999-05-05
US60/132,640 1999-05-05

Publications (2)

Publication Number Publication Date
WO2000068363A2 WO2000068363A2 (en) 2000-11-16
WO2000068363A3 true WO2000068363A3 (en) 2001-02-15

Family

ID=22454939

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/006692 Ceased WO2000068363A2 (en) 1999-05-05 2000-05-04 Elastase variants and substrates

Country Status (2)

Country Link
AU (1) AU4970900A (en)
WO (1) WO2000068363A2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8501449B2 (en) * 2007-12-04 2013-08-06 Proteon Therapeutics, Inc. Recombinant elastase proteins and methods of manufacturing and use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0307478A1 (en) * 1987-03-05 1989-03-22 Toray Industries, Inc. Serine protease and serine protease gene
JPH06303984A (en) * 1993-04-19 1994-11-01 Japan Tobacco Inc Recombinant dna, yeast transformed therewith and production of aqualysin i using the same
WO1998024886A1 (en) * 1996-12-04 1998-06-11 Brigham And Women's Hospital, Inc. Mast cell protease that cleaves fibrinogen

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0307478A1 (en) * 1987-03-05 1989-03-22 Toray Industries, Inc. Serine protease and serine protease gene
JPH06303984A (en) * 1993-04-19 1994-11-01 Japan Tobacco Inc Recombinant dna, yeast transformed therewith and production of aqualysin i using the same
WO1998024886A1 (en) * 1996-12-04 1998-06-11 Brigham And Women's Hospital, Inc. Mast cell protease that cleaves fibrinogen

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
DALL'ACQUA WILLIAM ET AL: "Elastase substrate specificity tailored through substrate-assisted catalysis and phage display.", PROTEIN ENGINEERING, vol. 12, no. 11, November 1999 (1999-11-01), pages 981 - 987, XP000960584, ISSN: 0269-2139 *
DAMAK S ET AL: "EXPRESSION OF THE HUMAN NEUTROPHIL ELASTASE GENE IN THE LUNGS OF TRANSGENIC MICE", JOURNAL OF CELLULAR BIOCHEMISTRY. SUPPLEMENT,US,A.R. LISS, NEW YORK, NY, no. SUPPL, 3 April 1992 (1992-04-03), pages 40, XP002910419, ISSN: 0733-1959 *
DATABASE WPI Section Ch Week 199503, Derwent World Patents Index; Class B04, AN 1995-018277, XP002152475 *
EDER JORG ET AL: "Folding of subtilisin BPN': Characterization of a folding intermediate.", BIOCHEMISTRY, vol. 32, no. 1, 1993, pages 18 - 26, XP000960578, ISSN: 0006-2960 *
REHEMTULLA A ET AL: "REGULATION OF PACE PROPEPTIDE-PROCESSING ACTIVITY REQUIREMENT FOR A POST-ENDOPLASMIC RETICULUM COMPARTMENT AND AUTOPROTEOLYTIC ACTIVATION", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES, vol. 89, no. 17, 1992, 1992, pages 8235 - 8239, XP000960579, ISSN: 0027-8424 *
TAKAHASHI H ET AL: "STRUCTURE OF THE HUMAN NEUTROPHIL ELASTASE GENE", JOURNAL OF BIOLOGICAL CHEMISTRY,US,AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, vol. 263, no. 29, 15 October 1988 (1988-10-15), pages 14739 - 14746, XP002911716, ISSN: 0021-9258 *

Also Published As

Publication number Publication date
AU4970900A (en) 2000-11-21
WO2000068363A2 (en) 2000-11-16

Similar Documents

Publication Publication Date Title
WO2000077027A3 (en) Serine protease inhibitors
WO2000076971A3 (en) Serine protease inhibitors
NZ606504A (en) Modified proteases that inhibit complement activation
AU3960400A (en) Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv
UA74372C2 (en) inhibitors of the serine proteaseS, pharmaceutical composition based thereon
CA2000342A1 (en) Novel peptidase inhibitors
HUP0104768A3 (en) 4-amino-3-oxo-azepanes as protease inhibitors and pharmaceutical compositions containing the same
AU2001272995A1 (en) Stable liquid enzyme compositions with enhanced activity
CA2189426A1 (en) Subtilisin bpn' variants having decreased adsorption and increased hydrolysis
AU2002328494A1 (en) Drugs containing chymase inhibitor and ACE inhibitor as the active ingredients
WO2000066104A3 (en) Ace-2 inhibiting compounds and methods of use thereof
CA2388476A1 (en) Bicyclic imidazo-5-yl-amine derivatives
WO2003010291A3 (en) Treatment of immune disorders and b cell disorders
WO2003011222A3 (en) Thrombin inhibitors
AU2001262732A1 (en) Inhibitor for enzyme having two divalent metal ions as active centers
WO2002062304A3 (en) Cosmetic and/or pharmaceutical agents containing an acylated amino acid and a protein condensate
WO2001096366A3 (en) Dipeptide inhibitors for the blood-clotting factor xa
WO2000001826A3 (en) Stabilized variants of streptomyces subtilisin inhibitor
WO2000068363A3 (en) Elastase variants and substrates
ATE307494T1 (en) COMPOSITION COMPRISING PECTINE METHYLSTERASE AND TWO SUBSTRATES
WO2001096540A3 (en) Hepatitis c protease exosite for inhibitor design
WO2002020091A3 (en) Antithrombotic compositions
WO2000061171A3 (en) Uses of mammalian ox2 protein and related reagents
WO2004024765A8 (en) Crystal structure of an angiotensin-converting enzyme (ace) and uses thereof
WO2003097664A3 (en) Non-covalent inhibitors of cysteine proteases with atripeptide backbone

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY CA CH CN CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY CA CH CN CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP