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WO2000071682A3 - Crystal structure data of cysteinprotease gingipain r - Google Patents

Crystal structure data of cysteinprotease gingipain r Download PDF

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Publication number
WO2000071682A3
WO2000071682A3 PCT/EP2000/004561 EP0004561W WO0071682A3 WO 2000071682 A3 WO2000071682 A3 WO 2000071682A3 EP 0004561 W EP0004561 W EP 0004561W WO 0071682 A3 WO0071682 A3 WO 0071682A3
Authority
WO
WIPO (PCT)
Prior art keywords
crystal structure
gingipain
cysteinprotease
structure data
phe
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/EP2000/004561
Other languages
French (fr)
Other versions
WO2000071682A2 (en
Inventor
Andreas Eichinger
Hans-Georg Beisel
Wolfram Bode
Robert Huber
Luis Moroder
James Travis
Jan Potempa
Stefan Alefelder
Eva Pleiner
Joerg Stuerzebecher
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.)
Max Planck Gesellschaft zur Foerderung der Wissenschaften
University of Georgia
University of Georgia Research Foundation Inc UGARF
Original Assignee
Max Planck Gesellschaft zur Foerderung der Wissenschaften
University of Georgia
University of Georgia Research Foundation Inc UGARF
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 Max Planck Gesellschaft zur Foerderung der Wissenschaften, University of Georgia, University of Georgia Research Foundation Inc UGARF filed Critical Max Planck Gesellschaft zur Foerderung der Wissenschaften
Priority to AU58088/00A priority Critical patent/AU5808800A/en
Publication of WO2000071682A2 publication Critical patent/WO2000071682A2/en
Publication of WO2000071682A3 publication Critical patent/WO2000071682A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING 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
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • 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)
    • C12N9/52—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from bacteria or Archaea
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/81—Protease inhibitors
    • G01N2333/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • G01N2333/8139—Cysteine protease (E.C. 3.4.22) inhibitors, e.g. cystatin
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G01N2333/948—Hydrolases (3) acting on peptide bonds (3.4)
    • G01N2333/95—Proteinases, i.e. endopeptidases (3.4.21-3.4.99)
    • G01N2333/964—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue
    • G01N2333/96425—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals
    • G01N2333/96427—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general
    • G01N2333/9643—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general with EC number
    • G01N2333/96466—Cysteine endopeptidases (3.4.22)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value

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  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Health & Medical Sciences (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Biophysics (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Peptides Or Proteins (AREA)
  • Steroid Compounds (AREA)

Abstract

The objects of the present invention are a crystal structure of gingipain R as shown in (Fig. 1) and a crystal structure of a gingipain R in complex with H-D-Phe-Phe-Arg-chloromethylketone as shown in (Fig. 4). A further object is the use of such crystal structure to obtain crystal structure data for the design and/or identification of inhibitors of gingipain R, which again form part of the present invention, as well as pharmaceutical compositions containing such inhibitors.
PCT/EP2000/004561 1999-05-20 2000-05-19 Crystal structure data of cysteinprotease gingipain r Ceased WO2000071682A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU58088/00A AU5808800A (en) 1999-05-20 2000-05-19 Crystal structure data of cysteinprotease gingipain r

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99109944.1 1999-05-20
EP99109944 1999-05-20

Publications (2)

Publication Number Publication Date
WO2000071682A2 WO2000071682A2 (en) 2000-11-30
WO2000071682A3 true WO2000071682A3 (en) 2001-10-18

Family

ID=8238215

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/004561 Ceased WO2000071682A2 (en) 1999-05-20 2000-05-19 Crystal structure data of cysteinprotease gingipain r

Country Status (2)

Country Link
AU (1) AU5808800A (en)
WO (1) WO2000071682A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2011214908A1 (en) * 2010-02-12 2012-09-20 Sydney West Area Health Services (Swahs) Protein domains and uses therefor
US11981789B2 (en) 2017-09-15 2024-05-14 Unm Rainforest Innovations Method and system to mimic a random structural pattern

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4973554A (en) * 1987-05-29 1990-11-27 National Research Council Of Canada Affinity process for trypsin purification and stabilization
WO1995007286A1 (en) * 1993-09-10 1995-03-16 University Of Georgia Research Foundation, Inc. Porphyromonas gingivalis arginine-specific proteinase coding sequences
WO1998049190A2 (en) * 1997-04-25 1998-11-05 Cortech, Inc. Substituted oxadiazole cysteine protease inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4973554A (en) * 1987-05-29 1990-11-27 National Research Council Of Canada Affinity process for trypsin purification and stabilization
WO1995007286A1 (en) * 1993-09-10 1995-03-16 University Of Georgia Research Foundation, Inc. Porphyromonas gingivalis arginine-specific proteinase coding sequences
WO1998049190A2 (en) * 1997-04-25 1998-11-05 Cortech, Inc. Substituted oxadiazole cysteine protease inhibitors

Non-Patent Citations (18)

* Cited by examiner, † Cited by third party
Title
BANBULA A ET AL: "Crystallization and preliminary X-ray diffraction analysis of gingipain R2 from Porphyromonas gingivalis in complex with H-D-Phe-Phe-Arg-chloromethylketone.", PROTEIN SCIENCE, (1998 MAY) 7 (5) 1259-61., XP002120682 *
BIOORGANIC AND MEDICINAL CHEMISTRY, (1998 DEC) 6 (12) 2477-94. *
DATABASE BIOSIS [online] BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; 1988, STUEBER W ET AL: "SYNTHESIS OF A TRIPEPTIDE WITH A CARBOXYL-TERMINAL NITRILE MOIETY AND THE INHIBITION OF PROTEINASES", XP002164556, Database accession no. PREV198885086104 *
DATABASE BIOSIS [online] BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; 1995, LALMANACH GILLES ET AL: "Conserved cystatin segments as models for designing specific substrates and inhibitors of cysteine proteinases.", XP002164557, Database accession no. PREV199698631164 *
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; SCHEIDT K A ET AL: "Structure - based design, synthesis and evaluation of conformationally constrained cysteine protease inhibitors.", XP002120877, retrieved from STN Database accession no. 1999122713 *
DATABASE XFIRE 11 July 1987 (1987-07-11), XP002164559 *
DATABASE XFIRE 11 July 1989 (1989-07-11), XP002164558 *
EICHINGER ANDREAS ET AL: "Crystal structure of gingipain R: An Arg-specific bacterial cysteine proteinase with a caspase-like fold.", EMBO (EUROPEAN MOLECULAR BIOLOGY ORGANIZATION) JOURNAL, vol. 18, no. 20, 15 October 1999 (1999-10-15), pages 5453 - 5462, XP002152750, ISSN: 0261-4189 *
INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, vol. 31, no. 1, 1988, pages 63 - 70, ISSN: 0367-8377 *
JOURNAL OF MEDICAL CHEMISTRY, vol. 12, 1969, pages 408 *
JOURNAL OF PROTEIN CHEMISTRY, vol. 14, no. 8, 1995, pages 645 - 653, ISSN: 0277-8033 *
NISHIKATA M ET AL: "SALIVARY HISTATIN AS AN INHIBITOR OF A PROTEASE PRODUCED BY THE ORAL BACTERIUM BACTEROIDES-GINGIVALIS", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, vol. 174, no. 2, 1991, pages 625 - 630, XP002164570, ISSN: 0006-291X *
PHARMAZIE, vol. 29, 1974, pages 383 *
POTEMPA J ET AL: "Titration and mapping of the active site of cysteine proteinases from Porphyromonas gingivalis ( gingipains ) using peptidyl chloromethanes.", BIOLOGICAL CHEMISTRY, (1997 MAR-APR) 378 (3-4) 223-30., XP002120683 *
RECANATINI M ET AL: "Quantitative structure-activity relationships and molecular graphics in ligand receptor interactions: amidine inhibition of trypsin", MOLECULAR PHARMACOLOGY, vol. 29, no. 4, 1986, pages 436-446, XP000990946 *
SHINOHARA CHIKARA ET AL: "Arg-gingipain inhibition and anti-bacterial activity selective for Porphyromonas gingivalis by malabaricone C.", BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY, vol. 63, no. 8, August 1999 (1999-08-01), pages 1475 - 1477, XP002164555, ISSN: 0916-8451 *
THOMPSON S K ET AL: "Structure - based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.", JOURNAL OF MEDICINAL CHEMISTRY, (1998 OCT 8) 41 (21) 3923-7., XP002120685 *
WALSMANN P ET AL: "Synthetische Inhibitoren der Serinproteinasen", PHARMAZIE, vol. 34, no. 3, 1979, pages 194 - 195, XP000990908 *

Also Published As

Publication number Publication date
AU5808800A (en) 2000-12-12
WO2000071682A2 (en) 2000-11-30

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