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WO2008101160A3 - Htra1-pdz and htra3-pdz modulators - Google Patents

Htra1-pdz and htra3-pdz modulators Download PDF

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Publication number
WO2008101160A3
WO2008101160A3 PCT/US2008/054081 US2008054081W WO2008101160A3 WO 2008101160 A3 WO2008101160 A3 WO 2008101160A3 US 2008054081 W US2008054081 W US 2008054081W WO 2008101160 A3 WO2008101160 A3 WO 2008101160A3
Authority
WO
WIPO (PCT)
Prior art keywords
pdz
htra3
htra1
modulators
pdz domain
Prior art date
Application number
PCT/US2008/054081
Other languages
French (fr)
Other versions
WO2008101160A2 (en
Inventor
Brent A Appleton
Steven T Runyon
Sachdev S Sidhu
Nicholas J Skelton
Christian Wiesmann
Yingnan Zhang
Original Assignee
Genentech Inc
Brent A Appleton
Steven T Runyon
Sachdev S Sidhu
Nicholas J Skelton
Christian Wiesmann
Yingnan Zhang
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, Brent A Appleton, Steven T Runyon, Sachdev S Sidhu, Nicholas J Skelton, Christian Wiesmann, Yingnan Zhang filed Critical Genentech Inc
Priority to EP08729968A priority Critical patent/EP2111413A2/en
Publication of WO2008101160A2 publication Critical patent/WO2008101160A2/en
Publication of WO2008101160A3 publication Critical patent/WO2008101160A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • 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
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Wood Science & Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Microbiology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biotechnology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Gyroscopes (AREA)
  • Compression, Expansion, Code Conversion, And Decoders (AREA)
  • Digital Transmission Methods That Use Modulated Carrier Waves (AREA)

Abstract

The invention provides optimized HtrA1 PDZ domain and HtrA3 PDZ domain ligands. The invention further provides modulators of HtrA1 PDZ domain-ligand interaction and HtrA3 PDZ domain-ligand interaction, and methods of identifying and using these modulators.
PCT/US2008/054081 2007-02-16 2008-02-15 Htra1-pdz and htra3-pdz modulators WO2008101160A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP08729968A EP2111413A2 (en) 2007-02-16 2008-02-15 Htra1-pdz and htra3-pdz modulators

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US89042807P 2007-02-16 2007-02-16
US60/890,428 2007-02-16

Publications (2)

Publication Number Publication Date
WO2008101160A2 WO2008101160A2 (en) 2008-08-21
WO2008101160A3 true WO2008101160A3 (en) 2009-02-19

Family

ID=39590928

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/054081 WO2008101160A2 (en) 2007-02-16 2008-02-15 Htra1-pdz and htra3-pdz modulators

Country Status (6)

Country Link
EP (1) EP2111413A2 (en)
AR (1) AR065370A1 (en)
CL (1) CL2008000493A1 (en)
PE (1) PE20081795A1 (en)
TW (1) TW200846358A (en)
WO (1) WO2008101160A2 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8168181B2 (en) 2006-02-13 2012-05-01 Alethia Biotherapeutics, Inc. Methods of impairing osteoclast differentiation using antibodies that bind siglec-15
EP1994155B2 (en) 2006-02-13 2022-05-04 Daiichi Sankyo Company, Limited Polynucleotide and polypeptide sequences involved in the process of bone remodeling
EA201490778A1 (en) 2011-10-14 2014-09-30 Дженентек, Инк. ANTIBODIES AGAINST HtrA1 AND METHODS OF APPLICATION
IN2014KN02933A (en) 2012-07-19 2015-05-08 Alethia Biotherapeutics Inc
KR102440160B1 (en) 2015-10-30 2022-09-02 제넨테크, 인크. Anti-HtrA1 antibodies and methods of use thereof
JP2019513698A (en) 2016-03-04 2019-05-30 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Novel trifluoromethylpropanamide derivatives as HTRA1 inhibitors
EP3423467B1 (en) 2016-03-04 2021-04-28 F. Hoffmann-La Roche AG New difluoroketamide derivatives as htra1 inhibitors
WO2018015240A1 (en) 2016-07-18 2018-01-25 F. Hoffmann-La Roche Ag New difluoroketamide derivatives as htra1 inhibitors
CN109563084A (en) 2016-08-23 2019-04-02 豪夫迈·罗氏有限公司 Novel trifluoromethyl propanamide derivative as HTRA1 inhibitor
JP2019526563A (en) 2016-08-23 2019-09-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Novel difluoroketamide derivatives as HTRA1 inhibitors
WO2018206816A1 (en) * 2017-05-12 2018-11-15 Universität Duisburg-Essen Tailored cyclodepsipeptides as potent non-covalent serine protease inhibitors
WO2020083916A1 (en) * 2018-10-22 2020-04-30 University Of Copenhagen Virally expressed inhibitors of pdz domains, such as pick1 and uses thereof
KR20220150313A (en) * 2020-03-06 2022-11-10 유니버시티 오브 코펜하겐 Lipid conjugated peptide inhibitor of PICK1

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040214272A1 (en) * 1999-05-06 2004-10-28 La Rosa Thomas J Nucleic acid molecules and other molecules associated with plants

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040214272A1 (en) * 1999-05-06 2004-10-28 La Rosa Thomas J Nucleic acid molecules and other molecules associated with plants

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
DATABASE UniProt 2004, XP002501527, Database accession no. Q6UK25 *
FACCIO L, ET AL.: "TISSUE-SPECIFIC SPLICING OF OMI STRESS-REGULATED ENDOPROTEASE LEADS TO AN INACTIVE PROTEASE WITH A MODIFIED PDZ MOTIF", GENOMICS, vol. 68, 2000, pages 343 - 347, XP004437838 *
GUPTA S, ET AL.: "THE C-TERMINAL TAIL OF PRESENILIN REGULATES OMI/HTRA2 PROTEASE ACTIVITY", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 279, no. 44, 2004, pages 45844 - 45854, XP002488179 *
JUNQUEIRA D, ET AL.: "RANDOM MUTAGENESIS OF PDZOMI DOMAIN AND SELECTION OF MUTANTS THAT SPECIFICALLY BIND THE MYC PROTO-ONCOGENE AND INDUCE APOPTOSIS", ONCOGENE, vol. 22, 2003, pages 2772 - 2781, XP002501627 *
LI W, ET AL.: "STRUCTURAL INSIGHTS INTO THE PRO-APOPTOTIC FUNCTION OF MITOCHONDRIAL SERINE PROTEASE HTRA2/OMI", NATURE STRUCTURAL BIOLOGY, vol. 9, no. 6, 2002, pages 436 - 441, XP002501628 *
MARTINS L MIGUEL ET AL: "Binding specificity and regulation of the serine protease and PDZ domains of HtrA2/Omi", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOCHEMICAL BIOLOGISTS, BIRMINGHAM,; US, vol. 278, no. 49, 5 December 2003 (2003-12-05), pages 49417 - 49427, XP002366468, ISSN: 0021-9258 *
MURWANTOKO ET AL: "Binding of proteins to the PDZ domain regulates proteolytic activity of HtrA1 serine protease", BIOCHEMICAL JOURNAL, THE BIOCHEMICAL SOCIETY, LONDON, vol. 381, no. 3, 1 August 2002 (2002-08-01), pages 895 - 904, XP009103026, ISSN: 0264-6021 *
NIE G-Y ET AL: "IDENTIFICATION AND CLONING OF TWO ISOFORMS OF HUMAN HIGH-TEMPERATURE REQUIREMENT FACTOR A3 (HTRA3), CHARACTERIZATION OF ITS GENOMIC STRUCTURE AND COMPARISON OF ITS TISSUE DISTRIBUTION WITH HTRA1 AND HTRA2", BIOCHEMICAL JOURNAL, THE BIOCHEMICAL SOCIETY, LONDON, vol. 371, no. PRT 1, 1 April 2003 (2003-04-01), pages 39 - 48, XP002976438, ISSN: 0264-6021 *
RUNYON STEVEN T ET AL: "Structural and functional analysis of the PDZ domains of human HtrA1 and HtrA3", PROTEIN SCIENCE, CAMBRIDGE UNIVERSITY PRESS, CAMBRIDGE, GB, vol. 16, no. 11, 1 November 2007 (2007-11-01), pages 2454 - 2471, XP009103036, ISSN: 0961-8368 *
ZHANG Y, ET AL.: "CONVERGENT AND DIVERGENT LIGAND SPECIFICITY AMONG PDZ DOMAINS OF THE LAP AND ZONULA OCCLUDENS (ZO) FAMILIES", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 281, no. 31, 2006, pages 22299 - 22311, XP002488178 *

Also Published As

Publication number Publication date
PE20081795A1 (en) 2009-01-08
WO2008101160A2 (en) 2008-08-21
AR065370A1 (en) 2009-06-03
EP2111413A2 (en) 2009-10-28
TW200846358A (en) 2008-12-01
CL2008000493A1 (en) 2008-06-27

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