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WO2005047538A3 - Ligands du represseur mycobacterien ethr, procedes de selection et applications - Google Patents

Ligands du represseur mycobacterien ethr, procedes de selection et applications Download PDF

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Publication number
WO2005047538A3
WO2005047538A3 PCT/FR2004/002721 FR2004002721W WO2005047538A3 WO 2005047538 A3 WO2005047538 A3 WO 2005047538A3 FR 2004002721 W FR2004002721 W FR 2004002721W WO 2005047538 A3 WO2005047538 A3 WO 2005047538A3
Authority
WO
WIPO (PCT)
Prior art keywords
mycobacterial
repressor
applications
ligands
ethr
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/FR2004/002721
Other languages
English (en)
Other versions
WO2005047538A2 (fr
Inventor
Frederic Frenois
Jean Engohang-Ndong
Vincent Villeret
Camille Locht
Alain Baulard
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.)
Centre National de la Recherche Scientifique CNRS
Institut Pasteur de Lille
Institut National de la Sante et de la Recherche Medicale INSERM
Institut Pasteur
Original Assignee
Centre National de la Recherche Scientifique CNRS
Institut Pasteur de Lille
Institut National de la Sante et de la Recherche Medicale INSERM
Institut Pasteur
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
Priority claimed from FR0312801A external-priority patent/FR2861742B1/fr
Application filed by Centre National de la Recherche Scientifique CNRS, Institut Pasteur de Lille, Institut National de la Sante et de la Recherche Medicale INSERM, Institut Pasteur filed Critical Centre National de la Recherche Scientifique CNRS
Publication of WO2005047538A2 publication Critical patent/WO2005047538A2/fr
Publication of WO2005047538A3 publication Critical patent/WO2005047538A3/fr
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
    • C12N15/63—Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
    • C12N15/635—Externally inducible repressor mediated regulation of gene expression, e.g. tetR inducible by tetracyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
    • A61K31/121—Ketones acyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Zoology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Plant Pathology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Physics & Mathematics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

La présente invention concerne des procédés de sélection de composés capables de se lier au répresseur mycobactérien EthR, cette liaison l’empêchant de réprimer l’expression du gène mycobactérien ethA codant EthA, le bio-activateur de l’éthionamide. L’invention a également pour objets les composés inhibiteurs du répresseur EthR, ainsi que leurs applications thérapeutiques.
PCT/FR2004/002721 2003-10-31 2004-10-22 Ligands du represseur mycobacterien ethr, procedes de selection et applications Ceased WO2005047538A2 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
FR0312801A FR2861742B1 (fr) 2003-10-31 2003-10-31 LIGANDS DU REPRESSEUR MYCOBATERIEN EthR, PROCEDES DE SELECTION ET APPLICATIONS
FR0312801 2003-10-31
FR0404636A FR2861745A1 (fr) 2003-10-31 2004-04-30 Ligands du repressseur mycobacterien ethr, procedes de selection et applications
FR0404636 2004-04-30

Publications (2)

Publication Number Publication Date
WO2005047538A2 WO2005047538A2 (fr) 2005-05-26
WO2005047538A3 true WO2005047538A3 (fr) 2005-07-07

Family

ID=34436803

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/FR2004/002721 Ceased WO2005047538A2 (fr) 2003-10-31 2004-10-22 Ligands du represseur mycobacterien ethr, procedes de selection et applications

Country Status (2)

Country Link
FR (1) FR2861745A1 (fr)
WO (1) WO2005047538A2 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2234643B1 (fr) * 2007-12-21 2013-01-09 ETH Zurich Composition pour le traitement de la tuberculose

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5378603A (en) * 1987-03-30 1995-01-03 Board Of Regents, The University Of Texas System Method and composition for identifying substances which activate transcription of the LDL receptor gene
DE19502584A1 (de) * 1994-01-28 1995-08-03 Medigene Gmbh Verfahren zur Bestimmung der Aktivität eines regulatorischen Faktors sowie Verwendung dieses Verfahrens
FR2750705A1 (fr) * 1996-07-04 1998-01-09 Centre Nat Rech Scient Systeme de detection des interactions proteine-proteine
WO2002064632A2 (fr) * 2001-02-01 2002-08-22 Smithkline Beecham Corporation Polypeptide cristallise du domaine de liaison au ligand de ppar$g(a) et procedes de criblage utilisant ce polypeptide

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR915M (fr) * 1960-03-14 1961-11-06
CA2442343A1 (fr) * 2001-02-07 2002-08-15 Serguei S. Likhodi Methode de traitement de troubles neurologiques
WO2002072809A1 (fr) * 2001-03-12 2002-09-19 Alydar Pharmaceuticals, Inc. Criblage de composes pheromonaux d'invertebres non-steroidiens et non-peptidiques ayant une activite modulant une proteine kinase activee par un mitogene

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5378603A (en) * 1987-03-30 1995-01-03 Board Of Regents, The University Of Texas System Method and composition for identifying substances which activate transcription of the LDL receptor gene
DE19502584A1 (de) * 1994-01-28 1995-08-03 Medigene Gmbh Verfahren zur Bestimmung der Aktivität eines regulatorischen Faktors sowie Verwendung dieses Verfahrens
FR2750705A1 (fr) * 1996-07-04 1998-01-09 Centre Nat Rech Scient Systeme de detection des interactions proteine-proteine
WO2002064632A2 (fr) * 2001-02-01 2002-08-22 Smithkline Beecham Corporation Polypeptide cristallise du domaine de liaison au ligand de ppar$g(a) et procedes de criblage utilisant ce polypeptide

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BAULARD A R ET AL: "Activation of the pro-drug ethionamide is regulated in mycobacteria.", THE JOURNAL OF BIOLOGICAL CHEMISTRY. UNITED STATES 8 SEP 2000, vol. 275, no. 36, 8 September 2000 (2000-09-08), pages 28326 - 28331, XP002283429, ISSN: 0021-9258 *
BAULARD A R ET AL: "In vivo monitoring of ETH activation in mycobacteria by 1H HRMAS NMR", ABSTRACTS OF THE GENERAL MEETING OF THE AMERICAN SOCIETY FOR, vol. 102, 2002, 102nd General Meeting of the American Society for Microbiology;Salt Lake City, UT, USA; May 19-23, 2002, 2002, pages 11, XP009031862, ISSN: 1060-2011 *
DEBARBER A E ET AL: "Ethionamide activation and sensitivity in multidrug-resistant Mycobacterium tuberculosis.", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA. UNITED STATES 15 AUG 2000, vol. 97, no. 17, 15 August 2000 (2000-08-15), pages 9677 - 9682, XP002283430, ISSN: 0027-8424 *
ENGOHANG-NDONG JEAN ET AL: "EthR, a repressor of the TetR/CamR family implicated in ethionamide resistance in mycobacteria, octamerizes cooperatively on its operator.", MOLECULAR MICROBIOLOGY. ENGLAND JAN 2004, vol. 51, no. 1, January 2004 (2004-01-01), pages 175 - 188, XP002283433, ISSN: 0950-382X *
FRAAIJE M W ET AL: "The prodrug activator EtaA from Mycobacterium tuberculosis is a Baeyer-Villiger monooxygenase", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, US, vol. 279, no. 5, 30 January 2004 (2004-01-30), pages 3354 - 3360, XP002303963, ISSN: 0021-9258 *
VANNELLI TOMMASO A ET AL: "The antituberculosis drug ethionamide is activated by a flavoprotein monooxygenase.", THE JOURNAL OF BIOLOGICAL CHEMISTRY. UNITED STATES 12 APR 2002, vol. 277, no. 15, 12 April 2002 (2002-04-12), pages 12824 - 12829, XP002283431, ISSN: 0021-9258 *

Also Published As

Publication number Publication date
WO2005047538A2 (fr) 2005-05-26
FR2861745A1 (fr) 2005-05-06

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