WO2002054064A3 - Method for screening for progesterone receptor isoform-specific ligands - Google Patents

Method for screening for progesterone receptor isoform-specific ligands Download PDF

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Publication number
WO2002054064A3
WO2002054064A3 PCT/EP2001/015200 EP0115200W WO02054064A3 WO 2002054064 A3 WO2002054064 A3 WO 2002054064A3 EP 0115200 W EP0115200 W EP 0115200W WO 02054064 A3 WO02054064 A3 WO 02054064A3
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WO
WIPO (PCT)
Prior art keywords
progesterone receptor
screening
ligands
isoform
present
Prior art date
Application number
PCT/EP2001/015200
Other languages
French (fr)
Other versions
WO2002054064A2 (en
Inventor
Ulrike Fuhrmann
Christa Hegele-Hartung
Michael Klotzbuecher
Original Assignee
Schering Ag
Ulrike Fuhrmann
Christa Hegele-Hartung
Michael Klotzbuecher
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 Schering Ag, Ulrike Fuhrmann, Christa Hegele-Hartung, Michael Klotzbuecher filed Critical Schering Ag
Priority to EP01272662A priority Critical patent/EP1373888A2/en
Priority to US10/250,400 priority patent/US20040121304A1/en
Priority to JP2002554712A priority patent/JP2004516841A/en
Priority to AU2002219218A priority patent/AU2002219218A1/en
Publication of WO2002054064A2 publication Critical patent/WO2002054064A2/en
Priority to NO20032969A priority patent/NO20032969L/en
Publication of WO2002054064A3 publication Critical patent/WO2002054064A3/en

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    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/502—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5082—Supracellular entities, e.g. tissue, organisms
    • G01N33/5088—Supracellular entities, e.g. tissue, organisms of vertebrates
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/743—Steroid hormones
    • 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
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/723—Steroid/thyroid hormone superfamily, e.g. GR, EcR, androgen receptor, oestrogen receptor

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cell Biology (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Toxicology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

The present invention provides a method for screening for progesterone receptor isoform specific ligands as well as a first method for screening for tissue-selective progesterone receptor ligands, both methods comprising selecting progesterone receptor isoform A or progesterone receptor isoform B selective ligands by means of an assay involving cells stably transfected with plasmids expressing the progesterone receptor isoform A or B. Furthermore, the present invention provides a second method for screening for tissue-selective progesterone receptor ligands, comprising in vivo tests in desired target tissues. The present invention further relates to cell lines suitable for this transactivation assay, a respective assay kit and medical uses of the isoform-specific and/or tissue-selective progesterone receptor ligands according to the present invention.
PCT/EP2001/015200 2000-12-28 2001-12-21 Method for screening for progesterone receptor isoform-specific ligands WO2002054064A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
EP01272662A EP1373888A2 (en) 2000-12-28 2001-12-21 Method for screening for progesterone receptor isoform-specific ligands
US10/250,400 US20040121304A1 (en) 2001-12-21 2001-12-21 Method for screening for progesterone receptor isoform-specific ligands and for tissue-selective progesterone receptor ligands
JP2002554712A JP2004516841A (en) 2000-12-28 2001-12-21 Methods for screening for progesterone receptor isoform-specific ligands and tissue-selective progesterone receptor ligands
AU2002219218A AU2002219218A1 (en) 2000-12-28 2001-12-21 Method for screening for progesterone receptor isoform-specific ligands
NO20032969A NO20032969L (en) 2000-12-28 2003-06-27 Method of Screening for Progesterone Receptor Isoform-Specific Ligands and for Tissue Selective Progesterone Receptor Ligands

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US25831200P 2000-12-28 2000-12-28
US60/258,312 2000-12-28
US30587501P 2001-07-18 2001-07-18
US60/305,875 2001-07-18

Publications (2)

Publication Number Publication Date
WO2002054064A2 WO2002054064A2 (en) 2002-07-11
WO2002054064A3 true WO2002054064A3 (en) 2003-10-16

Family

ID=26946565

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2001/015200 WO2002054064A2 (en) 2000-12-28 2001-12-21 Method for screening for progesterone receptor isoform-specific ligands

Country Status (8)

Country Link
EP (1) EP1373888A2 (en)
JP (1) JP2004516841A (en)
AR (1) AR032050A1 (en)
AU (1) AU2002219218A1 (en)
NO (1) NO20032969L (en)
PE (1) PE20020784A1 (en)
UY (1) UY27107A1 (en)
WO (1) WO2002054064A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003075915A1 (en) * 2002-03-11 2003-09-18 Schering Ag 5-}2-hydroxy-3-`1-(3-trifluoromethylphenyl)-cyclopropyl!-propionylamino}- phtalide and related compounds with progesterone receptor modulating activity for use in fertility control and hormone replacement therapy
DE102007049630A1 (en) 2007-10-11 2009-10-29 Bayer Schering Pharma Aktiengesellschaft New amide compounds used for therapy and/or prophylaxis of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy
DE102007023614A1 (en) 2007-05-21 2008-11-27 Bayer Schering Pharma Aktiengesellschaft New amide compounds used for treatment of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy, has general formula
DE102007032800A1 (en) 2007-07-10 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Nonsteroidal progesterone receptor modulators
DE102007058747A1 (en) 2007-12-05 2009-06-10 Bayer Schering Pharma Aktiengesellschaft Nonsteroidal progesterone receptor modulators
EP2070909A1 (en) 2007-12-15 2009-06-17 Bayer Schering Pharma AG Non-steroidal progesterone receptor modulators
CN113801889B (en) * 2021-09-18 2023-04-07 中国农业科学院农业质量标准与检测技术研究所 Cell screening model, construction method and application thereof, saccharomycete, preparation method and application thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0253503A2 (en) * 1986-07-18 1988-01-20 Imperial Chemical Industries Plc Substituted anilides having antiandrogenic properties
WO1995011973A1 (en) * 1993-10-28 1995-05-04 Ligand Pharmaceuticals Incorporated Methods for screening for regulators of intracellular receptor transcription using progesterone receptor a subtype
DE4337416A1 (en) * 1993-10-27 1995-05-04 Schering Ag 10,11beta-C¶2¶-bridged steroids
WO1995027725A1 (en) * 1994-04-12 1995-10-19 Schering Aktiengesellschaft 11β,19-BRIDGED 13α-ALKYL STEROIDS
US5523298A (en) * 1992-10-13 1996-06-04 Schering Aktiengesellschaft Progestationally active 19,11-bridged 4-estrenes
DE19723722A1 (en) * 1997-05-30 1998-12-10 Schering Ag Nonsteroidal progestogens

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0253503A2 (en) * 1986-07-18 1988-01-20 Imperial Chemical Industries Plc Substituted anilides having antiandrogenic properties
US5523298A (en) * 1992-10-13 1996-06-04 Schering Aktiengesellschaft Progestationally active 19,11-bridged 4-estrenes
DE4337416A1 (en) * 1993-10-27 1995-05-04 Schering Ag 10,11beta-C¶2¶-bridged steroids
WO1995011973A1 (en) * 1993-10-28 1995-05-04 Ligand Pharmaceuticals Incorporated Methods for screening for regulators of intracellular receptor transcription using progesterone receptor a subtype
WO1995027725A1 (en) * 1994-04-12 1995-10-19 Schering Aktiengesellschaft 11β,19-BRIDGED 13α-ALKYL STEROIDS
DE19723722A1 (en) * 1997-05-30 1998-12-10 Schering Ag Nonsteroidal progestogens

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DIJKEMA R ET AL: "Human progesterone receptor A and B isoforms in CHO cells. I. Stable transfection of receptor and receptor-responsive reporter genes: Transcription modulation by (anti)progestagens.", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, vol. 64, no. 3-4, February 1998 (1998-02-01), pages 147 - 156, XP002226482, ISSN: 0960-0760 *
LEE SANG-HYEON ET AL: "Up-regulation of D1A dopamine receptor gene transcription by estrogen.", MOLECULAR AND CELLULAR ENDOCRINOLOGY, vol. 156, no. 1-2, 25 October 1999 (1999-10-25), pages 151 - 157, XP002226939, ISSN: 0303-7207 *
SCHOONEN W G E J ET AL: "Human progesterone receptor A and B isoforms in CHO cells. II. Comparison of binding, transactivation and ED50 values of several synthetic (anti)progestagens in vitro in CHO and MCF-7 cells and in vivo in rabbits and rats.", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, vol. 64, no. 3-4, February 1998 (1998-02-01), pages 157 - 170, XP002226483, ISSN: 0960-0760 *

Also Published As

Publication number Publication date
EP1373888A2 (en) 2004-01-02
NO20032969D0 (en) 2003-06-27
AU2002219218A1 (en) 2002-07-16
AR032050A1 (en) 2003-10-22
JP2004516841A (en) 2004-06-10
PE20020784A1 (en) 2002-10-03
UY27107A1 (en) 2002-03-22
NO20032969L (en) 2003-08-28
WO2002054064A2 (en) 2002-07-11

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