CA2324060A1 - Methodes et composes de modulation d'activite de recepteurs nucleaires - Google Patents

Methodes et composes de modulation d'activite de recepteurs nucleaires Download PDF

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Publication number
CA2324060A1
CA2324060A1 CA002324060A CA2324060A CA2324060A1 CA 2324060 A1 CA2324060 A1 CA 2324060A1 CA 002324060 A CA002324060 A CA 002324060A CA 2324060 A CA2324060 A CA 2324060A CA 2324060 A1 CA2324060 A1 CA 2324060A1
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CA
Canada
Prior art keywords
atom
receptors
leu
receptor
nuclear receptor
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.)
Abandoned
Application number
CA002324060A
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English (en)
Inventor
Andrew Shiau
Peter J. Kushner
David A. Agard
Geoffrey L. Greene
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.)
University of California
Arch Development Corp
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Individual
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 Individual filed Critical Individual
Publication of CA2324060A1 publication Critical patent/CA2324060A1/fr
Abandoned legal-status Critical Current

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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
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6875—Nucleoproteins
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones
    • C07K14/721—Steroid/thyroid hormone superfamily, e.g. GR, EcR, androgen receptor, oestrogen receptor
    • 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
    • G01N33/78—Thyroid gland hormones, e.g. T3, T4, TBH, TBG or their receptors
    • 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
    • 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
    • G01N2500/20—Screening for compounds of potential therapeutic value cell-free systems

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Microbiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)

Abstract

La présente invention concerne des méthodes et des composés d'agonistes/antagonistes de modulation de l'activité de récepteurs nucléaires, et de liaison aux ligands de récepteurs nucléaires. L'invention concerne une méthode d'identification de résidus comprenant un domaine de liaison aux ligands d'un récepteur nucléaire présentant un certain intérêt. L'invention concerne également une méthode d'identification d'agonistes et/ou d'antagonistes se liant au domaine de liaison aux ligands des récepteurs nucléaires, et du récepteur d'oestrogènes en particulier. L'identification et la manipulation du domaine de liaison aux ligands du récepteur d'oestrogènes et de composés se liant à ce site illustrent la présente invention. Les méthodes selon la présente invention peuvent s'appliquer à d'autres récepteurs nucléaires, y compris TR, GR, et PR.
CA002324060A 1998-03-30 1999-03-30 Methodes et composes de modulation d'activite de recepteurs nucleaires Abandoned CA2324060A1 (fr)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US7995698P 1998-03-30 1998-03-30
US11314698P 1998-12-16 1998-12-16
US11301498P 1998-12-16 1998-12-16
US60/079,956 1998-12-16
US60/113,014 1998-12-16
US60/113,146 1998-12-16
PCT/US1999/006937 WO1999050658A2 (fr) 1998-03-30 1999-03-30 Methodes et composes de modulation d'activite de recepteurs nucleaires

Publications (1)

Publication Number Publication Date
CA2324060A1 true CA2324060A1 (fr) 1999-10-07

Family

ID=27373576

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002324060A Abandoned CA2324060A1 (fr) 1998-03-30 1999-03-30 Methodes et composes de modulation d'activite de recepteurs nucleaires

Country Status (6)

Country Link
EP (1) EP1144997A3 (fr)
JP (1) JP2002516983A (fr)
KR (1) KR20010042373A (fr)
AU (1) AU3457199A (fr)
CA (1) CA2324060A1 (fr)
WO (1) WO1999050658A2 (fr)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999060014A2 (fr) * 1998-03-30 1999-11-25 The Regents Of The University Of California Methodes et composes de modulation de la liaison d'un coactivateur a des recepteurs nucleaires
WO2000052050A2 (fr) * 1999-03-01 2000-09-08 Karo Bio Ab Modeles d'homologie du recepteur de glucocorticoide
IL148192A0 (en) 1999-10-14 2002-09-12 Bristol Myers Squibb Co Crystals of androgen receptor ligand binding domain and methods utilizing the coordinates of the crystal structure
FR2801311B1 (fr) * 1999-11-22 2005-08-26 Centre Nat Rech Scient Polypeptides derives du recepteur nucleaire de la vitamine d, et leurs utilisations notamment dans le cadre du criblage d'analogues de la vitamine d
WO2002002488A2 (fr) * 2000-06-30 2002-01-10 The Regents Of The University Of California Procedes et composes pour moduler la fixation de coactivateurs a des recepteurs nucleaires
DE10036461A1 (de) * 2000-07-25 2002-02-07 Bayer Ag Ligandenbindedomäne des Ultraspiracle (USP)-Proteins
JP4593754B2 (ja) * 2000-10-13 2010-12-08 一般財団法人 化学物質評価研究機構 化学物質の５０％阻害濃度決定方法
JP2002296282A (ja) * 2001-04-02 2002-10-09 Enbiotec Laboratories:Kk 外因性内分泌攪乱物質の検出方法
WO2003004458A1 (fr) * 2001-07-03 2003-01-16 Biovitrum Ab Composes nouveaux
GB0209507D0 (en) * 2002-04-25 2002-06-05 Karobio Ab Nuclear receptor structure
US7302347B2 (en) * 2002-12-10 2007-11-27 The Regents Of The University Of California Method for creating specific, high affinity nuclear receptor pharmaceuticals
JPWO2005022436A1 (ja) * 2003-08-29 2006-10-26 独立行政法人産業技術総合研究所 蛋白質機能発現機構表示のための蛋白質構造三次元表示システム
US7264813B2 (en) 2003-09-24 2007-09-04 Nikken Sohonsha Corporation Therapeutic uses of Dunaliella powder
CA2543329A1 (fr) * 2003-10-24 2005-05-06 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Commutateurs geniques orthogonaux
CN102905685A (zh) * 2010-03-31 2013-01-30 株式会社爱茉莉太平洋 含有香豆雌酚或包含香豆雌酚的豆提取物的、用于皮肤护理的化妆品组合物
WO2011156518A2 (fr) 2010-06-10 2011-12-15 Aragon Pharmaceuticals, Inc. Modulateur du récepteur oestrogénique et utilisation de ces derniers
US9193714B2 (en) 2011-12-14 2015-11-24 Seragon Pharmaceuticals, Inc. Fluorinated estrogen receptor modulators and uses thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5650489A (en) * 1990-07-02 1997-07-22 The Arizona Board Of Regents Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof
JP2001524926A (ja) * 1991-09-18 2001-12-04 アフィマックス テクノロジーズ ナームロゼ フェンノートシャップ オリゴマーの雑多ライブラリーの集合体を合成する方法
AU686186B2 (en) * 1993-05-27 1998-02-05 Aventisub Ii Inc. Topologically segregated, encoded solid phase libraries
IL106106A0 (en) * 1993-06-22 1993-10-20 Interpharm Lab Ltd Library of polymeric molecules and its preparation
ATE344279T1 (de) * 1995-12-13 2006-11-15 Univ California Kristalle der mit einem ligand komplexierten ligandenbindedomäne des schilddrüsenhormonrezeptors

Also Published As

Publication number Publication date
WO1999050658A2 (fr) 1999-10-07
EP1144997A3 (fr) 2002-08-28
EP1144997A2 (fr) 2001-10-17
AU3457199A (en) 1999-10-18
KR20010042373A (ko) 2001-05-25
WO1999050658A3 (fr) 2001-08-16
JP2002516983A (ja) 2002-06-11

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