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WO2003090666A3 - Structure de recepteur nucleaire - Google Patents

Structure de recepteur nucleaire Download PDF

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Publication number
WO2003090666A3
WO2003090666A3 PCT/EP2003/004900 EP0304900W WO03090666A3 WO 2003090666 A3 WO2003090666 A3 WO 2003090666A3 EP 0304900 W EP0304900 W EP 0304900W WO 03090666 A3 WO03090666 A3 WO 03090666A3
Authority
WO
WIPO (PCT)
Prior art keywords
glucocorticoid receptor
receptor protein
protein crystals
methods
receptor
Prior art date
Application number
PCT/EP2003/004900
Other languages
English (en)
Other versions
WO2003090666A2 (fr
Inventor
Clarissa G Jakob
Steven Muchmore
Bjoern Kauppi
Mathias Farnegaardh
John E Harlan
Jie Yang
Mats Carlquist
Owe Engstroem
Harri Ahola
Lars Oehman
Original Assignee
Karobio Ab
Abbott Lab
Clarissa G Jakob
Steven Muchmore
Bjoern Kauppi
Mathias Farnegaardh
John E Harlan
Jie Yang
Mats Carlquist
Owe Engstroem
Harri Ahola
Lars Oehman
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 Karobio Ab, Abbott Lab, Clarissa G Jakob, Steven Muchmore, Bjoern Kauppi, Mathias Farnegaardh, John E Harlan, Jie Yang, Mats Carlquist, Owe Engstroem, Harri Ahola, Lars Oehman filed Critical Karobio Ab
Priority to AU2003233315A priority Critical patent/AU2003233315A1/en
Publication of WO2003090666A2 publication Critical patent/WO2003090666A2/fr
Publication of WO2003090666A3 publication Critical patent/WO2003090666A3/fr

Links

Classifications

    • 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
    • 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
    • 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
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00—ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • G16B15/30—Drug targeting using structural data; Docking or binding prediction
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16C—COMPUTATIONAL CHEMISTRY; CHEMOINFORMATICS; COMPUTATIONAL MATERIALS SCIENCE
    • G16C20/00—Chemoinformatics, i.e. ICT specially adapted for the handling of physicochemical or structural data of chemical particles, elements, compounds or mixtures
    • G16C20/30—Prediction of properties of chemical compounds, compositions or mixtures
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A90/00—Technologies having an indirect contribution to adaptation to climate change
    • Y02A90/10—Information and communication technologies [ICT] supporting adaptation to climate change, e.g. for weather forecasting or climate simulation

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Organic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cell Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Zoology (AREA)
  • Microbiology (AREA)
  • Toxicology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention a trait aux domaines de la biotechnologie, de la purification et de la cristallisation des protéines, de l'analyse par diffraction de rayons X, de la modélisation moléculaire informatique tridimensionnelle et de la conception rationnelle de médicaments. L'invention se rapporte au récepteur des glucocorticoïdes et aux ligands associés à ce récepteur, et en particulier au récepteur cristallin des glucocorticoïdes (GR) et à des procédés d'identification des ligands utilisant le récepteur GR, ainsi qu'à des composés, des compositions et des procédés de sélection, fabrication et utilisation d'agents thérapeutiques ou diagnostiques présentant une activité de modulation du GR ou de liaison au GR.
PCT/EP2003/004900 2002-04-25 2003-04-25 Structure de recepteur nucleaire WO2003090666A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003233315A AU2003233315A1 (en) 2002-04-25 2003-04-25 Glucocorticoid receptor protein crystals

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0209507.3A GB0209507D0 (en) 2002-04-25 2002-04-25 Nuclear receptor structure
GB0209507.3 2002-04-25

Publications (2)

Publication Number Publication Date
WO2003090666A2 WO2003090666A2 (fr) 2003-11-06
WO2003090666A3 true WO2003090666A3 (fr) 2004-01-08

Family

ID=9935520

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/004900 WO2003090666A2 (fr) 2002-04-25 2003-04-25 Structure de recepteur nucleaire

Country Status (3)

Country Link
AU (1) AU2003233315A1 (fr)
GB (1) GB0209507D0 (fr)
WO (1) WO2003090666A2 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2337679T3 (es) * 2002-07-18 2010-04-28 Bristol-Myers Squibb Company Composiciones y procedimientos que implican el sitio ii de los receptores nucleares de hormonas.

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999050658A2 (fr) * 1998-03-30 1999-10-07 The Regents Of The University Of California Methodes et composes de modulation d'activite de recepteurs nucleaires
WO2000052050A2 (fr) * 1999-03-01 2000-09-08 Karo Bio Ab Modeles d'homologie du recepteur de glucocorticoide
WO2003015692A2 (fr) * 2001-07-17 2003-02-27 Smithkline Beecham Corporation Domaine de fixation aux ligands du recepteur du glucocorticoide cristallise et procedes de criblage l'utilisant

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999050658A2 (fr) * 1998-03-30 1999-10-07 The Regents Of The University Of California Methodes et composes de modulation d'activite de recepteurs nucleaires
WO2000052050A2 (fr) * 1999-03-01 2000-09-08 Karo Bio Ab Modeles d'homologie du recepteur de glucocorticoide
WO2003015692A2 (fr) * 2001-07-17 2003-02-27 Smithkline Beecham Corporation Domaine de fixation aux ligands du recepteur du glucocorticoide cristallise et procedes de criblage l'utilisant

Non-Patent Citations (16)

* Cited by examiner, † Cited by third party
Title
B.F. LUISI ET AL: "Crystallographic analysis of the interaction of the glucocorticoid receptor with DNA", NATURE, vol. 352, 8 August 1991 (1991-08-08), pages 497 - 505, XP002257986 *
BRIAN M. NECELA ET AL: "Crystallization of the human glucocorticoid receptor ligand binding domain: a step towards selective glucocorticoids", TRENDS IN PHARMACOLOGICAL SCIENCES, vol. 24, no. 2, February 2003 (2003-02-01), pages 58 - 61, XP002257982 *
CATHERINE ROBIN-JAGERSCHMIDT ET AL: "Residues in the Ligand Binding Domain That Confer Progestin or Glucocorticoid Specificity and Modulate the Receptor Transactivation Capacity", MOLECULAR ENDOCRINOLOGY, vol. 14, no. 7, 2000, pages 1028 - 1037, XP002257984 *
DATABASE BIOSIS [online] BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; 23 June 2000 (2000-06-23), LIND ULRIKA ET AL: "Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis: Gln-642 plays an important role in steroid recognition and binding", XP002257992, Database accession no. PREV200000369093 *
DATABASE GENBANK Accession no. AAA16603; XP002257991 *
DATABASE GENBANK ON NCBI Accession no. AAA16603; 10 March 1994 (1994-03-10), MUNROE, D. G. ET AL: "Alternative splicing within the DNA binding domain creates a novel isoform of the human glucocorticoid receptor", XP002257990 *
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; 20 June 2003 (2003-06-20), KAUPPI BJÖRN ET AL: "The three-dimensional structures of antagonistic and agonistic forms of the glucocorticoid receptor ligand-binding domain: RU-486 induces a transconformation that leads to active antagonism.", XP002257983, Database accession no. NLM12686538 *
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; August 2001 (2001-08-01), DEY R ET AL: "Homology modelling of the ligand-binding domain of glucocorticoid receptor: binding site interactions with cortisol and corticosterone.", XP002257985, Database accession no. NLM11579225 *
DATABASE REGISTRY FILE XP002258182 *
JAN-ŸKE GUSTAFSSON ET AL: "Structure, function and regulation of the glucocorticoid receptor", PROGRESS IN CLINICAL AND BIOLOGICAL RESEARCH, vol. 322, 1990, pages 65 - 80, XP002257989 *
JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 275, no. 25, 23 June 2000 (2000-06-23), pages 19041 - 19049, ISSN: 0021-9258 *
PROTEIN ENGINEERING. ENGLAND AUG 2001, vol. 14, no. 8, August 2001 (2001-08-01), pages 565 - 571, ISSN: 0269-2139 *
RANDY K. BLEDSOE ET AL: "Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Reveals a Novel Mode of Receptor Dimerization and Coactivator Recognition", CELL, vol. 110, 12 July 2002 (2002-07-12), pages 93 - 105, XP002257981 *
THE JOURNAL OF BIOLOGICAL CHEMISTRY. UNITED STATES 20 JUN 2003, vol. 278, no. 25, 20 June 2003 (2003-06-20), pages 22748 - 22754, ISSN: 0021-9258 *
WILLIAM BOURGUET ET AL: "Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-alpha", NATURE, vol. 375, 1 June 1995 (1995-06-01), pages 377 - 382, XP002257987 *
YIHOUNG WAN ET AL: "Separable Features of the Ligand-Binding Domain Determine the Differential Subcellular Localization and Ligand-Binding Specificity of Glucocorticoid Receptor and Progesterone Receptor", MOLECULAR ENDOCRINOLOGY, vol. 15, no. 1, 2001, pages 17 - 31, XP002257988 *

Also Published As

Publication number Publication date
AU2003233315A8 (en) 2003-11-10
WO2003090666A2 (fr) 2003-11-06
GB0209507D0 (en) 2002-06-05
AU2003233315A1 (en) 2003-11-10

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