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EP1021462A1 - Essais pour ligands a recepteurs nucleaires reposant sur le transfert d'energie de resonance en fluorescence - Google Patents

Essais pour ligands a recepteurs nucleaires reposant sur le transfert d'energie de resonance en fluorescence

Info

Publication number
EP1021462A1
EP1021462A1 EP98956094A EP98956094A EP1021462A1 EP 1021462 A1 EP1021462 A1 EP 1021462A1 EP 98956094 A EP98956094 A EP 98956094A EP 98956094 A EP98956094 A EP 98956094A EP 1021462 A1 EP1021462 A1 EP 1021462A1
Authority
EP
European Patent Office
Prior art keywords
nuclear receptor
binding domain
ligand binding
cbp
human
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.)
Withdrawn
Application number
EP98956094A
Other languages
German (de)
English (en)
Other versions
EP1021462A4 (fr
Inventor
Richard T. Cummings
Jeffrey D. Hermes
David E. Moller
Gaochao Zhou
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.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP1021462A1 publication Critical patent/EP1021462A1/fr
Publication of EP1021462A4 publication Critical patent/EP1021462A4/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • C07K14/475—Growth factors; Growth regulators
    • 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
    • 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
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/536—Immunoassay; Biospecific binding assay; Materials therefor with immune complex formed in liquid phase
    • G01N33/542—Immunoassay; Biospecific binding assay; Materials therefor with immune complex formed in liquid phase with steric inhibition or signal modification, e.g. fluorescent quenching
    • 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
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/566—Immunoassay; Biospecific binding assay; Materials therefor using specific carrier or receptor proteins as ligand binding reagents where possible specific carrier or receptor proteins are classified with their target compounds
    • 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
    • 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
    • G01N2333/70567—Nuclear receptors, e.g. retinoic acid receptor [RAR], RXR, nuclear orphan receptors
    • 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

Definitions

  • the nuclear receptor co-activator is human SRC-1 and the binding portion includes a contiguous stretch of amino acids of human SRC-1 selected from the group consisting of: positions 45-53, 632-640, 689-696, 748-755, and 1434-1441.
  • a nuclear receptor or ligand binding domain thereof labeled with a first fluorescent reagent (a) a nuclear receptor or ligand binding domain thereof labeled with a first fluorescent reagent; (b) CBP, p300, or other nuclear receptor co-activator, or a binding portion thereof, labeled with a second fluorescent reagent; (c) an agonist of the nuclear receptor; and
  • FRET donor-acceptor pairs are suitable for the practice of the present invention.
  • the following donor- acceptor pairs can be used: dansyl/fluorescein; fluorescein/rhodamine; tryptophan/aminocoumarin.
  • Human PPAR ⁇ 2 contains the same amino acid sequence as human PPAR ⁇ l except for an amino terminal addition of 24 amino acids (see Elbrecht et al., 1996, Biochem. Biophys. Res. Comm. 224:431-437).
  • hCBPl-113 was directly labeled with europium cryptate (Eu3+K); hPPAR ⁇ lLBD was indirectly labeled with

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Cell Biology (AREA)
  • Organic Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Food Science & Technology (AREA)
  • Microbiology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Zoology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Peptides Or Proteins (AREA)

Abstract

L'invention concerne un procédé permettant d'identifier des agonistes et des antagonistes vis-à-vis de récepteurs nucléaires, qui consiste à mesurer le transfert d'énergie de résonance en fluorescence entre un récepteur nucléaire ou un domaine de liaison marqué par fluorescence et une protéine se liant au CRE, p300, un autre co-activateur nucléaire ou une partie de liaison qui lui appartient. Le procédé est simple, rapide, et peu onéreux. L'invention concerne également des récepteurs nucléaires et des co-activateurs de ces récepteurs marqués au moyen de réactifs fluorescents, qui sont destinés à être utilisés aux fins du procédé considéré.
EP98956094A 1997-10-07 1998-10-06 Essais pour ligands a recepteurs nucleaires reposant sur le transfert d'energie de resonance en fluorescence Withdrawn EP1021462A4 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US6138597P 1997-10-07 1997-10-07
US61385P 1997-10-07
PCT/US1998/021049 WO1999018124A1 (fr) 1997-10-07 1998-10-06 Essais pour ligands a recepteurs nucleaires reposant sur le transfert d'energie de resonance en fluorescence

Publications (2)

Publication Number Publication Date
EP1021462A1 true EP1021462A1 (fr) 2000-07-26
EP1021462A4 EP1021462A4 (fr) 2005-04-13

Family

ID=22035450

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98956094A Withdrawn EP1021462A4 (fr) 1997-10-07 1998-10-06 Essais pour ligands a recepteurs nucleaires reposant sur le transfert d'energie de resonance en fluorescence

Country Status (4)

Country Link
EP (1) EP1021462A4 (fr)
JP (1) JP2001519525A (fr)
CA (1) CA2305711A1 (fr)
WO (1) WO1999018124A1 (fr)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000025134A1 (fr) * 1998-10-23 2000-05-04 Glaxo Group Limited Procede d'identification de ligands de recepteurs nucleaires
ES2326850T3 (es) * 1998-12-23 2009-10-20 Glaxo Group Limited Ensayos para ligandos de receptores nucleares.
WO2001020326A2 (fr) * 1999-09-13 2001-03-22 Equitech Laboratories, Inc. Materiaux et procede de detection et de quantification d'un analysat
WO2001040805A1 (fr) * 1999-11-30 2001-06-07 Akzo Nobel N.V. Composes steroidiques destines a des dosages par liaison de recepteur de steroides
AU2001250898A1 (en) * 2000-03-17 2001-10-03 The Salk Institute For Biological Studies Compositions associated with complex formation
US7198924B2 (en) 2000-12-11 2007-04-03 Invitrogen Corporation Methods and compositions for synthesis of nucleic acid molecules using multiple recognition sites
US6924311B2 (en) 2001-10-17 2005-08-02 X-Ceptor Therapeutics, Inc. Methods for affecting various diseases utilizing LXR compounds
EP1310799B1 (fr) 2001-11-07 2005-12-21 Schering AG Procédé de criblage de ligands du récepteur de l'estrogène
CA2491468A1 (fr) * 2002-07-24 2004-01-29 3-Dimensional Pharmaceuticals, Inc. Methode d'identification de ligands
DE60320828D1 (de) 2002-11-07 2008-06-19 Univ Erasmus Fret proben und verfahren zur erkennung aufeinander einwirkeneden moleküle
JP4803976B2 (ja) * 2003-07-09 2011-10-26 独立行政法人科学技術振興機構 細胞内ｉｐ３測定用分子センサー
NZ545568A (en) * 2003-08-28 2009-06-26 Choongwae Pharma Corp Use of compounds that modulate beta-catenin/TCF activated transcription for manufacture of a medicamnet to treat cancer
US8304189B2 (en) 2003-12-01 2012-11-06 Life Technologies Corporation Nucleic acid molecules containing recombination sites and methods of using the same
US20080286260A1 (en) * 2004-03-26 2008-11-20 Bayer Healthcare Ag Diagnostic and Therapeutics for Diseases Associated with Peroxisome Proliferative Activated Receptor Alpha (Ppara)
KR100704011B1 (ko) 2005-02-16 2007-04-04 한국과학기술원 금속나노입자와 양자점의 ｆｒｅｔ에 의한 생체분자특이결합 검출 방법
WO2007002654A2 (fr) 2005-06-28 2007-01-04 Daiichi Sankyo Company, Limited. Methode d'essai de ligand lxr
JP5264421B2 (ja) 2007-11-22 2013-08-14 富士フイルム株式会社 被験物測定用担体およびその製造方法
WO2009141926A1 (fr) * 2008-05-23 2009-11-26 国立大学法人東京大学 Procédé d'acquisition d'un composé capable d'agir sur le métabolisme du glucose/métabolisme lipidique
LT4026917T (lt) * 2014-04-14 2024-03-12 Yissum Research And Development Company Of The Hebrew University Of Jerusalem Ltd. Ląstelių ar audinio žūties nustatymo arba iš audinio ar ląstelės gautos dnr kilmės nustatymo dnr metilinimo analizės būdu metodas ir rinkinys
WO2017212428A1 (fr) 2016-06-07 2017-12-14 The Regents Of The University Of California Motifs de méthylation d'adn acellulaire pour l'analyse de maladies et d'affections

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9608143D0 (en) * 1996-04-19 1996-06-26 Ver Nl Kanker Inst Assay
WO1998056806A1 (fr) * 1997-06-12 1998-12-17 The Regents Of The University Of California Proteine de coactivation de facteur de transcription, p/cip
CA2319167A1 (fr) * 1998-02-12 1999-08-19 Prolifix Limited Interaction de la cycline d1 et des coactivateurs de recepteur steroidien, et utilisations aux fins d'essais

Also Published As

Publication number Publication date
JP2001519525A (ja) 2001-10-23
EP1021462A4 (fr) 2005-04-13
WO1999018124A1 (fr) 1999-04-15
CA2305711A1 (fr) 1999-04-15

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