WO2003055914A3 - Modified receptors for the discovery of therapeutic ligands - Google Patents

Modified receptors for the discovery of therapeutic ligands Download PDF

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Publication number
WO2003055914A3
WO2003055914A3 PCT/DK2002/000900 DK0200900W WO03055914A3 WO 2003055914 A3 WO2003055914 A3 WO 2003055914A3 DK 0200900 W DK0200900 W DK 0200900W WO 03055914 A3 WO03055914 A3 WO 03055914A3
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WO
WIPO (PCT)
Prior art keywords
receptors
protein
interaction
modified
conformation
Prior art date
Application number
PCT/DK2002/000900
Other languages
French (fr)
Other versions
WO2003055914A2 (en
Inventor
Thue W Schwartz
Lene Martini
Arne Heydorn
Rasmus Joergensen
Original Assignee
7Tm Pharma As
Thue W Schwartz
Lene Martini
Arne Heydorn
Rasmus Joergensen
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 7Tm Pharma As, Thue W Schwartz, Lene Martini, Arne Heydorn, Rasmus Joergensen filed Critical 7Tm Pharma As
Priority to AU2002358469A priority Critical patent/AU2002358469A1/en
Publication of WO2003055914A2 publication Critical patent/WO2003055914A2/en
Publication of WO2003055914A3 publication Critical patent/WO2003055914A3/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
    • G01N33/5091—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing the pathological state of an organism
    • 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
    • G01N33/5005—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
    • G01N33/502—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
    • G01N33/5035—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 on sub-cellular localization
    • 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
    • G01N33/5041—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 involving analysis of members of signalling pathways
    • 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
    • G01N33/5306—Improving reaction conditions, e.g. reduction of non-specific binding, promotion of specific binding
    • 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
    • G01N33/6863—Cytokines, i.e. immune system proteins modifying a biological response such as cell growth proliferation or differentiation, e.g. TNF, CNF, GM-CSF, lymphotoxin, MIF or their receptors
    • 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
    • G01N33/6872—Intracellular protein regulatory factors and their receptors, e.g. including ion channels
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide

Abstract

A drug discovery method for selecting a compound selected from the group consisting of a small organic substance, a biopharmaceutical and an antibody or part thereof. The method comprises the steps of i) expressing one or more receptors on a cell membrane, such as, e.g., an exterior cell surface of a cell, ii) contacting one or more expressed receptors with a test compound or a selection of test compounds (libraries) and iii) selecting one or more compounds based on its ability to bind one or more receptors. The step of expressing the one or more receptors comprises capturing one or more receptors on the exterior cell surface in a conformation that predominantly enables binding or interaction with a ligand, and the conformation that predominantly enables binding or interaction with a ligand is provided by modification of one or more receptors by a method comprising at least one of the following: (a) fusion with any protein which keeps the receptor in the desired conformation such as, e.g. an arrestin, a modified arrestin, a G-protein or a modified G-protein, (b) site-directed mutagenesis, and (c) deletion. The receptors may be captured on the exterior cell surface by at least one of the following: (d) interaction of the receptor with a scaffolding protein, optionally, with a scaffolding protein network and (e) means for blocking receptor internalization, e.g. by co-expression of a mutated dynamin or a modified arrestin or by use of chemicals such as, e.g., sucrose and/or Tris.
PCT/DK2002/000900 2001-12-21 2002-12-20 Modified receptors for the discovery of therapeutic ligands WO2003055914A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002358469A AU2002358469A1 (en) 2001-12-21 2002-12-20 Modified receptors for the discovery of therapeutic ligands

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
DKPA200101944 2001-12-21
DKPA200101944 2001-12-21
DKPA200200113 2002-01-22
DKPA200200113 2002-01-22
US39412202P 2002-07-03 2002-07-03
DKPA200201043 2002-07-03
DKPA200201043 2002-07-03
US60/394,122 2002-07-03

Publications (2)

Publication Number Publication Date
WO2003055914A2 WO2003055914A2 (en) 2003-07-10
WO2003055914A3 true WO2003055914A3 (en) 2003-10-23

Family

ID=27439851

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DK2002/000900 WO2003055914A2 (en) 2001-12-21 2002-12-20 Modified receptors for the discovery of therapeutic ligands

Country Status (2)

Country Link
AU (1) AU2002358469A1 (en)
WO (1) WO2003055914A2 (en)

Cited By (1)

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US9308204B2 (en) 2009-11-02 2016-04-12 Pfizer Inc. Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives

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US7871619B2 (en) * 2001-11-30 2011-01-18 Chemocentryx, Inc. Compositions and methods for detecting and treating diseases and conditions related to chemokine receptors
WO2006113679A2 (en) 2005-04-15 2006-10-26 Board Of Regents, The University Of Texas System Delivery of sirna by neutral lipid compositions
US20090155272A1 (en) * 2005-09-30 2009-06-18 Muschler John L Targeted pharmaceuticals and ligands
EP1857818A1 (en) * 2006-05-15 2007-11-21 DIGILAB BioVisioN GmbH Diagnostic and therapeutic uses of peptides for pre-forms of type 2 diabetes and conditions associated therewith
US8435762B2 (en) 2008-10-09 2013-05-07 Howard Hughes Medical Institute Chimeric ligand-gated ion channels and methods of use thereof
CA2781682A1 (en) 2009-12-04 2011-06-09 Genentech, Inc. Multispecific antibodies, antibody analogs, compositions, and methods
US10294303B2 (en) * 2015-12-23 2019-05-21 Amgen Inc. Method of treating or ameliorating metabolic disorders using binding proteins for gastric inhibitory peptide receptor (GIPR) in combination with GLP-1 agonists
US20210087286A1 (en) * 2017-06-20 2021-03-25 Amgen Inc. Method of treating or ameliorating metabolic disorders using binding proteins for gastric inhibitory peptide receptor (gipr) in combination with glp-1 agonists

Citations (5)

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WO2001050127A2 (en) * 1999-12-30 2001-07-12 7Tm Pharma Screening using biological target molecules with metal-ion binding sites
WO2001058923A2 (en) * 2000-02-07 2001-08-16 Tropix, Inc. Improved systems for sensitive detection of g-protein coupled receptor and orphan receptor function using reporter enzyme mutant complementation
WO2001059451A1 (en) * 2000-02-07 2001-08-16 Tropix, Inc. Enzyme-based gprotein-coupled receptor assay
WO2001067106A2 (en) * 2000-03-03 2001-09-13 Millennium Pharmaceuticals, Inc. Identification of g protein-coupled receptor ligands and modulators
WO2002046763A1 (en) * 2000-12-04 2002-06-13 Novo Nordisk A/S Method of identifying compounds capable of acting as agonists or antagonists of g-protein coupled receptors

Patent Citations (5)

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Publication number Priority date Publication date Assignee Title
WO2001050127A2 (en) * 1999-12-30 2001-07-12 7Tm Pharma Screening using biological target molecules with metal-ion binding sites
WO2001058923A2 (en) * 2000-02-07 2001-08-16 Tropix, Inc. Improved systems for sensitive detection of g-protein coupled receptor and orphan receptor function using reporter enzyme mutant complementation
WO2001059451A1 (en) * 2000-02-07 2001-08-16 Tropix, Inc. Enzyme-based gprotein-coupled receptor assay
WO2001067106A2 (en) * 2000-03-03 2001-09-13 Millennium Pharmaceuticals, Inc. Identification of g protein-coupled receptor ligands and modulators
WO2002046763A1 (en) * 2000-12-04 2002-06-13 Novo Nordisk A/S Method of identifying compounds capable of acting as agonists or antagonists of g-protein coupled receptors

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Title
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HILAIRET SANDRINE ET AL: "Agonist-promoted internalization of a ternary complex between calcitonin receptor-like receptor, receptor activity-modifying protein 1 (RAMP1), and beta-arrestin.", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 276, no. 45, 9 November 2001 (2001-11-09), November 9, 2001, pages 42182 - 42190, XP002243925, ISSN: 0021-9258 *
LAPORTE STEPHANE A ET AL: "The interaction of beta-arrestin with the AP-2 adaptor is required for the clustering of beta2-adrenergic receptor into clathrin-coated pits.", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 275, no. 30, 28 July 2000 (2000-07-28), pages 23120 - 23126, XP002243926, ISSN: 0021-9258 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9308204B2 (en) 2009-11-02 2016-04-12 Pfizer Inc. Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives
US9439902B2 (en) 2009-11-02 2016-09-13 Pfizer Inc. Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives
US9439901B2 (en) 2009-11-02 2016-09-13 Pfizer Inc. Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives

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AU2002358469A8 (en) 2003-07-15
WO2003055914A2 (en) 2003-07-10
AU2002358469A1 (en) 2003-07-15

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