METHOD OF IDENTIFYING COMPOUNDS CAPABLE OF ACTING AS AGONISTS OR ANTAGONISTS OF G-PROTEIN COUPLED RECEPTORS
The present invention relates to a method for identifying compounds capable of affecting the activity of G-protein coupled receptors (GPCRs), i.e. identifying agonists or antagonists of said receptor type. In one embodiment said method comprises (a) contacting a test compound with cell membrane from...
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Main Authors | , , |
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Format | Patent |
Language | English French |
Published |
13.06.2002
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Edition | 7 |
Subjects | |
Online Access | Get full text |
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Abstract | The present invention relates to a method for identifying compounds capable of affecting the activity of G-protein coupled receptors (GPCRs), i.e. identifying agonists or antagonists of said receptor type. In one embodiment said method comprises (a) contacting a test compound with cell membrane from a GPCR expressing cell, an arrestin and a kinase in a buffer, (b) separating the GPCR-bound arerstin from tne unbound arrestin, and (c) determining the level of GCFR-bound arrestin. In another embodiment the method includes contacting a test compound with cell membrane and a phophorylation independant beta-arrestin mutant.
L'invention concerne un procédé d'identification de composés capables de modifier l'activité de récepteurs couplés à la protéine G (GPCR), c'est-à-dire d'identification d'agonistes et d'antagonistes dudit type de récepteur. Dans un mode de réalisation, le procédé consiste a) à mettre en contact un composé test avec une membrane cellulaire d'une cellule exprimant GPCR, une arrestine et une kinase dans un tampon, b) à séparer l'arrestine liée à GPCR de l'arrestine non liée, et c) à déterminer le niveau d'arrestine liée à GPCR. Dans un autre mode de réalisation, le procédé consiste à mettre en contact un composé test avec une membrane cellulaire et un mutant de bêta-arrestine indépendant de la phosphorylation. |
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AbstractList | The present invention relates to a method for identifying compounds capable of affecting the activity of G-protein coupled receptors (GPCRs), i.e. identifying agonists or antagonists of said receptor type. In one embodiment said method comprises (a) contacting a test compound with cell membrane from a GPCR expressing cell, an arrestin and a kinase in a buffer, (b) separating the GPCR-bound arerstin from tne unbound arrestin, and (c) determining the level of GCFR-bound arrestin. In another embodiment the method includes contacting a test compound with cell membrane and a phophorylation independant beta-arrestin mutant.
L'invention concerne un procédé d'identification de composés capables de modifier l'activité de récepteurs couplés à la protéine G (GPCR), c'est-à-dire d'identification d'agonistes et d'antagonistes dudit type de récepteur. Dans un mode de réalisation, le procédé consiste a) à mettre en contact un composé test avec une membrane cellulaire d'une cellule exprimant GPCR, une arrestine et une kinase dans un tampon, b) à séparer l'arrestine liée à GPCR de l'arrestine non liée, et c) à déterminer le niveau d'arrestine liée à GPCR. Dans un autre mode de réalisation, le procédé consiste à mettre en contact un composé test avec une membrane cellulaire et un mutant de bêta-arrestine indépendant de la phosphorylation. |
Author | POULSEN, FRITZ HEDING, ANDERS KNUDSEN, SANNE, MOELLER |
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DocumentTitleAlternate | PROCEDE D'IDENTIFICATION DE COMPOSES CAPABLES D'AGIR EN TANT QU'AGONISTES OU ANTAGONISTES DE RECEPTEURS COUPLES A LA PROTEINE G |
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Snippet | The present invention relates to a method for identifying compounds capable of affecting the activity of G-protein coupled receptors (GPCRs), i.e. identifying... |
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SubjectTerms | BEER BIOCHEMISTRY CHEMISTRY COMPOSITIONS OR TEST PAPERS THEREFOR CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES ENZYMOLOGY INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES MEASURING MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS METALLURGY MICROBIOLOGY MUTATION OR GENETIC ENGINEERING PHYSICS PROCESSES OF PREPARING SUCH COMPOSITIONS SPIRITS TESTING VINEGAR WINE |
Title | METHOD OF IDENTIFYING COMPOUNDS CAPABLE OF ACTING AS AGONISTS OR ANTAGONISTS OF G-PROTEIN COUPLED RECEPTORS |
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