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publicationDate 2020-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2020157441-A1
titleOfInvention Method for measuring the modulation of the activation of a g protein-coupled receptor with gtp analogues
abstract The invention concerns a method for determining the ability of a molecule to modulate the activation of a G protein-coupled receptor (GPCR), the method comprising the following steps: a) introducing, into a first container: - a membrane preparation bearing one or more GPCR(s) and one or more Galpha protein(s), - a source of non-hydrolysable or slowly hydrolysable GTP labelled by a first member of a pair of RET partners, - a ligand of the alpha sub-unit of a G protein (Galpha protein) labelled by a second member of the pair of RET partners, the ligand being capable of binding with the full Galpha protein bound to the non-hydrolysable or slowly hydrolysable GTP labelled by the first member of a pair of RET partners, - optionally, a GPCR agonist; b) measuring the RET signal emitted in the first container; c) introducing, (i) into a second container, the same reagents as in step a) and the molecule to be tested or, (ii) into the first container, the molecule to be tested; d) measuring the RET signal emitted in the second container or in the first container obtained in step c); e) comparing the signals obtained in steps b) and d), a modulation in the signal obtained in step d) relative to that obtained in step b) indicating that the molecule to be tested is capable of modulating the activation of the GPCR.
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP13636
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226423208
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http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID25686
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP31356
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ03343
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Total number of triples: 480.