VERFAHREN ZUR MESSUNG DER MODULATION DER AKTIVITÄT EINES G-PROTEIN-GEKOPPELTEN REZEPTORS

摘要

The invention relates to a method for determining the ability of a molecule to modulate the activity of a G protein-coupled receptor (GPCR), said method comprising the following steps: a) introducing, into a first container: - a first membrane preparation bearing one or more GPCRs and one or more G protein(s), - a source of GDP or a source of GTP, - a first ligand of the alpha subunit of a G protein (Galpha protein) labelled with a first member of a pair of RET partners, and a second ligand of the Galpha protein labelled with a second member of the pair of RET partners, said ligands being able to specifically bind, either individually or in combination, to the empty Galpha protein or to the full Galpha protein; b) measuring the RET signal emitted in the first container; c) introducing (i) into a second container, the same reactants 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).