Method for selecting allosteric regulators of class III G protein-coupled receptors
AssigneeCentre National de la Recherche Scientifique (CNRS)
InventorsFlorence Gaven, Cyril Goudet, Jean-Philippe Pin, Laurent Prezeau
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Abstract
A method for identifying and selecting a compound acting as an allosteric regulator of a GPCR-III is described. A method comparing the activity level of a recombinant GPCR-III (GPCR-III-Δ), essentially depleted of the extracellular domain of the corresponding native GPCR-III, in the presence of a given compound, with the activity level of the same GPCR-III-Δ is described. A method of identifying positive or negative allosteric regulators of GPCRs-III is described.
Claims13
A method for identifying and selecting a compound that acts as a positive allosteric regulator of a class III G protein-coupled receptor (GPCR-III) selected from the group consisting of:
- glutamate-activated receptors;
- GABA-activated receptors;
- putative pheromone receptors;
- and
- taste receptors, said method comprising at least the following steps:
- a) producing a recombinant GPCR-III (GPCR-III-Δ) essentially depleted of the extracellular domain of the corresponding native GPCR-III;
- b) bringing said compound into contact with said GPCR-III-Δ in the absence of an agonist of said GPRC-III;
- c) measuring the level N1 of activity of said GPCR-III-Δ in the presence of said compound;
- d) comparing the level N1 measured in step c) with the level N0 of activity of the GPCR-III-Δ in the absence of said compound;
- and
- e) if N1 is significantly different from N0, identifying and selecting said positive allosteric regulator,
- where said positive allosteric regulator has no effect on the GPCR-III, if GPCR-III is not simultaneously activated by an agonist of GPCR-III, but behaves like an agonist or an inverse agonist of said GPCR-III-Δ.
Dependencies are inferred from the claim text.