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US 6,806,054 B2Granted
Non-endogenous, constitutively activated known G protein-coupled receptors
AssigneeArena Pharmaceuticals, Inc.
InventorsKarin Lehmann-Bruinsma, Chen W. Liaw, I-Lin Lin
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Abstract
The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is known (“known GPCRs”), and most particularly to mutated (non-endogenous) versions of the known GPCRs for use, most preferably in screening assays for the direct identification of candidate compounds as inverse agonists, agonists and partial agonists.
Claims3
A method for directly identifying a non-endogenous compound as a compound having an activity selected from the group consisting of:
- inverse agonists, agonists, and partial agonists, to a non-endogenous, constitutively activated version of a known G protein-coupled receptor, said receptor comprising a transmembrane-6 region and an intracellular region, comprising the steps of:
- (a) selecting a non-endogenous version of a known GPCR;
- (b) confirming that the selected non-endogenous GPCR of step (a) is constitutively active;
- (c) contacting a non-endogenous candidate compound with the non-endogenous, constitutively activated GPCR of step of (b);
- and
- (d) determining, by measurement of the compound efficacy at said contacted receptor, whether said non-endogenous compound is an inverse agonist, an agonist, or a partial agonist to said receptor of step (b);
- wherein said receptor of step (b) comprises the amino acid sequence of SEQ ID NO:449.
4 more elements
Dependencies are inferred from the claim text.