Non-endogenous, constitutively activated known G protein-coupled receptors
First Claim
1. A method for directly identifying a non-endogenous compound as a compound having inverse agonist, agonist, or partial agonist activity to a non-endogenous, constitutively activated version of a known G protein-coupled receptor, wherein said non-endogenous, constitutively activated version comprises the amino acid sequence of SEQ ID NO:
- 453, said method comprising;
(a) contacting a non-endogenous candidate compound with said non-endogenous, constitutively activated version of the known GPCR comprising the amino acid sequence of SEQ ID NO;
453; and
(b) the compound efficacy at said contacted receptor, and identifying whether said non-endogenous compound has inverse activity, or partial agonist activity at said contacted receptor.
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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.
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Citations
3 Claims
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1. A method for directly identifying a non-endogenous compound as a compound having inverse agonist, agonist, or partial agonist activity to a non-endogenous, constitutively activated version of a known G protein-coupled receptor, wherein said non-endogenous, constitutively activated version comprises the amino acid sequence of SEQ ID NO:
- 453, said method comprising;
(a) contacting a non-endogenous candidate compound with said non-endogenous, constitutively activated version of the known GPCR comprising the amino acid sequence of SEQ ID NO;
453; and(b) the compound efficacy at said contacted receptor, and identifying whether said non-endogenous compound has inverse activity, or partial agonist activity at said contacted receptor. - View Dependent Claims (2, 3)
- 453, said method comprising;
Specification