Methods of assaying for G protein-coupled receptor ligands and modulators
OwnerGabriel Bersteininventor
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Abstract
The present invention features methods of assaying for ligands and/or modulators of G protein-coupled receptors, for example, orphan G protein-coupled receptors. The methods of the invention feature constitutively active arrestin mutants, in particular, phosphorylation independent mutants. Also described are specific phosphorylation independent arrestin mutants and methods of making such mutants.
Claims38
A method of identifying a G protein-coupled receptor (GPCR) ligand comprising contacting a composition comprising the GPCR and a constitutively active arrestin mutant with a test compound and determining the ability of the test compound to modulate binding of the arrestin mutant to the GPCR, wherein modulation of binding indicates that the test compound is a GPCR ligand.
A method of identifying a G protein-coupled receptor (GPCR) antagonist comprising contacting a composition comprising the GPCR, a phosphorylation-independent arrestin mutant and a GPCR agonist with a test compound and determining the ability of the test compound to modulate binding of the arrestin mutant to said GPCR, wherein modulation of binding indicates that the test compound is a GPCR antagonist.
A method of identifying a G protein-coupled receptor (GPCR) ligand comprising contacting a GPCR with a phosphorylation-independent arrestin mutant and a test compound and determining the ability of the test compound to modulate binding of the arrestin mutant to the GPCR, wherein modulation of binding indicates that the test compound is a GPCR ligand.
A method of identifying a surrogate ligand for an orphan G protein-coupled receptor (GPCR) comprising contacting a membrane preparation comprising said orphan GPCR and a phosphorylation-independent arrestin mutant with a test compound and determining the ability of the test compound to effect binding of said arrestin mutant to said orphan GPCR.
A phosphorylation-independent β arrestin mutant.
A phosphorylation-independent β arrestin mutant having the amino acid of SEQ ID NO:
- 7.
A phosphorylation-independent β arrestin mutant having the amino acid sequence of SEQ ID NO:
- 8.
Dependencies are inferred from the claim text.