Methods for screening for binding partners of G-protein coupled receptors
AssigneeHeptares Therapeutics Limited
InventorsMalcolm Peter Weir, Fiona Hamilton Marshall
Life of this patent
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Abstract
A method of producing a conformational specific binding partner of a GPCR, the method comprising: a) providing a mutant GPCR of a parent GPCR, wherein the mutant GPCR has increased stability in a particular conformation relative to the parent GPCR; b) providing a test compound; c) determining whether the test compound binds to the mutant GPCR when residing in a particular conformation; and d) isolating a test compound that binds to the mutant GPCR when residing in the particular formation. Methods of producing GPCRs with increased stability relative to a parent GPCR are also disclosed.
Claims20
A biosensor comprising a mutant GPCR of a parent GPCR, wherein the mutant GPCR is able to bind to the same ligand as the parent GPCR and which has increased stability in a particular conformation relative to the parent GPCR in the same particular conformation under denaturing conditions, which stability in a particular conformation can be determined by measuring denaturation as manifest by loss of ligand binding ability, and wherein when a target substance binds to said mutant GPCR, a detectable signal is produced.
A method of producing a biosensor comprising a mutant GPCR of a parent GPCR, wherein the mutant GPCR is one that is able to bind to the same ligand as the parent GPCR and which has increased stability in a particular conformation relative to the parent GPCR in the same particular conformation under denaturing conditions, which stability in a particular conformation can be determined by measuring denaturation as manifest by loss of ligand binding ability, and wherein when a target substance binds to said mutant GPCR, a detectable signal is produced, the method comprising:
- (a) providing a mutant GPCR of a parent GPCR, wherein the mutant GPCR has increased stability in a particular conformation relative to the parent GPCR;
- and
- (b) immobilising the mutant GPCR onto a solid support for incorporation into a biosensor.
Dependencies are inferred from the claim text.