Methods for screening for binding partners of G-protein coupled receptors
First Claim
1. 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.
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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.
136 Citations
20 Claims
- 1. 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.
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12. 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:
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(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. - View Dependent Claims (13, 14, 15, 16, 17, 18, 19, 20)
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Specification