Method of screening binding of a compound to a receptor
AssigneeMarquette University
InventorVasanthi Jayaraman
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Abstract
Disclosed is a method of measuring affinity of a test compound for a receptor protein. The method includes the steps of providing a receptor-ligand complex comprising a receptor and a quinoxaline derivative ligand bound thereto; then contacting the receptor-ligand complex with a test compound, thereby yielding a receptor-test compound complex and an amount of free quinoxaline derivative; and then measuring the amount of the free quinoxaline derivative generated as a result of the previous step. In this fashion, the affinity of the test compound for the receptor can be determined.
Claims20
A method of measuring affinity of a test compound for a receptor protein, the method comprising:
- (a) providing a receptor-ligand complex comprising a receptor and a quinoxaline derivative ligand bound thereto;
- then
- (b) contacting the receptor-ligand complex of step (a) with a test compound under conditions and for a time sufficient to allow the test compound to bind to the receptor, thereby yielding a receptor-test compound complex and an amount of free quinoxaline derivative;
- and then
- (c) measuring the amount of the free quinoxaline derivative generated as a result of step (b), whereby the affinity of the test compound for the receptor is determined.
A method of measuring affinity of a test compound for a receptor protein, the method comprising:
- (a) providing a receptor-test compound complex comprising a non-NMDA glutamate receptor and a test compound bound thereto;
- then
- (b) contacting the receptor-test compound complex of step (a) with a known concentration of quinoxaline derivative under conditions and for a time sufficient to allow the quinoxaline derivative to bind to the receptor, thereby yielding a receptor-quinoxaline complex and an amount of free quinoxaline derivative;
- and then
- (c) measuring the amount of the free quinoxaline derivative generated as a result of step (b) and comparing the amount of the free quinoxline to the known concentration of quinoxaline used in step (b), whereby the affinity of the test compound for the receptor is determined.
A method of measuring affinity of a test compound for a non-NMDA glutamate receptor protein, the method comprising:
- (a) contacting a non-NMDA glutamate receptor with a known amount of a quinoxaline derivative under conditions and for a time sufficient to allow at least a portion of the quinoxaline derivative to bind to the receptor, thereby yielding a receptor-quinoxaline complex and a first amount of free quinoxline derivative;
- then
- (b) recording a visible spectrum of the free quinoxline from step (a);
- then
- (c) contacting the complex of step (a) with a test compound under conditions and for a time sufficient to allow the test compound to bind to the receptor, thereby displacing at least a portion of the quinoxaline derivative from the complex and yielding a receptor-test compound complex and a second amount of free quinoxaline derivative;
- (d) recording a visible spectrum of the free quinoxline derivative from step (c);
- and then
- (e) comparing the spectrum from step (b) with the spectrum from step (d), whereby the affinity of the test compound for the receptor is determined.
Dependencies are inferred from the claim text.