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US 2006/0188944 A1Published application
Methods of assaying receptor activity
AssigneeDuke University
InventorsLawrence Barak, Marc Caron, Stephen Ferguson, Jie Zhang
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Abstract
Described are methods of detecting G-protein coupled receptor (GPCR) activity in vivo and in vitro; methods of assaying GPCR activity; and methods of screening for GPCR ligands, G Protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process.
Claims11
1-13. (canceled)
A method of automatically screening compounds for an effect on G protein coupled receptor (GPCR) pathway activity in a cell under test conditions in response to exposure to a test compound comprising:
- a. providing cells including a detectably labeled cellular component involved in the desensitization pathway of a GPCR, wherein said cellular component is an arrestin, said cells over-expressing said GPCR;
- b. providing a tool for at least one of detecting or measuring said detectably labeled cellular component;
- c. providing a computer for controlling said tool for at least one of detecting or measuring said detectably labeled cellular component;
- d. exposing the cells to one or more test compounds;
- e. detecting or measuring translocation of said detectably labeled cellular component involved in the desensitization of a GPCR with said tool, said computer controlling said tool, wherein the detectably labeled cellular component is translocated from the cytosol of a cell to the membrane edge of said cell;
- and
- f. wherein said detecting or measuring translocation indicates an effect on said protein coupled receptor (GPCR) pathway activity.
4 more elements
Dependencies are inferred from the claim text.