| 摘要 |
<p>Simple, rapid, high-throughput functional bioassays for identifying agents that act as either agonists or antagonists of G-protein coupled receptors (GPCRs) are disclosed. In the methods of the invention, a test composition is contacted with an indicator cell expressing a GPCR and at least one parameter of cellular metabolism of the indicator cells is measured to identify a test compound(s) in the test composition as a receptor agonist or antagonist. The assays can be used to screen libraries of test compounds to identify therapeutically useful agonists or antagonists of GPCRs involved in disease conditions. The assays can also be used to identify ligands of 'orphan' GPCRs whose natural ligands are unknown. Methods of generating indicator cells expressing GPCRs, and isolated populations of such indicator cells, are also disclosed.</p> |
