FRAGMENT COMPLEMENTATION ASSAYS FOR G-PROTEIN-COUPLED RECEPTORS AND THEIR SIGNALING PATHWAYS

摘要

This invention relates generally to the fields of biology, molecular biology, chemistry and biochemistry. The invention is directed to a large number of novel assays for G-protein-coupled receptors (GPCRs) and their signaling pathways. Methods are described for constructing such assays for one or more steps in a GPCR pathway. The invention can be used for functional characterization of GPCRs, target validation, de-orphanization of receptors, high-throughput screening, high-content screening, pharmacological profiling, and other drug discovery applications. The assays can be used directly to assess whether a compound library or a biological extract contains an agonist or antagonist of a receptor. Assay compositions are also provided. The development of such assays is shown to be straightforward, providing for a broad, flexible and biologically relevant platform for the discovery of novel drugs and natural ligands that act on GPCRs or their cognate pathways.