293/CRE-Luc

The G-protein-coupled receptor (GPCR) superfamily represents one of the most important classes of drug targets in the industry. At present, about 50% of all medicines currently in the market are targeted to GPCRs. GPCRs can be divided into several subfamilies according to the kind of Gα protein to which they couple: There are Gαs-, Gαi-, and Gαq-coupled receptors. Gαs proteins can activate adenyl cyclase and increase the intracellular concentration of cAMP. At GenScript, we employ both 3xCRE element and firefly luciferase as reporters to establish host cell lines that can be used for research involving GPCRs, particularly Gs-coupled GPCRs. This cell line demonstrates an approximately 50-fold dynamic range in the luciferase assay, providing a good screening window that is suitable for screening GPCR agonists and antagonists.