G protein-coupled receptors (GPCRs) make up a major family of cell surface receptors which mediate intercellular communication and GPCRs are a source of "druggable" targets. With the increasing popularity of functional assays for high-throughput screening, an increasing need arises for robust second messenger assays that reflect GPCR activation and that are readily amenable for miniaturization. GPCRs modulate adenylyl cyclase activity upon agonist stimulation and, consequently, cellular cyclic adenosine monophosphate (cAMP) that acts on ion channels, kinases and cell metabolism.
DiscoverX' HitHunter® cAMP XS+ is targeted to enhance performance and usability. Here, we describe a cAMP assay based on the enzyme fragmentation complementation of §-galactosidase.
Excellent results were achieved on the PHERAstar® reader which is designed to read all leading HTS detection modes in all formats up to 1536. The high degree of sensitivity, easy-to-use software, robust hardware, and optimized detection systems make the PHERAstar ideal for high throughput GPCR analyses.