Tracey Worzella1, Sarah Shultz1, Jean Shleh2 and Aoife Gallagher3
1Promega Corporation, 2800 Woods Hollow Rd. Madison, WI 53711
2Labcyte Inc., Sunnyvale, CA 94089; 3Deerac Fluidics, Dublin, Ireland
GPCRs are popular targets in drug discovery, and a well designed assay can speed up the discovery of novel drug candidates.The Promega cAMP-Glo™ Assay monitors cAMP production in cells in response to the effect of an agonist or test compound on GPCRs. The assay is based on the principle that cyclic AMP (cAMP) stimulates protein kinase A (PKA) holoenzyme activity, decreasing available ATP and leading to decreased light production in a luciferase reaction. Together with the Labcyte® Echo™ 555 acoustic liquid handler and the Deerac Fluidics™ Equator™ HTS reagent dispenser, compounds can be screened in 1536-well format for effects on GPCRs. Implementing a high-throughput miniaturized GPCR assay as demonstrated in this poster allows cost-effective screening to identify lead modulators of GPCR signaling.