Gi, Gs, and Gq-Coupled GPCR Screening Assay using Protein-Protein Interactions and EFC Technology
30 May 2007
GPCR targets can be addressed with a variety of technologies and they are increasingly being evaluated with multiple different assay approaches. DiscoveRx has validated over 60 GPCR targets (Gi, Gs, Gq, Type A & Type B) in a novel generic cell-based assay format utilizing protein-protein interaction between the GPCR C-terminus and ß-arrestin2. Unlike reporter gene assays or imaging approaches, this assay provides direct readout between the GPCR of interest and ß-arrestin. It can be detected as soon as 30 seconds after compound treatment. This approach offers a unique enzyme amplification step during signal generation, resulting in very robust performance metrics and S:B ratios that can exceed 70-fold, which has proven particularly effective in addressing certain difficult GPCR and Gi-coupled receptors in general. This poster demonstrates the application of EFC technology to a protein-protein interaction assay which monitors ß-arrestin binding to activated GPCRs.