[App Note] Discovery of Novel G-Protein or Arrestin-Biased Ligands Using a Suite of GPCR Signaling Platforms
As more is learned about the intricacies of GPCR signaling, the harder it becomes to accurately describe ligand activity using a single functional readout. This creates the need for a comprehensive suite of naturally coupled cell-based assays that allows quantitative examination of multiple signaling pathways in parallel using the same robust, reliable and high-throughput screening friendly format. DiscoveRx® has developed an industry leading menu of functional assays designed to detect GPCR signaling through second messenger activation, Arrestin binding and receptor internalization. Access to the same target in multiple readouts provides a unique opportunity to identify novel biased ligands that selectively target different aspects of GPCR activation in hopes of developing new and improved drugs with greater therapeutic benefit.