Protocol

G Protein-Coupled Receptors in Drug Discovery

Volume 552 of the series Methods in Molecular Biology pp 239-252

Date:

Resonant Waveguide Grating Biosensor for Whole-Cell GPCR Assays

  • Ye FangAffiliated withBiochemical Technologies, Science and Technology Division, Corning Incorporated
  • , Ann M. FerrieAffiliated withBiochemical Technologies, Science and Technology Division, Corning Incorporated
  • , Elizabeth TranAffiliated withBiochemical Technologies, Science and Technology Division, Corning Incorporated

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Summary

Current drug discovery campaigns for G protein-coupled receptors (GPCRs) heavily rely on assay technologies that use artificial cell systems tailored to a point-of-contact readout and as a consequence are mostly pathway biased. Recently, we have developed label-free optical biosensor cellular assays that are capable of examining systems cell biology of endogenous receptors and systems cell pharmacology of GPCR ligands in both physiologically and disease relevant environments. We have shown that these biosensor assays enable high-throughput screening of pathway-biased ligands acting on endogenous β2-adrenergic receptor in cells. These biosensor cellular assays hold the potential to reduce attrition rates in drug discovery and development process.

Key words

G protein-coupled receptor Optical biosensor Resonant waveguide grating biosensor Dynamic mass redistribution Ligand-directed functional selectivity