G protein-coupled receptors (GPCRs) have been proven to be the largest
family of druggable targets in the human genome. Given the importance of GPCRs as
drug targets and the de-orphanization of novel targets, GPCRs are likely to remain the
frequent targets of many drug discovery programs. Traditionally, molecular assays
dominate in the process of GPCR drug discovery and development. With recent
advances in instrumentation and pathway deconvolution of GPCR ligand-induced
biosensor signatures, label-free biosensor-enabled cell-based assays have become a very
active area for GPCR screening. This article reviews the principles, current status and
future directions of leading label-free technology platforms for GPCR drug discovery.
Dynamic mass redistribution, electrical biosensor, G protein-coupled
receptor, high throughput screening, impedance, ligand-directed functional
selectivity, optical biosensor, resonant waveguide grating biosensor.
Biochemical Technologies, Science and Technology Division, Corning Incorporated, Sullivan Park, Corning, NY 14831, USA.