1386-2073/08 $55.00+.00 © 2008 Bentham Science Publishers Ltd. Label-Free Cell-Based Assays for GPCR Screening Ye Fang

Abstract: G protein-coupled receptors (GPCRs) have been proven to be the largest family of druggable targets in the hu-man 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. With recent advances in instrumentation and understand-ing of cellular mechanisms for the signals measured, biosensor-centered label-free cell assay technologies become a very active area for GPCR screening. This article reviews the principles and potential of current label-free cell assay technolo-gies in GPCR drug discovery