Functional assays for screening GPCR targets.

Authors: Thomsen W, Frazer J, Unett D.
Publisher/Year: Curr Opin Biotechnol. 2005 Dec;16(6):655-65. Epub 2005 Oct 28.
Pub Med ID/Journal ID: PMID: 16257523


G-protein-coupled receptors (GPCRs) are valuable molecular targets for drug discovery. An important aspect of the early drug discovery process is the design and implementation of high-throughput GPCR functional assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates. Several functional assay kits based on fluorescence and/or chemiluminescence detection are commercially available for convenient screen development, each having advantages and disadvantages. In addition, new GPCR biosensors and high-content imaging technologies have recently been developed that hold promise for the development of functional GPCR screens in living cells.