Functional assays for screening GPCR targets.
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.
Thomsen
William
W
Arena Pharmaceuticals Inc., San Diego, California 92121, USA. bthomsen@arenapharm.com
Frazer
John
J
Unett
David
D
D000818:Animals; D001681:Biological Assay / Q000379:methods / Q000639:trends; D015374:Biosensing Techniques / Q000379:methods / Q000639:trends; D015195:Drug Design; D006801:Humans; D008163:Luminescent Measurements / Q000379:methods / Q000639:trends; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
D043562:Receptors, G-Protein-Coupled