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  • Title: Functional assays for screening GPCR targets.
    Author: Thomsen W, Frazer J, Unett D.
    Journal: Curr Opin Biotechnol; 2005 Dec; 16(6):655-65. PubMed ID: 16257523.
    Abstract:
    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.
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