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J Recept Signal Transduct Res. 2009;29(3-4):146-53. doi: 10.1080/10799890903064390.

Label-free optical biosensor: a tool for G protein-coupled receptors pharmacology profiling and inverse agonists identification.

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Lead Discovery, Amgen Inc, Thousand Oaks, California 91320, USA.


Current GPCR cell-based assays often rely on the measurement of a loaded fluorescent dye, fluorescently tagged targets, or the expression of a reporter. These manipulations may alter the cellular physiology of the target GPCR, and the measurements may be subject to off-target interference of compounds. Label-free optical biosensor-based technologies that provide a noninvasive methodology to study GPCR activation and signaling have been developed. These technologies enable the evaluation of drug effects on various GPCRs that couple to different signal transduction pathways using only one assay platform. This technology is highly sensitive and detects inverse agonism, therefore providing a convenient tool to study the pharmacology of drugs. Furthermore, its real-time kinetic measurements give researchers additional information about the biological responses induced by the drug. This assay platform when applied in early drug discovery efforts can provide valuable information on the mechanism of action and pharmacology profiles of drug candidates.

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