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• W151128456 abstract "Advances in instrumentation, informatics, and biology now allow routine screening of chemical compounds for their therapeutic properties using cell-based assays. Whole-cell assays have emerged as a viable alternative to traditional drug-screening assays that employ cell components and often use radioactivity, with its inherent waste disposal and safety issues. These new assays employ fluorescent and luminescent markers to track the effects of drug candidates on cell functions mediated through receptors, ion channels, enzymes, and intracellular signaling pathways. Additionally, these assays can measure changes in cell secretions, cell surface markers, chemotaxis, cell viability, and metabolism. There are several advantages to using whole cells over isolated cell components such as membrane fractions. Primarily, the protein target is in a more natural conformation than in a membrane or cytoplasm extract and includes the entire apparatus of cell signal transduction. Second, cell-based assays allow assessment of a compound's agonist, partial agonist, or antagonist activities at a target, not just its binding affinity. Third, these assays can simultaneously screen a drug against several known targets and measure their multiple cellular responses. Lastly, one can use cellular assays to explore previously unidentified targets or pathways, allowing for the discovery of new cell response mechanisms. This chapter is introduced with a discussion of the different sources of cells that can be employed in cell-based assays. Then, in accordance with the particular nature of the cellular response, we discuss common techniques that can be used to quantify them best. Finally, examples of practical applications covering several drug development targets are discussed in detail, including ion channels, G protein-coupled receptors (GPCRs), multiplex assays, and cell toxicity. While this chapter makes an effort to cover the broad spectrum of cell-based assays, its focus is on the more popular methods and techniques used for drug screening." @default.
• W151128456 created "2016-06-24" @default.
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• W151128456 date "2007-01-01" @default.
• W151128456 modified "2023-09-23" @default.
• W151128456 title "Cell-Based Screening Assays" @default.
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• W151128456 doi "https://doi.org/10.1016/b0-08-045044-x/00102-4" @default.
• W151128456 hasPublicationYear "2007" @default.
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