Reports Outline Pharmacology Study Results from
Our news journalists obtained a quote from the research, "High-content screening is particularly well suited for GPCR drug discovery given the ability to image and quantify changes in multiple cellular parameters, to resolve subcellular structures, and to monitor events within a physiologically relevant environment. Focusing on the sphingosine-1-phosphate (S1P1) receptor, we evaluated the utility of high-content approaches in hit identification efforts by developing and applying assays to monitor beta-arrestin translocation, GPCR internalization, and GPCR recycling kinetics. Using these approaches in combination with more traditional GPCR screening assays, we identified compounds whose unique pharmacological profiles would have gone unnoticed if using a single platform. In addition, we identified a compound that induces an atypical pattern of beta-arrestin translocation and GPCR recycling kinetics."
According to the news editors, the research concluded: "Our results highlight the value of high-content imaging in GPCR drug discovery efforts and emphasize the value of a multiassay approach to study pharmacological properties of compounds of interest."
For more information on this research see: Integrating High-Content Analysis into a Multiplexed Screening Approach to Identify and Characterize GPCR Agonists.
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