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Enhancing dimensionality of in-vitro GPCR drug discovery

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As the largest super-family of membrane bound receptor proteins, G Protein-Coupled Receptors (GPCRs) play crucial roles not only in everyday physiology, but many pathologies. Although over a third of FDA approved pharmaceuticals target GPC Rs, many prospective drug candidates fail due to on-target but undesirable effects. Such adverse effects are likely due to the pleiotropic nature of GPCR signalling pathways. Here, the development of a novel biosensor platform for investigating this pleiotropy is outlined and the first iteration presented. The Multi-Response Element GPCR Sensor (MREGS) allows for the simultaneous investigation of five signalling events downstream of GPCR activation using a multiplexed based assay system (Sarrion-Perdigones et al., 2019). This system can now be applied to search for more pathway specific pharmaceuticals with fewer side effects.

This talk is part of the Darwin College Science Seminars series.

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