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More than 30% of all pharmaceuticals target G-protein-coupled receptors (GPCRs). Here, we present a GPCR-based screen in yeast to identify ligands for human serotonin receptor 4 (5-HTR4). Serotonin receptor 4 agonists are used for the treatment of irritable bowel syndrome with constipation. Specifically, the HTR4-based screen couples activation of 5-HTR4 on the yeast cell surface to luciferase reporter expression. The HTR4-based screen has a throughput of one compound per second allowing the screening of more than a thousand compounds per day.


Emily A Yasi, Pamela Peralta-Yahya. Screening for Serotonin Receptor 4 Agonists Using a GPCR-Based Sensor in Yeast. Methods in molecular biology (Clifton, N.J.). 2021;2268:77-84

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PMID: 34085262

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