Screening for Serotonin Receptor 4 Agonists Using a GPCR-Based Sensor in Yeast

Methods Mol Biol. 2021;2268:77-84. doi: 10.1007/978-1-0716-1221-7_5.ABSTRACTMore 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.PMID:34085262 | DOI:10.1007/978-1-0716-1221-7_5

Source: Mol Biol Cell - June 4, 2021 Category: Molecular Biology Authors: Emily A Yasi Pamela Peralta-Yahya Source Type: research