School of Chemistry and Biochemistry, Georgia Institute of Technology, Atlanta, GA, USA.
School of Chemical and Biomolecular Engineering, Georgia Institute of Technology, Atlanta, GA, USA.
Methods Mol Biol. 2021;2268:77-84. doi: 10.1007/978-1-0716-1221-7_5.
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-HTR). Serotonin receptor 4 agonists are used for the treatment of irritable bowel syndrome with constipation. Specifically, the HTR-based screen couples activation of 5-HTR on the yeast cell surface to luciferase reporter expression. The HTR-based screen has a throughput of one compound per second allowing the screening of more than a thousand compounds per day.
超过 30%的药物都以 G 蛋白偶联受体（GPCR）为靶点。在这里，我们在酵母中展示了一种基于 GPCR 的筛选方法，以鉴定人类血清素受体 4（5-HTR）的配体。血清素受体 4 激动剂用于治疗便秘型肠易激综合征。具体来说，基于 HTR 的筛选将酵母细胞表面上 5-HTR 的激活与荧光素酶报告基因表达偶联。基于 HTR 的筛选方法的通量为每秒一种化合物，允许每天筛选超过一千种化合物。
