使用基于 G 蛋白偶联受体的酵母传感器筛选血清素受体 4 激动剂。
Screening for Serotonin Receptor 4 Agonists Using a GPCR-Based Sensor in Yeast.
机构信息
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.
出版信息
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。
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