Hattori Mitsuru, Ozawa Takeaki
Department of Chemistry, School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan.
Methods Mol Biol. 2016;1461:195-202. doi: 10.1007/978-1-4939-3813-1_16.
G protein-coupled receptors (GPCRs) are notable targets of basic therapeutics. Many screening methods have been established to identify novel agents for GPCR signaling in a high-throughput manner. However, information related to the temporal reaction of GPCR with specific ligands remains poor. We recently developed a bioluminescence method for the quantitative detection of the interaction between GPCR and β-arrestin using split luciferase complementation. To monitor time-course variation of the interactions, a new imaging system contributes to the accurate evaluation of drugs for GPCRs in a high-throughput manner.
G蛋白偶联受体（GPCRs）是基础治疗学的重要靶点。已经建立了许多筛选方法，以高通量方式鉴定用于GPCR信号传导的新型药物。然而，与GPCR与特定配体的瞬时反应相关的信息仍然匮乏。我们最近开发了一种生物发光方法，用于使用分裂荧光素酶互补技术定量检测GPCR与β-抑制蛋白之间的相互作用。为了监测相互作用的时间进程变化，一种新的成像系统有助于以高通量方式准确评估用于GPCR的药物。
