Thomsen William, Frazer John, Unett David
Arena Pharmaceuticals Inc., San Diego, California 92121, USA.
Curr Opin Biotechnol. 2005 Dec;16(6):655-65. doi: 10.1016/j.copbio.2005.10.008. Epub 2005 Oct 28.
G-protein-coupled receptors (GPCRs) are valuable molecular targets for drug discovery. An important aspect of the early drug discovery process is the design and implementation of high-throughput GPCR functional assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates. Several functional assay kits based on fluorescence and/or chemiluminescence detection are commercially available for convenient screen development, each having advantages and disadvantages. In addition, new GPCR biosensors and high-content imaging technologies have recently been developed that hold promise for the development of functional GPCR screens in living cells.
G蛋白偶联受体（GPCRs）是药物研发中很有价值的分子靶点。早期药物研发过程的一个重要方面是高通量GPCR功能测定法的设计与实施，这种方法能以经济高效的方式筛选大型化合物文库，以识别新的候选药物。有几种基于荧光和/或化学发光检测的功能测定试剂盒可供商业使用，便于开发筛选方法，每种试剂盒都有其优缺点。此外，最近还开发了新的GPCR生物传感器和高内涵成像技术，有望用于活细胞中功能性GPCR筛选的开发。
