Mustafa Sanam, Pfleger Kevin D G
Laboratory for Molecular Endocrinology-GPCRs, Western Australian Institute for Medical Research (WAIMR) and Centre for Medical Research, University of Western Australia, Nedlands, Western Australia, Australia.
J Lab Autom. 2011 Aug;16(4):285-91. doi: 10.1016/j.jala.2011.03.002. Epub 2011 May 31.
Traditionally, G protein-coupled receptors (GPCRs) were thought to function as monomeric units activating linear signaling pathways to reach a single functional response. However, it is now recognized that GPCRs can exist as higher order structures, such as homomers or heteromers. The potential for unique pharmacology attributed to these GPCR complexes has opened up the possibility of a new class of targets that can be exploited for drug discovery. In this innovation brief, a novel technology developed to identify and profile GPCR heteromers and their ligands will be reviewed.
传统上，G蛋白偶联受体（GPCRs）被认为作为单体单元发挥作用，激活线性信号通路以实现单一功能反应。然而，现在人们认识到GPCRs可以以更高阶结构存在，例如同源二聚体或异源二聚体。这些GPCR复合物具有独特药理学特性，这为一类可用于药物发现的新靶点开辟了可能性。在本创新简报中，将对一种用于识别和分析GPCR异源二聚体及其配体的新技术进行综述。
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