Tollin Gordon, Salamon Zdzislaw, Hruby Victor J
Department of Biochemistry and Molecular Biophysics, University of Arizona, Tucson, AZ 85721, USA.
Trends Pharmacol Sci. 2003 Dec;24(12):655-9. doi: 10.1016/j.tips.2003.10.010.
Plasmon-waveguide resonance (PWR) spectroscopy can be applied to integral membrane proteins incorporated into a supported lipid bilayer without the need for labeling. With high sensitivity and wide dynamic range, this technique can be used to characterize the kinetics and thermodynamics of conformational events associated with the binding of ligands to G-protein-coupled receptors (GPCRs), and to directly examine the interactions of GPCRs with G proteins and other downstream effectors in signal transduction. This allows an easy distinction to be made between agonists, antagonists and inverse agonists, and provides a powerful new tool for studying membrane signaling and for drug development.
表面等离子体波导共振(PWR)光谱可应用于整合到支撑脂质双分子层中的完整膜蛋白,无需进行标记。该技术具有高灵敏度和宽动态范围,可用于表征与配体与G蛋白偶联受体(GPCR)结合相关的构象事件的动力学和热力学,并直接检测GPCR在信号转导中与G蛋白和其他下游效应器的相互作用。这使得能够轻松区分激动剂、拮抗剂和反向激动剂,并为研究膜信号传导和药物开发提供了一个强大的新工具。