G 蛋白偶联受体（GPCR）的重构和标记用于溶液核磁共振（NMR）研究跨膜信号转导的结构基础。
G Protein-coupled Receptor (GPCR) Reconstitution and Labeling for Solution Nuclear Magnetic Resonance (NMR) Studies of the Structural Basis of Transmembrane Signaling.
机构信息
iHuman Institute, ShanghaiTech University, Shanghai 201210, China.
School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China.
出版信息
Molecules. 2022 Apr 20;27(9):2658. doi: 10.3390/molecules27092658.
G protein-coupled receptors (GPCRs) are a large membrane protein family found in higher organisms, including the human body. GPCRs mediate cellular responses to diverse extracellular stimuli and thus control key physiological functions, which makes them important targets for drug design. Signaling by GPCRs is related to the structure and dynamics of these proteins, which are modulated by extrinsic ligands as well as by intracellular binding partners such as G proteins and arrestins. Here, we review some basics of using nuclear magnetic resonance (NMR) spectroscopy in solution for the characterization of GPCR conformations and intermolecular interactions that relate to transmembrane signaling.
G 蛋白偶联受体（GPCRs）是一种在高等生物中发现的大型膜蛋白家族，包括人体。GPCR 介导细胞对各种细胞外刺激的反应，从而控制关键的生理功能，这使得它们成为药物设计的重要靶点。GPCR 的信号转导与这些蛋白质的结构和动力学有关，这些结构和动力学受外在配体以及细胞内结合伴侣（如 G 蛋白和阻滞蛋白）的调节。在这里，我们回顾了一些使用核磁共振（NMR）光谱在溶液中对 GPCR 构象和与跨膜信号转导相关的分子间相互作用进行表征的基础知识。
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