G Protein-coupled Receptor (GPCR) Reconstitution and Labeling for Solution Nuclear Magnetic Resonance (NMR) Studies of the Structural Basis of Transmembrane Signaling.

G Protein-coupled Receptor (GPCR) Reconstitution and Labeling for Solution Nuclear Magnetic Resonance (NMR) Studies of the Structural Basis of Transmembrane Signaling.
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G 蛋白偶联受体 (GPCR) 重建和标记,用于跨膜信号传导结构基础的溶液核磁共振 (NMR) 研究

DOI:
10.3390/molecules27092658
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发表时间:
2022-04-20
期刊:
Molecules (Basel, Switzerland)
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其他
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G蛋白偶联受体(GPCR)是在包括人体在内的高等生物中发现的一个大的膜蛋白家族。GPCR介导细胞对多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标。GPCR的信号传导与这些蛋白质的结构和动力学有关,这些蛋白质的结构和动力学受外部配体以及细胞内结合伴侣如G蛋白和抑制蛋白的调节。在这里,我们回顾了一些基本的使用核磁共振(NMR)光谱在溶液中的GPCR构象和分子间相互作用,涉及跨膜信号的表征。
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.
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