Department of Molecular and Cellular Physiology, Stanford University School of Medicine, Stanford, CA, USA.
Nat Struct Mol Biol. 2018 Jan;25(1):4-12. doi: 10.1038/s41594-017-0011-7. Epub 2018 Jan 8.
G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering intracellular signaling through coupling with G proteins and arrestins. Recent breakthroughs in the structural determination of GPCRs and GPCR-transducer complexes represent important steps toward deciphering GPCR signal transduction at a molecular level. A full understanding of the molecular basis of GPCR-mediated signaling requires elucidation of the dynamics of receptors and their transducer complexes as well as their energy landscapes and conformational transition rates. Here, we summarize current insights into the structural plasticity of GPCR-G-protein and GPCR-arrestin complexes that underlies the regulation of the receptor's intracellular signaling profile.
G 蛋白偶联受体（GPCRs）通过与 G 蛋白和阻滞蛋白偶联触发细胞内信号转导，传递众多细胞外信号。近年来，GPCR 结构测定和 GPCR 转导复合物的突破性进展代表了在分子水平上破译 GPCR 信号转导的重要步骤。要全面了解 GPCR 介导的信号转导的分子基础，就需要阐明受体及其转导复合物的动力学以及它们的能量景观和构象转变速率。在这里，我们总结了目前对 GPCR-G 蛋白和 GPCR-阻滞蛋白复合物结构可塑性的理解，这种结构可塑性是受体细胞内信号转导谱调节的基础。
