G protein-coupled receptors (GPCRs), which mediate processes as diverse as olfaction and maintenance of metabolic homeostasis, have become the single most effective class of therapeutic drug targets. As a result, understanding the molecular basis for their activity is of paramount importance. Recent technological advances have made GPCR structural biology increasingly tractable, offering views of these receptors in unprecedented atomic detail. Structural and biophysical data have shown that GPCRs function as complex allosteric machines, communicating ligand-binding events through conformational change. Changes in receptor conformation lead to activation of effector proteins, such as G proteins and arrestins, which are themselves conformational switches. Here, we review how structural biology has illuminated the agonist-induced cascade of conformational changes that culminate in a cellular response to GPCR activation.

中文翻译：

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G蛋白偶联受体信号传导的结构基础。

G蛋白偶联受体（GPCR）介导嗅觉和维持代谢稳态的过程多种多样，已成为治疗药物靶标中最有效的一类。因此，了解其活性的分子基础至关重要。最近的技术进步使GPCR结构生物学变得越来越容易处理，以前所未有的原子细节提供了对这些受体的看法。结构和生物物理数据表明，GPCR充当复杂的变构机器，通过构象变化传达配体结合事件。受体构象的改变导致效应子蛋白如G蛋白和抑制蛋白的活化，它们本身是构象转换。这里，