Factors regulating the temporal and spatial assembly of G-protein coupled receptor-mediated arrestin complexes

G蛋白偶联受体是存在于人体大多数细胞表面的蛋白质。它们识别并结合特定的分子，如荷尔蒙，这些分子的行为导致特定的信号被传递到细胞中。这种信号改变了细胞的功能，因此它在类型和持续时间上都是适当的，这是至关重要的。G蛋白偶联受体和激活它们的分子在人体内为细胞之间的沟通提供了基本的功能，从而也就是器官之间的沟通。它们是神经信号传递和荷尔蒙调节身体功能的主要机制。因此，它们是制药的重要目标，高达50%的符合道德的药物和许多滥用药物对它们起作用。了解这些受体在接收到适当的信号后如何改变细胞功能是至关重要的，但了解这些反应是如何关闭的也是至关重要的。阻滞素是细胞内的一种蛋白质，它与G蛋白偶联受体相互作用，‘阻止’它们的信号传递。它们使细胞对持续的刺激不敏感，但也能使细胞对未来的单独信号做出反应。最近，它们还被证明提供了通过与其他细胞蛋白相互作用来改变细胞活动的替代机制。一旦G蛋白偶联受体被激活，这些相互作用极大地增加了细胞做出反应的潜在方式。如果我们要充分开发这一重要受体家族的巨大治疗潜力，了解由此产生的复杂性是必不可少的。

G-protein coupled receptors are proteins that are present at the surface of most cells in the human body. They recognise and bind to specific molecules, such as hormones, the act of which results in a specific signal being transmitted into the cell. This signal alters the function of the cell and so it is critical that it is appropriate, both in type and duration. G-protein coupled receptors and the molecules that activate them provide an essential function within the human body for communicating between cells, and consequently between organs. They are a major mechanism by which nerve signals are transmitted and hormones regulate bodily functions. They are therefore an important target for pharmaceuticals, with up to 50% of ethical drugs and many drugs of abuse acting upon them. It is critical to understand how these receptors alter cellular function once they receive an appropriate signal, but it is also essential to know how such responses are switched off. Arrestins are proteins within cells that interact with G-protein coupled receptors to 'arrest' their signalling. They desensitise the cell to continuous stimulation, but also act to resensitise the cell to respond to future, separate signals. Recently, they have also been shown to provide alternative mechanisms of altering cellular activity by interacting with other cellular proteins. These interactions greatly increase the potential ways in which a cell can respond once a G-protein coupled receptor is activated. Understanding the resulting complexity is essential if we are to fully exploit the vast therapeutic potential of this important receptor family.