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

调节 G 蛋白偶联受体介导的抑制蛋白复合物的时间和空间组装的因素

• 批准号: nhmrc : 404087
• 负责人: A/Pr Kevin Pfleger
• 金额: $ 31.52万
• 依托单位: The University of Western Australia
• 依托单位国家: 澳大利亚
• 项目类别: NHMRC Project Grants
• 财政年份: 2006
• 资助国家: 澳大利亚
• 起止时间: 2006-01-01 至 2008-12-31
• 项目状态: 已结题
• 来源: https://researchdata.edu.au/factors-regulating-temporal-arrestin-complexes/101015
• 关键词: Factors; regulating; temporal; spatial; assembly

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.

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分子，例如激素，其作用导致特定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。G蛋白偶联受体和激活它们的分子在人体内提供细胞之间以及器官之间的通信的基本功能。它们是神经信号传递和激素调节身体功能的主要机制。因此，它们是药物的一个重要目标，高达50%的伦理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至关重要，但了解此类反应如何关闭也至关重要。Arrestins是细胞内的蛋白质，与G蛋白偶联受体相互作用以“逮捕”它们的信号传导。它们使细胞对持续刺激脱敏，但也使细胞对未来的单独信号重新敏感。最近，它们还被证明通过与其他细胞蛋白相互作用来提供改变细胞活性的替代机制。一旦G蛋白偶联受体被激活，这些相互作用大大增加了细胞可以响应的潜在方式。如果我们要充分利用这个重要受体家族的巨大治疗潜力，了解由此产生的复杂性是至关重要的。