The internalization of G protein-coupled receptors (GPCRs) is an important mechanism regulating the signal strength and limiting the opportunity of receptor activation. Based on the importance of GPCRs, the detailed knowledge about the regulation of signal transduction is crucial. Here, current knowledge about the agonist-induced, arrestin-dependent internalization process of rhodopsin-like GPCRs is reviewed. Arrestins are conserved molecules that act as key players within the internalization process of many GPCRs. Based on highly conserved structural characteristics within the rhodopsin-like GPCRs, the identification of arrestin interaction sites in model systems can be compared and used for the investigation of internalization processes of other receptors. The increasing understanding of this essential regulation mechanism of receptors can be used for drug development targeting rhodopsin-like GPCRs. Here, we focus on the neuropeptide Y receptor family, as these receptors transmit various physiological processes such as food intake, energy homeostasis, and regulation of emotional behavior, and are further involved in pathophysiological processes like cancer, obesity and mood disorders. Hence, this receptor family represents an interesting target for the development of novel therapeutics requiring the understanding of the regulatory mechanisms influencing receptor mediated signaling.

中文翻译：

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视紫红质样 G 蛋白偶联受体的抑制素依赖性内化

G蛋白偶联受体（GPCRs）的内化是调节信号强度和限制受体激活机会的重要机制。基于 GPCR 的重要性，有关信号转导调控的详细知识至关重要。在这里，回顾了目前关于视紫红质样 GPCR 的激动剂诱导的抑制素依赖性内化过程的知识。Arrestins 是保守分子，在许多 GPCR 的内化过程中充当关键角色。基于视紫红质样 GPCR 中高度保守的结构特征，模型系统中抑制蛋白相互作用位点的鉴定可以进行比较，并用于研究其他受体的内化过程。对受体的这种基本调节机制的日益了解可用于靶向视紫红质样 GPCR 的药物开发。在这里，我们专注于神经肽 Y 受体家族，因为这些受体传递各种生理过程，如食物摄入、能量稳态和情绪行为的调节，并进一步参与癌症、肥胖和情绪障碍等病理生理过程。因此，该受体家族代表了开发新疗法的一个有趣目标，需要了解影响受体介导的信号传导的调节机制。和情绪行为的调节，并进一步参与癌症、肥胖和情绪障碍等病理生理过程。因此，该受体家族代表了开发新疗法的一个有趣目标，需要了解影响受体介导的信号传导的调节机制。和情绪行为的调节，并进一步参与癌症、肥胖和情绪障碍等病理生理过程。因此，该受体家族代表了开发新疗法的一个有趣目标，需要了解影响受体介导的信号传导的调节机制。