β-arrestin2 是抑制蛋白家族的成员，介导大多数 G 蛋白偶联受体 (GPCR) 的脱敏和内化，并在信号通路中充当支架蛋白。此前的研究表明，β-arrestin2在恶性肿瘤、纤维化疾病、心血管疾病和代谢疾病中表达失调，提示其病理作用。转录和转录后修饰可影响 β-arrestin2 的表达。此外，磷酸化、泛素化、SUMO化和S-亚硝基化等翻译后修饰会影响β-arrestin2的细胞定位及其与下游信号分子的相互作用，从而进一步调节β-arrestin2的活性。本文综述了β-arrestin2的结构和功能，并揭示了β-arrestin2在多个层面上的调控机制。此外，还对近期β-arrestin2在一些重大疾病中的作用及其治疗前景的研究进行了讨论，为针对β-arrestin2的药物开发提供参考。© 2024 英国药理学会。

β-arrestin2, a member of the arrestin family, mediates the desensitization and internalization of most G protein-coupled receptors (GPCRs) and functions as a scaffold protein in signalling pathways. Previous studies have demonstrated that β-arrestin2 expression is dysregulated in malignant tumours, fibrotic diseases, cardiovascular diseases and metabolic diseases, suggesting its pathological roles. Transcription and post-transcriptional modifications can affect the expression of β-arrestin2. Furthermore, post-translational modifications, such as phosphorylation, ubiquitination, SUMOylation and S-nitrosylation affect the cellular localization of β-arrestin2 and its interaction with downstream signalling molecules, which further regulate the activity of β-arrestin2. This review summarizes the structure and function of β-arrestin2 and reveals the mechanisms involved in the regulation of β-arrestin2 at multiple levels. Additionally, recent studies on the role of β-arrestin2 in some major diseases and its therapeutic prospects have been discussed to provide a reference for the development of drugs targeting β-arrestin2.© 2024 British Pharmacological Society.