G蛋白偶联受体（GPCR）在调节内部环境的稳态中发挥着关键作用，并且作为细胞信号传导的主要介质与肿瘤进展密切相关。作为一个多样化、多功能的蛋白质组，G 蛋白信号调节因子 (RGS) 家族被证明参与 GPCR 的细胞转导。越来越多的证据表明 RGS 蛋白失调是一种常见现象，并强调了这些蛋白在人类癌症中的关键作用。此外，它们的差异表达可能成为肿瘤诊断、治疗和预后的潜在生物标志物。最重要的是，目前对RGS家族成员的功能/机制特征和临床应用的系统评价很少。在这篇综述中，我们重点关注 G 蛋白信号调节因子 (RGS) 家族，该家族包括 20 多个家族成员。我们分析了RGS家族成员的分类、基本结构和主要功能。此外，我们还总结了RGS家族各成员在各种人类癌症中的表达变化及其在调节癌细胞增殖、干细胞维持、肿瘤发生和癌症转移中的重要作用。在此基础上，我们概述了一些 RGS 家族成员参与肿瘤进展的分子信号通路。最后讨论了它们在不同类型癌症的精准诊断、预后和治疗中的潜在应用以及目前临床应用可能存在的主要问题。我们的综述提供了对 RGS 在调节肿瘤进展中的作用和潜在机制的全面了解。视频摘要。© 2023。作者。

G protein-coupled receptors (GPCRs) play a key role in regulating the homeostasis of the internal environment and are closely associated with tumour progression as major mediators of cellular signalling. As a diverse and multifunctional group of proteins, the G protein signalling regulator (RGS) family was proven to be involved in the cellular transduction of GPCRs. Growing evidence has revealed dysregulation of RGS proteins as a common phenomenon and highlighted the key roles of these proteins in human cancers. Furthermore, their differential expression may be a potential biomarker for tumour diagnosis, treatment and prognosis. Most importantly, there are few systematic reviews on the functional/mechanistic characteristics and clinical application of RGS family members at present. In this review, we focus on the G-protein signalling regulator (RGS) family, which includes more than 20 family members. We analysed the classification, basic structure, and major functions of the RGS family members. Moreover, we summarize the expression changes of each RGS family member in various human cancers and their important roles in regulating cancer cell proliferation, stem cell maintenance, tumorigenesis and cancer metastasis. On this basis, we outline the molecular signalling pathways in which some RGS family members are involved in tumour progression. Finally, their potential application in the precise diagnosis, prognosis and treatment of different types of cancers and the main possible problems for clinical application at present are discussed. Our review provides a comprehensive understanding of the role and potential mechanisms of RGS in regulating tumour progression. Video Abstract.© 2023. The Author(s).