Regulating the regulators: Epigenetic, transcriptional, and post-translational regulation of RGS proteins.
Regulating the regulators: Epigenetic, transcriptional, and post-translational regulation of RGS proteins.
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DOI：
10.1016/j.cellsig.2017.10.007
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发表时间：
2018-01
影响因子：
4.8
通讯作者：
Hooks SB
中科院分区：
文献类型：
--
作者：
Alqinyah M;Hooks SB
G蛋白信号传导调节因子（Regulators of G protein signaling，RGS）是一类典型的加速G蛋白内在GT3活性的蛋白质家族，其导致异源三聚体G蛋白的加速失活和G蛋白偶联受体信号传导的抑制。RGS蛋白在重要的细胞过程中起主要作用，并且RGS蛋白表达的失调涉及多种疾病，包括癌症、心血管和神经退行性疾病。RGS蛋白的表达是高度动态的，并受表观遗传、转录和翻译后机制的调节。本文综述了RGS蛋白在疾病状态下表达失调的研究，并介绍了调节RGS蛋白表达的药物的例子。此外，本文还详细讨论了RGS蛋白表达调控的转录和转录后机制，并进一步评估了靶向这些机制的治疗潜力。了解控制RGS蛋白表达的分子机制对于开发通过调节RGS蛋白表达间接调节G蛋白信号传导的治疗剂是必不可少的。
Regulators of G protein signalling (RGS) are a family of proteins classically known to accelerate the intrinsic GTPase activity of G proteins, which results in accelerated inactivation of heterotrimeric G proteins and inhibition of G protein coupled receptor signaling. RGS proteins play major roles in essential cellular processes, and dysregulation of RGS protein expression is implicated in multiple diseases, including cancer, cardiovascular and neurodegenerative diseases. The expression of RGS proteins is highly dynamic and is regulated by epigenetic, transcriptional and post-translational mechanisms. This review summarizes studies that report dysregulation of RGS protein expression in disease states, and presents examples of drugs that regulate RGS protein expression. Additionally, this review discusses, in detail, the transcriptional and post-transcriptional mechanisms regulating RGS protein expression, and further assesses the therapeutic potential of targeting these mechanisms. Understanding the molecular mechanisms controlling the expression of RGS proteins is essential for the development of therapeutics that indirectly modulate G protein signalling by regulating expression of RGS proteins.
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