Laboratory of Veterinary Pathology and Platelet Signaling, College of Veterinary Medicine, Chungbuk National University, Cheongju 28644, Korea.
Int J Mol Sci. 2021 Mar 25;22(7):3375. doi: 10.3390/ijms22073375.
G protein-coupled receptor kinases (GRKs) are protein kinases that function in concert with arrestins in the regulation of a diverse class of G protein-coupled receptors (GPCRs) signaling. Although GRKs and arrestins are key participants in the regulation of GPCR cascades, the complex regulatory mechanisms of GRK expression, its alternation, and their function are not thoroughly understood. Several studies together with the work from our lab in recent years have revealed the critical role of these kinases in various physiological and pathophysiological processes, including cardiovascular biology, inflammation and immunity, neurodegeneration, thrombosis, and hemostasis. A comprehensive understanding of the mechanisms underlying functional interactions with multiple receptor proteins and how these interactions take part in the development of various pathobiological processes may give rise to novel diagnostic and therapeutic strategies. In this review, we summarize the current research linking the role of GRKs to various aspects of cell biology, pathology, and therapeutics, with a particular focus on thrombosis and hemostasis.
G 蛋白偶联受体激酶（GRKs）是一类与 arrestin 协同作用的蛋白激酶，在调节多种 G 蛋白偶联受体（GPCR）信号中发挥作用。尽管 GRKs 和 arrestin 是 GPCR 级联调节的关键参与者，但 GRK 表达、其改变及其功能的复杂调节机制尚未完全阐明。近年来，几项研究以及我们实验室的工作揭示了这些激酶在多种生理和病理生理过程中的关键作用，包括心血管生物学、炎症和免疫、神经退行性变、血栓形成和止血。全面了解与多种受体蛋白的功能相互作用的机制，以及这些相互作用如何参与各种病理生物过程的发展，可能会产生新的诊断和治疗策略。在这篇综述中，我们总结了目前将 GRKs 的作用与细胞生物学、病理学和治疗学的各个方面联系起来的研究，特别关注血栓形成和止血。
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