2024年12月25日 · GRK2 (G Protein-Coupled Receptor Kinase 2) is a Protein Coding gene. Diseases associated with GRK2 include Short-Rib Thoracic Dysplasia 1 With Or Without Polydactyly and Asphyxiating Thoracic Dystrophy .

G-protein-coupled receptor kinase 2 (GRK2) is an enzyme that in humans is encoded by the ADRBK1 gene. [5] GRK2 was initially called Beta-adrenergic receptor kinase (βARK or βARK1), and is a member of the G protein-coupled receptor kinase subfamily of the Ser/Thr protein kinases that is most highly similar to GRK3 (βARK2).

2023年8月2日 · Structural studies on the complex containing G-protein-coupled receptor kinase 2 (GRK2), neurotensin receptor 1 (NTSR1), Gαq and the arrestin-biased ligand SBI-553 provide insights into these ...

2025年2月8日 · GRK2-phosphorylated recombinant ribosomal protein P2 reconstitutes translational activity of 60S ribosomal subunits and represents a potential novel signaling pathway responsible for P2 phosphorylation. GRK2 is potential marker for organ injury and survival after cardiopulmonary bypass

2016年10月27日 · G-protein-coupled receptor kinase 2 (GRK2) is a G-protein-coupled receptor kinase that is ubiquitously expressed in many tissues and regulates various intracellular mechanisms. The up- or down-regulation of GRK2 correlates with several pathological disorders. GRK2 plays an important role in the main …

2012年3月1日 · In this review, we discuss traditional and newly discovered roles of GRK2 in receptor internalization and signaling as well as its impact on non-receptor substrates. We also discuss novel exciting roles of GRK2 in the regulation of dopamine receptor signaling and in the activation and trafficking of the atypical GPCR, Smoothened (Smo).

2023年8月2日，中国科学院上海药物研究所徐华强研究员、段佳研究员和杨德华研究员共同在Nature杂志上发表了最新研究成果“GPCR activation and GRK2 assembly by a biased intracellular agonist”，在国际上报道了第一个高分辨率GPCR—— 神经降压素受体 （neurotensin …

2009年12月28日 · G protein–coupled receptor kinase 2 (GRK2) plays a central role in G protein–coupled receptor regulation. Recent research is uncovering its involvement in additional cellular functions, but the potential role of GRK2 in the cell cycle has not been addressed.

2022年6月1日 · In addition to the inhibitory effect of GRK2/arrestins in GPCR signal transduction, emerging evidence suggests that GRK2 and β-arrestins regulate intracellular signaling independently of GPCRs by affecting non-GPCR receptors or by direct interaction with various cellular target molecules involved in signal transduction. β-arrestins can be ...

2019年2月18日 · G protein-coupled receptor kinase 2 (GRK2) is a central signaling node involved in the modulation of many G protein-coupled receptors (GPCRs) and also displaying regulatory functions in other cell signaling routes.

2019年8月20日 · Accumulating evidence indicates that G protein-coupled receptor kinase 2 (GRK2) is a versatile protein that acts as a signaling hub by modulating G protein-coupled receptor (GPCR) signaling and also via phosphorylation or scaffolding interactions with an extensive number of non-GPCR cellular partners.

In this review, we discuss traditional and newly discovered roles of GRK2 in receptor internalization and signaling as well as its impact on non-receptor substrates. We also discuss novel exciting roles of GRK2 in the regulation of dopamine receptor signaling and in the activation and trafficking of the atypical GPCR, Smoothened (Smo).

2024年7月3日 · G protein-coupled receptors (GPCRs) are mainly regulated by GPCR kinase (GRK) phosphorylation and subsequent β-arrestin recruitment. The ubiquitously expressed GRKs are classified into cytosolic...

2017年1月1日 · GRK2 is a multidomain protein consisting of two regulator of G protein signaling (RGS) homology domains (RH; colored in red), a highly conserved serine/threonine kinase catalytic domain (colored in yellow), and a pleckstrin homology domain (PH; colored in turquoise).

Down-regulation and desensitization of β-adrenergic receptors (β-AR) caused by G-protein-coupled receptor (GPCR) kinase 2 (GRK2) are prominent features of HF.

In this review, we discuss traditional and newly discovered roles of GRK2 in receptor internalization and signaling as well as its impact on non-receptor substrates. We also discuss novel exciting roles of GRK2 in the regulation of dopamine receptor signaling and in the activation and trafficking of the atypical GPCR, Smoothened (Smo).

该基因编码 G 蛋白偶联受体激酶蛋白家族的成员。 编码的蛋白质磷酸化 β-肾上腺素能受体以及广泛的其他底物，包括非 GPCR 细胞表面受体，以及细胞骨架、线粒体和转录因子蛋白。 来自啮齿动物模型的数据支持该基因在胚胎发育、心脏功能和新陈代谢中的作用。 已在患有心力衰竭和阿尔茨海默氏病的人类患者中观察到该基因表达升高。 [RefSeq 提供，2017 年 9 月] This gene encodes a member of the G protein-coupled receptor kinase family of proteins.

GRK2 is a ubiquitous member of the G protein-coupled receptor kinase (GRK) family that appears to play a central, integrative role in signal transduction cascades. GRKs participate together with arrestins in the regulation of G protein-coupled receptors (GPCR), a family of hundreds of membrane prote …

2025年3月7日 · GRK2 with Paxil bound to its active site. Priyanka Naik, CC BY-ND. For example, in 2012, one of my colleagues discovered that the antidepressant Paxil could inhibit GRK2. To build on this ...

GRK2 is a RhoA effector that serves as a RhoA-activated scaffold protein for the ERK MAP kinase cascade. The ability of GRK2 to bind to Raf1, MEK1 and ERK2 is dependent on RhoAGTP binding to the catalytic domain of the kinase.