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GRK2

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https://www.readbyqxmd.com/read/27895163/g-protein-coupled-receptor-kinase-2-grk2-as-a-potential-modulator-of-the-hallmarks-of-cancer
#1
Laura Nogues, Clara Reglero, Veronica Rivas, Maria Neves, Petronila Penela, Federico Mayor
Malignant features such as sustained proliferation, refractoriness to growth suppressors, resistance to cell death or aberrant motility and metastasis can be triggered by a variety of mutations and signaling adaptations. Signaling nodes can act as cancer-associated factors by cooperating with oncogene-governed pathways or participating in compensatory transduction networks to strengthen tumor properties. G-protein-coupled receptor kinase 2 (GRK2) is arising as one of such nodes. Via its complex network of connections with other cellular proteins, GRK2 contributes to the modulation of basic cellular functions such as cell proliferation, survival or motility, and is involved in metabolic homeostasis, inflammation or angiogenic processes...
November 28, 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27865836/g-protein-coupled-kinase-2-upregulation-causes-%C3%AE%C2%BA-opioid-receptor-desensitization-in-diabetic-heart
#2
Xiyao Chen, Shihao Zhao, Yunlong Xia, Zhenyu Xiong, Yueyang Li, Ling Tao, Fuyang Zhang, Xiaoming Wang
Activation of κ-opioid receptor (KOR) ameliorates myocardial ischemia/reperfusion (I/R) injury; however, cardioprotective effects of KOR stimulation disappear in type 1 diabetic subjects with hyperglycemia. The molecular mechanisms underlying this phenomenon remain unknown. Here we found that KOR expression was obviously downregulated and KOR agonism-induced contractile-regulatory/cardioprotective effects were significantly impaired in hearts isolated from streptozotocin (STZ) injection-induced diabetic mice...
November 16, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27862165/grk2-%C3%AE-arrestin-mediates-arginine-vasopressin-induced-cardiac-fibroblast-proliferation
#3
Yunxuan Chen, Feifei Xu, Lingling Zhang, Xiaojun Wang, Yifan Wang, AnthonyYiu-Ho Woo, Weizhong Zhu
Cardiac fibrosis is a pathological feature commonly foundinheartsexposed to hemodynamic orneurohormonal stress. Elevated levels of arginine vasopressin (AVP) are closely associated with the progression ofheart failure and could be an underlyingcauseof cardiac fibrosis. The aim of this study is to characterize the effect of AVP on neonatal rat cardiac fibroblasts (NRCFs) and to illustrate itssignallingmechanism. The proliferative effect of AVP was assessed by methylthiazolyldiphenyl-tetrazoliumassay and 5-bromo-2'-deoxyuridine (BrdU) incorporation assay, and the amounts of cellular signallingproteins α-smooth muscle actin(α-SMA),matrix metalloproteinase (MMP) 2, MMP9, and phosphorylated ERK1/2 were determined by Western blotting...
November 14, 2016: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/27832814/obesity-induced-cardiac-lipid-accumulation-in-adult-mice-is-modulated-by-g-protein-coupled-receptor-kinase-2-levels
#4
Elisa Lucas, Rocio Vila-Bedmar, Alba C Arcones, Marta Cruces-Sande, Victoria Cachofeiro, Federico Mayor, Cristina Murga
BACKGROUND: The leading cause of death among the obese population is heart failure and stroke prompted by structural and functional changes in the heart. The molecular mechanisms that underlie obesity-related cardiac remodeling are complex, and include hemodynamic and metabolic alterations that ultimately affect the functionality of the myocardium. G protein-coupled receptor kinase 2 (GRK2) is an ubiquitous kinase able to desensitize the active form of several G protein-coupled receptors (GPCR) and is known to play an important role in cardiac GPCR modulation...
November 10, 2016: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/27815373/inhibiting-insulin-mediated-%C3%AE-2ar-activation-prevents-diabetes-associated-cardiac-dysfunction
#5
Qingtong Wang, Yongming Liu, Qin Fu, Bing Xu, Yuan Zhang, Sungjin Kim, Ruensern Tan, Federica Barbagallo, Toni M West, Ethan J Anderson, Wei Wei, E Dale Abel, Yang K Xiang
BACKGROUND: -Type-2 diabetes and obesity independently increases the risk of heart failure via incompletely understood mechanisms. We propose that hyperinsulinemia might promote adverse consequences in hearts of subjects with type-2 diabetes and obesity. METHODS: -High fat diet feeding was used to induce obesity and diabetes in wild type mice or mice lacking β 2-adrenergic receptor (β2AR) or β -arrestin2. Wild type mice fed with high fat diet were treated with β -blocker carvedilol or G-protein receptor kinase 2 (GRK2) inhibitor...
November 4, 2016: Circulation
https://www.readbyqxmd.com/read/27773680/vasopressin-v1a-receptor-mediates-cell-proliferation-through-grk2-egfr-erk1-2-pathway-in-a7r5-cells
#6
Lingling Zhang, Xiaojun Wang, Hong Cao, Yunxuan Chen, Xianfan Chen, Xi Zhao, Feifei Xu, Yifan Wang, Anthony Yiu-Ho Woo, Weizhong Zhu
Abnormal proliferation and hypertrophy of vascular smooth muscle (VSMC), as the main structural component of the vasculature, is an important pathological mechanism of hypertension. Recently, increased levels of arginine vasopressin (AVP) and copeptin, the C-terminal fragment of provasopressin, have been shown to correlate with the development of preeclampsia. AVP targets on the Gq-coupled vasopressin V1A receptor and the Gs-coupled V2 receptor in VSMC and the kidneys to regulate vascular tone and water homeostasis...
October 20, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27720394/g-protein-coupled-receptor-kinase-2-grk2-promotes-breast-tumorigenesis-through-a-hdac6-pin1-axis
#7
Laura Nogués, Clara Reglero, Verónica Rivas, Alicia Salcedo, Vanesa Lafarga, Maria Neves, Paula Ramos, Marta Mendiola, Alberto Berjón, Kostas Stamatakis, Xiao Zhen Zhou, Kun Ping Lu, David Hardisson, Federico Mayor, Petronila Penela
In addition to oncogenic drivers, signaling nodes can critically modulate cancer-related cellular networks to strength tumor hallmarks. We identify G-protein-coupled receptor kinase 2 (GRK2) as a relevant player in breast cancer. GRK2 is up-regulated in breast cancer cell lines, in spontaneous tumors in mice, and in a proportion of invasive ductal carcinoma patients. Increased GRK2 functionality promotes the phosphorylation and activation of the Histone Deacetylase 6 (HDAC6) leading to de-acetylation of the Prolyl Isomerase Pin1, a central modulator of tumor progression, thereby enhancing its stability and functional interaction with key mitotic regulators...
October 1, 2016: EBioMedicine
https://www.readbyqxmd.com/read/27714516/role-of-amino-acid-residues-surrounding-the-phosphorylation-site-in-peptide-substrates-of-g-protein-coupled-receptor-kinase-2-grk2
#8
Daisuke Asai, Masaharu Murata, Riki Toita, Takahito Kawano, Hideki Nakashima, Jeong-Hun Kang
A series of amino acid substitutions was made in a previously identified β-tubulin-derived GRK2 substrate peptide ((404)DEMEFTEAESNMN(416)) to examine the role of amino acid residues surrounding the phosphorylation site. Anionic amino acid residues surrounding the phosphorylation site played an important role in the affinity for GRK2. Compared to the original peptide, a modified peptide (Ac-EEMEFSEAEANMN-NH2) exhibited markedly higher affinity for GRK2, but very low affinity for GRK5, suggesting that it can be a sensitive and selective peptide for GRK2...
October 6, 2016: Amino Acids
https://www.readbyqxmd.com/read/27695334/effects-of-paroxetine-mediated-inhibition-of-grk2-expression-on-depression-and-cardiovascular-function-in-patients-with-myocardial-infarction
#9
Xiuqing Tian, Qing Wang, Rui Guo, Lingling Xu, Qin M Chen, Yinglong Hou
BACKGROUND: Paroxetine is a selective serotonin reuptake inhibitor utilized in the treatment of depression and anxiety disorders. Recent studies have identified paroxetine as a G protein-coupled receptor kinase-2 (GRK2) inhibitor capable of reversing cardiac dysfunction and remodeling in experimental models of acute myocardial infarction (AMI). We determine the clinical importance of paroxetine on cardiac functions in patients having AMI with depression (AMID) in comparison with fluoxetine, an unrelated selective serotonin reuptake inhibitor that does not inhibit GRK2...
2016: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/27664063/grk2-targeted-knock-down-results-in-spontaneous-hypertension-and-altered-vascular-gpcr-signaling
#10
Elena Tutunea-Fatan, Fabiana A Caetano, Robert Gros, Stephen S G Ferguson
No abstract text is available yet for this article.
September 23, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27650728/easy-to-use-strategy-for-reference-gene-selection-in-quantitative-real-time-pcr-experiments
#11
Stefanie Klenke, Kristina Renckhoff, Andrea Engler, Jürgen Peters, Ulrich H Frey
Real-time PCR is an indispensable technique for mRNA expression analysis but conclusions depend on appropriate reference gene selection. However, while reference gene selection has been a topic of publications, this issue is often disregarded when measuring target mRNA expression. Therefore, we (1) evaluated the frequency of appropriate reference gene selection, (2) suggest an easy-to-use tool for least variability reference gene selection, (3) demonstrate application of this tool, and (4) show effects on target gene expression profiles...
September 20, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27601479/cardiac-fibroblast-grk2-deletion-enhances-contractility-and-remodeling-following-ischemia-reperfusion-injury
#12
Meryl C Woodall, Benjamin P Woodall, Erhe Gao, Ancai Yuan, Walter J Koch
RATIONALE: G protein-coupled receptor kinase 2 (GRK2) is an important molecule upregulated after myocardial injury and during heart failure. Myocyte-specific GRK2 loss before and after myocardial ischemic injury improves cardiac function and remodeling. The cardiac fibroblast plays an important role in the repair and remodeling events after cardiac ischemia; the importance of GRK2 in these events has not been investigated. OBJECTIVE: The aim of this study is to elucidate the in vivo implications of deleting GRK2 in the cardiac fibroblast after ischemia/reperfusion injury...
October 28, 2016: Circulation Research
https://www.readbyqxmd.com/read/27573285/regulatory-effects-of-grk2-on-gpcrs-and-non-gpcrs-and-possible-use-as-a-drug-target-review
#13
Chen-Chen Han, Yang Ma, Yifan Li, Yang Wang, Wei Wei
G protein-coupled receptor kinase 2 (GRK2) is a key member of the G protein-coupled receptor kinase (GRK) family. GRK2 activity is regulated by the C-terminus of GRK2 which contains a plekstrin homology domain and the N-terminus of GRK2 which contains the RGS homology domain with binding sites for several proteins and lipids such as G protein-coupled receptors (GPCRs), G protein, phospholipase C, phosphatidylinositol 4,5-bisphosphate, extracellular signal‑regulated kinase, protein kinase A and Gβγ...
October 2016: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/27568556/grk2-constitutively-governs-peripheral-delta-opioid-receptor-activity
#14
Allison Doyle Brackley, Ruben Gomez, Armen N Akopian, Michael A Henry, Nathaniel A Jeske
Opioids remain the standard for analgesic care; however, adverse effects of systemic treatments contraindicate long-term administration. While most clinical opioids target mu opioid receptors (MOR), those that target the delta class (DOR) also demonstrate analgesic efficacy. Furthermore, peripherally restrictive opioids represent an attractive direction for analgesia. However, opioid receptors including DOR are analgesically incompetent in the absence of inflammation. Here, we report that G protein-coupled receptor kinase 2 (GRK2) naively associates with plasma membrane DOR in peripheral sensory neurons to inhibit analgesic agonist efficacy...
September 6, 2016: Cell Reports
https://www.readbyqxmd.com/read/27566547/skeletal-muscle-specific-g-protein-coupled-receptor-kinase-2-ablation-alters-isolated-skeletal-muscle-mechanics-and-enhances-clenbuterol-stimulated-hypertrophy
#15
Benjamin P Woodall, Meryl C Woodall, Timothy S Luongo, Laurel A Grisanti, Douglas G Tilley, John W Elrod, Walter J Koch
GRK2, a G protein-coupled receptor kinase, plays a critical role in cardiac physiology. Adrenergic receptors are the primary target for GRK2 activity in the heart; phosphorylation by GRK2 leads to desensitization of these receptors. As such, levels of GRK2 activity in the heart directly correlate with cardiac contractile function. Furthermore, increased expression of GRK2 after cardiac insult exacerbates injury and speeds progression to heart failure. Despite the importance of this kinase in both the physiology and pathophysiology of the heart, relatively little is known about the role of GRK2 in skeletal muscle function and disease...
October 14, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27543854/astragaloside-iv-alleviates-e-coli-caused-peritonitis-via-upregulation-of-neutrophil-influx-to-the-site-of-infection
#16
Ping Huang, Xiaoyan Lu, Baohong Yuan, Tao Liu, Liangcheng Dai, Yunjun Liu, Hui Yin
Astragaloside IV (AS-IV), an active saponin purified from Astragali Radix, has been identified with broad biological and pharmacological activities. In the present study, we continue to explore the potential effect of AS-IV on antibacterial response using an acute E. coli peritoneal infection model. Our findings implied that administration of AS-IV decreases mortality in mice challenged by lethal E. coli infection. The protection of AS-IV was related to promotion of neutrophil extravasation into the peritoneum and bacterial clearance...
October 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27492965/agonist-induced-internalization-and-desensitization-of-the-apelin-receptor
#17
George R Pope, Sharada Tilve, Craig A McArdle, Stephen J Lolait, Anne-Marie O'Carroll
Apelin acts via the G protein-coupled apelin receptor (APJ) to mediate effects on cardiovascular and fluid homeostasis. G protein-coupled receptor (GPCR) trafficking has an important role in the regulation of receptor signalling pathways and cellular functions, however in the case of APJ the mechanisms and proteins involved in apelin-induced trafficking are not well understood. We generated a stable HEK-293 cell line expressing N-terminus HA-tagged mouse (m) APJ, and used a semi-automated imaging protocol to quantitate APJ trafficking and ERK1/2 activation following stimulation with [Pyr(1)]apelin-13...
December 5, 2016: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/27462452/hypertension-associated-c825t-polymorphism-impairs-the-function-of-g%C3%AE-3-to-target-grk2-ubiquitination
#18
Zhengyu Zha, Xiao-Ran Han, Matthew D Smith, Qun-Ying Lei, Kun-Liang Guan, Yue Xiong
Population-based and case-control studies in different ethnicities have linked a polymorphism, C825T, in exon 10 of GNB3 gene to hypertension and several additional diseases. The 825T allele is associated with alternative splicing and results in a shortened Gβ3 protein, referred to as Gβ3s, which loses 41 amino acids encompassing one WD40 repeat domain. The mechanism of how Gβ3 C825T polymorphism is associated with hypertension has remained unclear, but an impairment of its canonical function in G-protein-coupled receptor signaling has been ruled out...
2016: Cell Discovery
https://www.readbyqxmd.com/read/27412951/g-protein-coupled-receptor-kinase-2-terminates-g-protein-coupled-receptor-function-in-steroid-hormone-20-hydroxyecdysone-signaling
#19
Wen-Li Zhao, Di Wang, Chun-Yan Liu, Xiao-Fan Zhao
G-protein-coupled receptors (GPCRs) transmit extracellular signals across the cell membrane. GPCR kinases (GRKs) desensitize GPCR signals in the cell membrane. However, the role and mechanism of GRKs in the desensitization of steroid hormone signaling are unclear. In this study, we propose that GRK2 is phosphorylated by protein kinase C (PKC) in response to induction by the steroid hormone 20-hydroxyecdysone (20E), which determines its translocation to the cell membrane of the lepidopteran Helicoverpa armigera...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27385268/understanding-perspectives-of-signalling-mechanisms-regulating-pebp1-function
#20
REVIEW
Karthik Rajkumar, Aare Nichita, Pawan Kumar Anoor, Swathi Raju, Surya Satyanarayana Singh, Sandeepta Burgula
UNLABELLED: Phosphatidylethanolamine-binding protein 1 (PEBP1), also known as Raf kinase inhibitor protein, belongs to PEBP family of proteins. It is known to interact with many proteins that are mainly involved in pathways that monitor cell proliferation and differentiation. PEBP1 in many cells interacts with several pathways, namely MAPK, GRK2, NF-кB, etc. that keeps the cell proliferation and differentiation in check. This protein is expressed by many cells in humans, including neurons where it is predominantly involved in production of choline acetyltransferase...
August 2016: Cell Biochemistry and Function
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