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https://www.readbyqxmd.com/read/28077324/grk2-as-negative-modulator-of-no-bioavailability-implications-for-cardiovascular-disease
#1
REVIEW
Alessandro Cannavo, Walter J Koch
Nitric oxide (NO), initially identified as endothelium-derived relaxing factor (EDRF), is a gaso-transmitter with important regulatory roles in the cardiovascular, nervous and immune systems. In the former, this diatomic molecule and free radical gas controls vascular tone and cardiac mechanics, among others. In the cardiovascular system, it is now understood that β-adrenergic receptor (βAR) activation is a key modulator of NO generation. Therefore, it is not surprising that the up-regulation of G protein-coupled receptor kinases (GRKs), in particular GRK2, that restrains βAR activity contributes to impaired cardiovascular functions via alteration of NO bioavailability...
January 7, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28035008/regulator-of-g-protein-signaling-6-protects-the-heart-from-ischemic-injury
#2
Boyd R Rorabaugh, Bandana Chakravarti, Nathaniel W Mabe, Sarah L Seeley, Albert D Bui, Jianqi Yang, Stephanie W Watts, Richard R Neubig, Rory A Fisher
Gαi-coupled receptors play important roles in protecting the heart from ischemic injury. Regulator of G protein signaling (RGS) proteins suppress Gαi signaling by accelerating the GTPase activity of Gαi subunits. However, the roles of individual RGS proteins in modulating ischemic injury are unknown. In the present study, we investigated the impact of RGS6 deletion on myocardial sensitivity to ischemic injury. Hearts from RGS6 knockout (RGS6-/-) and wildtype (RGS6+/+) mice were subjected to 30 min ischemia and 2 hr reperfusion on a Langendorff heart apparatus...
December 29, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27999776/-freeze-don-t-move-how-to-arrest-a-suspect-in-heart-failure-a-review-on-available-grk2-inhibitors
#3
REVIEW
Daniela Sorriento, Michele Ciccarelli, Ersilia Cipolletta, Bruno Trimarco, Guido Iaccarino
Cardiovascular disease and heart failure (HF) still collect the largest toll of death in western societies and all over the world. A growing number of molecular mechanisms represent possible targets for new therapeutic strategies, which can counteract the metabolic and structural changes observed in the failing heart. G protein-coupled receptor kinase 2 (GRK2) is one of such targets for which experimental and clinical evidence are established. Indeed, several strategies have been carried out in place to interface with the known GRK2 mechanisms of action in the failing heart...
2016: Frontiers in Cardiovascular Medicine
https://www.readbyqxmd.com/read/27992454/the-effects-of-swiprosin-1-on-the-formation-of-pseudopodia-like-structures-and-%C3%AE-adrenoceptor-coupling-in-cultured-adult-rat-ventricular-cardiomyocytes
#4
Franziska Nippert, Rolf Schreckenberg, Antonia Hess, Martin Weber, Klaus-Dieter Schlüter
BACKGROUND: Recent findings suggest that adult terminally differentiated cardiomyocytes adapt to stress by cellular de- and redifferentiation. In the present study we tested the hypothesis that swiprosin-1 is a key player in this process. Furthermore, the relationship between swiprosin-1 and β-adrenoceptor coupling was analyzed. METHODS: In order to study the function of swiprosin-1 in adult rat ventricular cardiomyocytes (ARVC) they were isolated and cultured in a medium containing 20% fetal calf serum (FCS)...
2016: PloS One
https://www.readbyqxmd.com/read/27895163/g-protein-coupled-receptor-kinase-2-grk2-as-a-potential-modulator-of-the-hallmarks-of-cancer
#5
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-receptor-kinase-2-upregulation-causes-%C3%AE%C2%BA-opioid-receptor-desensitization-in-diabetic-heart
#6
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 and cardioprotective effects were significantly impaired in hearts isolated from streptozotocin (STZ) injection-induced diabetic mice...
January 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27862165/grk2-%C3%AE-arrestin-mediates-arginine-vasopressin-induced-cardiac-fibroblast-proliferation
#7
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
#8
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-2-adrenergic-receptor-activation-prevents-diabetes-associated-cardiac-dysfunction
#9
Qingtong Wang, Yongming Liu, Qin Fu, Bing Xu, Yuan Zhang, Sungjin Kim, Ruensern Tan, Federica Barbagallo, Toni West, Ethan Anderson, Wei Wei, E Dale Abel, Yang K Xiang
BACKGROUND: Type 2 diabetes mellitus (DM) and obesity independently increase the risk of heart failure by incompletely understood mechanisms. We propose that hyperinsulinemia might promote adverse consequences in the hearts of subjects with type-2 DM and obesity. METHODS: High-fat diet feeding was used to induce obesity and DM in wild-type mice or mice lacking β2-adrenergic receptor (β2AR) or β-arrestin2. Wild-type mice fed with high-fat diet were treated with a β-blocker carvedilol or a GRK2 (G-protein-coupled receptor kinase 2) inhibitor...
January 3, 2017: Circulation
https://www.readbyqxmd.com/read/27773680/vasopressin-v1a-receptor-mediates-cell-proliferation-through-grk2-egfr-erk1-2-pathway-in-a7r5-cells
#10
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...
December 5, 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
#11
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...
November 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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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