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https://www.readbyqxmd.com/read/29154938/assessments-of-cellular-melatonin-receptor-signaling-pathways-%C3%AE-arrestin-recruitment-receptor-internalization-and-impedance-variations
#1
Clémence Dupré, Olivier Bruno, Anne Bonnaud, Adeline Giganti, Olivier Nosjean, Céline Legros, Jean A Boutin
Melatonin receptors belong to the family of G-protein coupled receptors. Agonist-induced receptor activation is terminated with the recruitment of β-arrestin, which leads to receptor internalization. Furthermore, agonist binding induces a shift in cellular shape that translates into a change in the electric impedance of the cell. In the present study, we employed engineered cells to study these internalization-related processes in the context of the two melatonin receptors, MT1 and MT2. To assess these three receptor internalization-related functions and validate the results, we employed four classical ligands of melatonin receptors: the natural agonist melatonin; the super-agonist 2-iodo-melatonin and the two antagonists luzindole and 4-phenyl-2-propionamidotetralin...
November 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29146594/heterologous-phosphorylation-induced-formation-of-a-stability-lock-permits-regulation-of-inactive-receptors-by-%C3%AE-arrestins
#2
András D Tóth, Susanne Prokop, Pál Gyombolai, Péter Várnai, András Balla, Vsevolod V Gurevich, László Hunyady, Gábor Turu
β-arrestins are key regulators and signal transducers of G protein-coupled receptors (GPCRs). The interaction between receptors and β-arrestins is generally believed to require both receptor activity and phosphorylation by GPCR kinases. In this study, we investigated whether β-arrestins are able to bind second messenger kinase-phosphorylated, but inactive receptors as well. Since heterologous phosphorylation is a common phenomenon among GPCRs, this mode of β-arrestin activation may represent a novel mechanism of signal transduction and receptor cross-talk...
November 16, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29137031/subcellular-localization-of-%C3%AE-arrestin1-and-its-prognostic-value-in-lung-adenocarcinoma
#3
Xiaowei Li, Keying Che, Liguang Wang, Tiehong Zhang, Guanghui Wang, Zhaofei Pang, Hongchang Shen, Jiajun Du
β-Arrestins play important roles in cancer progression, and the subcellular localization of β-arrestin1 has been receiving increasingly more attention. Intriguingly, several studies, including some of our previous work, showed that the effects of β-arrestin1 on outcomes of cancer patients were controversial.Specimens were obtained from 133 patients with lung adenocarcinoma. Immunohistochemistry was used to detect the expression of β-arrestin1 and p300 in the collected tissues. The Kaplan-Meier analysis and Cox proportional hazards regression were used to examine the relationship between β-arrestin1 and patient survival...
November 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29133163/non-visual-arrestins-regulate-the-focal-adhesion-formation-via-small-gtpases-rhoa-and-rac1-independently-of-gpcrs
#4
Whitney M Cleghorn, Nada Bulus, Seunghyi Kook, Vsevolod V Gurevich, Roy Zent, Eugenia V Gurevich
Arrestins recruit a variety of signaling proteins to active phosphorylated G protein-coupled receptors in the plasma membrane and to the cytoskeleton. Loss of arrestins leads to decreased cell migration, altered cell shape, and an increase in focal adhesions. Small GTPases of the Rho family are molecular switches that regulate actin cytoskeleton and affect a variety of dynamic cellular functions including cell migration and cell morphology. Here we show that non-visual arrestins differentially regulate RhoA and Rac1 activity to promote cell spreading via actin reorganization, and focal adhesion formation via two distinct mechanisms...
November 11, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/29130787/mir-19a-and-mir-424-target-tgfbr3-to-promote-epithelial-to-mesenchymal-transition-and-migration-of-tongue-squamous-cell-carcinoma-cells
#5
Duo Li, Ke Liu, Zhiyong Li, Jian Wang, Xiaofeng Wang
Previous studies indicate that TGFBR3 (transforming growth factor type III receptor, also known as betaglycan), a novel suppressor of progression in certain cancers, is down-regulated in tongue squamous cell carcinoma (TSCC). However, the role of this factor as an upstream regulator in TSCC cells remains to be elucidated. The present study was designed to elucidate whether TGFBR3 gene expression is regulated by two microRNA molecules, miR-19a and miR-424. The study also aimed to determine if these microRNAs promote migration of CAL-27 human oral squamous cells...
November 13, 2017: Cell Adhesion & Migration
https://www.readbyqxmd.com/read/29130686/thioamide-substitution-selectively-modulates-proteolysis-and-receptor-activity-of-therapeutic-peptide-hormones
#6
Xing Chen, Elizabeth G Mietlicki-Baase, Taylor M Barrett, Lauren E McGrath, Kieran Koch-Laskowski, John J Ferrie, Matthew R Hayes, E James Petersson
Peptide hormones are attractive as injectable therapeutics and imaging agents, but they often require extensive modification by mutagenesis and/or chemical synthesis to prevent rapid in vivo degradation. Alternatively, the single-atom, O-to-S modification of peptide backbone thioamidation has the potential to selectively perturb interactions with proteases while preserving interactions with other proteins, such as target receptors. Here, we use the validated diabetes therapeutic, glucagon-like peptide-1 (GLP-1), and the target of clinical investigation, gastric inhibitory polypeptide (GIP), as proof-of-principle peptides to demonstrate the value of thioamide substitution...
November 13, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29127291/structural-basis-of-arrestin-3-activation-and-signaling
#7
Qiuyan Chen, Nicole A Perry, Sergey A Vishnivetskiy, Sandra Berndt, Nathaniel C Gilbert, Ya Zhuo, Prashant K Singh, Jonas Tholen, Melanie D Ohi, Eugenia V Gurevich, Chad A Brautigam, Candice S Klug, Vsevolod V Gurevich, T M Iverson
A unique aspect of arrestin-3 is its ability to support both receptor-dependent and receptor-independent signaling. Here, we show that inositol hexakisphosphate (IP6) is a non-receptor activator of arrestin-3 and report the structure of IP6-activated arrestin-3 at 2.4-Å resolution. IP6-activated arrestin-3 exhibits an inter-domain twist and a displaced C-tail, hallmarks of active arrestin. IP6 binds to the arrestin phosphate sensor, and is stabilized by trimerization. Analysis of the trimerization surface, which is also the receptor-binding surface, suggests a feature called the finger loop as a key region of the activation sensor...
November 10, 2017: Nature Communications
https://www.readbyqxmd.com/read/29123644/rnai-targeting-caenorhabditis-elegans-%C3%AE-arrestins-marginally-affects-lifespan
#8
Sangsoon Park, Yoonji Jung, Seon Woo A An, Heehwa G Son, Wooseon Hwang, Dongyeop Lee, Murat Artan, Hae-Eun H Park, Dae-Eun Jeong, Yujin Lee, Seung-Jae V Lee
Background: α-arrestins are a family of proteins that are implicated in multiple biological processes, including metabolism and receptor desensitization. Methods: Here, we sought to examine the roles of α-arrestins in the longevity of Caenorhabditis elegans through an RNA interference screen. Results: We found that knocking down each of 24 out of total 29 C. elegans α-arrestins had small or no effects on lifespan. Thus, individual C. elegans α-arrestins may have minor effects on longevity. Conclusions: This study will provide useful information for future research on the functional role of α-arrestins in aging and longevity...
2017: F1000Research
https://www.readbyqxmd.com/read/29122578/a-carvedilol-responsive-microrna-mir-125b-5p-protects-the-heart-from-acute-myocardial-infarction-by-repressing-pro-apoptotic-bak1-and-klf13-in-cardiomyocytes
#9
Ahmed S Bayoumi, Kyoung-Mi Park, Yongchao Wang, Jian-Peng Teoh, Tatsuya Aonuma, Yaoliang Tang, Huabo Su, Neal L Weintraub, Il-Man Kim
BACKGROUND: Cardiac injury is accompanied by dynamic changes in the expression of microRNAs (miRs), small non-coding RNAs that post-transcriptionally regulate target genes. MiR-125b-5p is downregulated in patients with end-stage dilated and ischemic cardiomyopathy, and has been proposed as a biomarker of heart failure. We previously reported that the β-blocker carvedilol promotes cardioprotection via β-arrestin-biased agonism of β1-adrenergic receptor while stimulating miR-125b-5p processing in the mouse heart...
November 7, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/29116339/%C3%AE-arrestin-1-deficiency-ameliorates-renal-interstitial-fibrosis-by-blocking-wnt1-%C3%AE-catenin-signaling-in-mice
#10
Huiyan Xu, Quanxin Li, Jiang Liu, Jiaqing Zhu, Liang Li, Ziying Wang, Yan Zhang, Yu Sun, Jinpeng Sun, Rong Wang, Fan Yi
Despite substantial progress being made in understanding the mechanisms contributing to the pathogenesis of renal fibrosis, there are only a few therapies available to treat or prevent renal fibrosis in clinical use today. Therefore, identifying the key cellular and molecular mediators involved in the pathogenesis of renal fibrosis will provide new therapeutic strategy for treating patients with chronic kidney disease (CKD). β-Arrestin-1, a member of β-arrestin family, not only is a negative adaptor of G protein-coupled receptors (GPCRs), but also acts as a scaffold protein and regulates a diverse array of cellular functions independent of GPCR activation...
November 7, 2017: Journal of Molecular Medicine: Official Organ of the "Gesellschaft Deutscher Naturforscher und Ärzte"
https://www.readbyqxmd.com/read/29104500/clenbuterol-induces-cell-cycle-arrest-in-c2c12-myoblasts-by-delaying-p27-degradation-through-%C3%AE-arrestin-2-signaling
#11
Min Chen, Chuncheng Liu, Meng Wang, Hong Wang, Kuo Zhang, Yu Zheng, Zhengquan Yu, Xiangdong Li, Wei Guo, Ning Li, Qingyong Meng
β2-Adrenoceptor (β2-AR) agonists promote muscle growth. The aim of this study was to elucidate some effects of the selective β2-adrenoceptor agonist clenbuterol (CLB) on myoblast proliferation. We found that CLB induces cell cycle arrest in C2C12 myoblasts. This effect is partly due to the enhanced stability of p27, rather than the increased gene transcription via cAMP response element-binding protein (CREB). Specifically, CLB treatment enhanced the accumulation of p27 in the nucleus while depleting it from the cytosol via a mechanism that requires β2-AR...
2017: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/29089368/discovery-of-a-positive-allosteric-modulator-of-the-tsh-receptor-potentiation-of-tsh-mediated-preosteoblast-differentiation-in-vitro
#12
Susanne Neumann, Elena Eliseeva, Alisa Boutin, Elena Barnaeva, Marc Ferrer, Noel Southall, David Kim, Xin Hu, Sarah J Morgan, Juan J Marugan, Marvin C Gershengorn
Recently, we showed that TSH-enhanced differentiation of a human preosteoblast-like cell model involved a β-arrestin 1 (β-Arr 1) mediated pathway. To study this pathway in more detail, we sought to discover a small molecule ligand that was functionally selective toward human TSH receptor (TSHR) activation of β-Arr 1. High-throughput screening using a cell line stably expressing mutated TSHRs and mutated β-Arr 1 (DiscoverX1 cells) led to the discovery of agonists that stimulated translocation of β-Arr 1 to the TSHR, but did not activate Gs-mediated signaling pathways, i...
October 31, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29081032/prolonged-morphine-treatment-alters-expression-and-plasma-membrane-distribution-of-%C3%AE-adrenergic-receptors-and-some-other-components-of-their-signaling-system-in-rat-cerebral-cortex
#13
Lucie Hejnova, Jitka Skrabalova, Jiri Novotny
β-Adrenergic signaling plays an important role in regulating diverse brain functions and alterations in this signaling have been observed in different neuropathological conditions. In this study, we investigated the effect of a 10-day treatment with high doses of morphine (10 mg/kg per day) on major components and functional state of the β-adrenergic receptor (β-AR) signaling system in the rat cerebral cortex. β-ARs were characterized by radioligand binding assays and amounts of various G protein subunits, adenylyl cyclase (AC) isoforms, G protein-coupled receptor kinases (GRKs), and β-arrestin were examined by Western blot analysis...
October 28, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/29078372/dephosphorylation-by-protein-phosphatase-2a-regulates-visual-pigment-regeneration-and-the-dark-adaptation-of-mammalian-photoreceptors
#14
Alexander V Kolesnikov, Tivadar Orban, Hui Jin, Celine Brooks, Lukas Hofmann, Zhiqian Dong, Maxim Sokolov, Krzysztof Palczewski, Vladimir J Kefalov
Resetting of G-protein-coupled receptors (GPCRs) from their active state back to their biologically inert ground state is an integral part of GPCR signaling. This "on-off" GPCR cycle is regulated by reversible phosphorylation. Retinal rod and cone photoreceptors arguably represent the best-understood example of such GPCR signaling. Their visual pigments (opsins) are activated by light, transduce the signal, and are then inactivated by a GPCR kinase and arrestin. Although pigment inactivation by phosphorylation is well understood, the enzyme(s) responsible for pigment dephosphorylation and the functional significance of this reaction remain unknown...
November 7, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29073113/%C3%AE-2-adrenoceptor-signaling-in-airway-epithelial-cells-promotes-eosinophilic-inflammation-mucous-metaplasia-and-airway-contractility
#15
Long P Nguyen, Nour A Al-Sawalha, Sergio Parra, Indira Pokkunuri, Ozozoma Omoluabi, Adedoyin A Okulate, Elizabeth Windham Li, Matthew Hazen, Jose M Gonzalez-Granado, Craig J Daly, John C McGrath, Michael J Tuvim, Brian J Knoll, Burton F Dickey, Richard A Bond
The mostly widely used bronchodilators in asthma therapy are β2-adrenoreceptor (β2AR) agonists, but their chronic use causes paradoxical adverse effects. We have previously determined that β2AR activation is required for expression of the asthma phenotype in mice, but the cell types involved are unknown. We now demonstrate that β2AR signaling in the airway epithelium is sufficient to mediate key features of the asthmatic responses to IL-13 in murine models. Our data show that inhibition of β2AR signaling with an aerosolized antagonist attenuates airway hyperresponsiveness (AHR), eosinophilic inflammation, and mucus-production responses to IL-13, whereas treatment with an aerosolized agonist worsens these phenotypes, suggesting that β2AR signaling on resident lung cells modulates the asthma phenotype...
October 24, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29070696/structural-determinants-influencing-the-potency-and-selectivity-of-indazole-paroxetine-hybrid-g-protein-coupled-receptor-kinase-2-inhibitors
#16
Renee Bouley, Helen V Waldschmidt, M Claire Cato, Alessandro Cannavo, Jianliang Song, Joseph Y Cheung, Xin-Qiu Yao, Walter J Koch, Scott D Larsen, John J Tesmer
G protein-coupled receptor kinases (GRKs) phosphorylate activated receptors to promote arrestin binding, decoupling from heterotrimeric G proteins, and internalization. GRK2 and GRK5 are overexpressed in the failing heart and thus have become therapeutic targets. Previously, we discovered two classes of GRK2-selective inhibitors, one stemming from GSK180736A, a ROCK1 inhibitor, and the other from paroxetine, a selective serotonin-reuptake inhibitor. These two classes of compounds bind to the GRK2 active site in a similar configuration, but contain different hinge-binding "warheads": indazole and benzodioxole, respectively...
October 25, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29068002/engineered-d2r-variants-reveal-the-balanced-and-biased-contributions-of-g-protein-and-%C3%AE-arrestin-to-dopamine-dependent-functions
#17
Samuel J Rose, Thomas F Pack, Sean M Peterson, Kaitlin Payne, Emiliana Borrelli, Marc G Caron
The dopamine D2 receptor (D2R), like many G-protein coupled-receptors, signals through G-protein and β-arrestin-dependent pathways. Preferential activation of one of these pathways is termed functional selectivity or biased signaling and is a promising therapeutic strategy. Though biased signaling through D2Rs has been demonstrated, acquiring the mechanistic details of biased D2R/G-protein and D2R/β-arrestin signaling in vivo has been challenging due to the lack of techniques that specifically target these interactions in discrete cell populations...
October 25, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29063139/dissociable-effects-of-the-kappa-opioid-receptor-agonist-nalfurafine-on-pain-itch-stimulated-and-pain-itch-depressed-behaviors-in-male-rats
#18
Matthew L Lazenka, Megan J Moerke, E Andrew Townsend, Kevin B Freeman, F Ivy Carroll, S Stevens Negus
RATIONALE: Nalfurafine is a G protein signaling-biased kappa opioid receptor (KOR) agonist approved in Japan for second-line treatment of uremic pruritus. Neither nalfurafine nor any other KOR agonist is currently approved anywhere for treatment of pain, but recent evidence suggests that G protein signaling-biased KOR agonists may have promise as candidate analgesics/antipruritics with reduced side effects compared to nonbiased or ß-arrestin-signaling-biased KOR agonists. OBJECTIVES: This study compared nalfurafine effects in rats using assays of pain-stimulated and pain-depressed behavior used previously to evaluate other candidate analgesics...
October 24, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29062240/a-randomized-phase-iib-study-investigating-oliceridine-trv130-a-novel-%C3%A2%C2%B5-receptor-g-protein-pathway-selective-%C3%AE-gps-modulator-for-the-management-of-moderate-to-severe-acute-pain-following-abdominoplasty
#19
Neil Singla, Harold S Minkowitz, David G Soergel, David A Burt, Ruth Ann Subach, Monica Y Salamea, Michael J Fossler, Franck Skobieranda
BACKGROUND: Oliceridine (TRV130), a novel μ-receptor G-protein pathway selective (μ-GPS) modulator, was designed to improve the therapeutic window of conventional opioids by activating G-protein signaling while causing low β-arrestin recruitment to the μ receptor. This randomized, double-blind, patient-controlled analgesia Phase IIb study was conducted to investigate the efficacy, safety, and tolerability of oliceridine compared with morphine and placebo in patients with moderate to severe pain following abdominoplasty (NCT02335294; oliceridine is an investigational agent not yet approved by the US Food and Drug Administration)...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/29062223/enhancing-the-efficacy-of-areds-antioxidants-in-light-induced-retinal-degeneration
#20
Paul Wong, M Markey, C M Rapp, R M Darrow, A Ziesel, D T Organisciak
PURPOSE: Light-induced photoreceptor cell degeneration and disease progression in age-related macular degeneration (AMD) involve oxidative stress and visual cell loss, which can be prevented, or slowed, by antioxidants. Our goal was to test the protective efficacy of a traditional Age-related Eye Disease Study antioxidant formulation (AREDS) and AREDS combined with non-traditional antioxidants in a preclinical animal model of photooxidative retinal damage. METHODS: Male Sprague-Dawley rats were reared in a low-intensity (20 lux) or high-intensity (200 lux) cyclic light environment for 6 weeks...
2017: Molecular Vision
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