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https://www.readbyqxmd.com/read/28536260/functional-role-of-the-three-conserved-cysteines-in-the-n-domain-of-visual-arrestin-1
#1
Sergey A Vishnivetskiy, Regina J Lee, X Edward Zhou, Andreas Franz, Qiuyi Xu, H Eric Xu, Vsevolod V Gurevich
Arrestins specifically bind active and phosphorylated forms of their cognate G protein-coupled receptors, blocking G protein coupling and often redirecting the signaling to alternative pathways. High-affinity receptor binding is accompanied by the two major structural changes in arrestin: the release of the C-tail and rotation of the two domains relative to each other. The first requires the detachment of the arrestin C-tail from the body of the molecule, whereas the second requires the disruption of the network of charge-charge interactions at the interdomain interface, termed the polar core...
May 23, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28534985/microarray-analysis-of-differentially-expressed-genes-in-l929-mouse-fibroblast-cells-exposed-to-leptin-and-hypoxia
#2
Ping Ouyang, Sen Wang, He Zhang, Zhigang Huang, Pei Wei, Ye Zhang, Zhuguo Wu, Tao Li
Leptin and hypoxia are pro-fibrotic factors involved in fibrogenesis, however, the gene expression profiles remain to be fully elucidated. The aim of the present study was to investigate the regulatory roles of leptin and hypoxia on the L929 mouse fibroblast cell line. The cells were assigned to a normoxia, normoxia with leptin, hypoxia, and hypoxia with leptin group. The cDNA expression was detected using an Agilent mRNA array platform. The differentially expressed genes (DEGs) in response to leptin and hypoxia were identified using reverse transcription‑quantitative polymerase chain reaction analysis, followed by clustering analysis, Gene Ontology analysis and pathway analysis...
May 17, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28533287/trv0109101-a-g-protein-biased-agonist-of-the-%C3%A2%C2%B5-opioid-receptor-does-not-promote-opioid-induced-mechanical-allodynia-following-chronic-administration
#3
Michael Koblish, Richard Carr, Edward R Siuda, David H Rominger, William Gowen-MacDonald, Conrad L Cowan, Aimee L Crombie, Jonathan D Violin, Michael W Lark
Prescription opioids are a mainstay in the treatment of acute moderate to severe pain. However, chronic use leads to a host of adverse consequences including tolerance and opioid-induced hyperalgesia (OIH), leading to more complex treatment regimens and diminished patient compliance. Patients experiencing OIH paradoxically experience exaggerated nociceptive responses instead of pain reduction after chronic opioid usage. The development of OIH and tolerance tend to occur simultaneously and, thus, present a challenge when studying the molecular mechanisms driving each phenomenon...
May 22, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28527699/at1-receptor-signaling-pathways-in-the-cardiovascular-system
#4
REVIEW
Tatsuo Kawai, Steven J Forrester, Shannon O'Brien, Ariele Baggett, Victor Rizzo, Satoru Eguchi
The importance of the renin angiotensin aldosterone system in cardiovascular physiology and pathophysiology has been well described whereas the detailed molecular mechanisms remain elusive. The angiotensin II type 1 receptor (AT1 receptor) is one of the key players in the renin angiotensin aldosterone system. The AT1 receptor promotes various intracellular signaling pathways resulting in hypertension, endothelial dysfunction, vascular remodeling and end organ damage. Accumulating evidence shows the complex picture of AT1 receptor-mediated signaling; AT1 receptor-mediated heterotrimeric G protein-dependent signaling, transactivation of growth factor receptors, NADPH oxidase and ROS signaling, G protein-independent signaling, including the β-arrestin signals and interaction with several AT1 receptor interacting proteins...
May 17, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28525390/microrna-155-attenuates-late-sepsis-induced-cardiac-dysfunction-through-jnk-and-%C3%AE-arrestin-2
#5
Yu Zhou, Yan Song, Zahir Shaikh, Hui Li, Haiju Zhang, Yi Caudle, Shouhua Zheng, Hui Yan, Dan Hu, Charles Stuart, Deling Yin
Cardiac dysfunction is correlated with detrimental prognosis of sepsis and contributes to a high risk of mortality. After an initial hyperinflammatory reaction, most patients enter a protracted state of immunosuppression (late sepsis) that alters both innate and adaptive immunity. The changes of cardiac function in late sepsis are not yet known. MicroRNA-155 (miR-155) is previously found to play important roles in both regulations of immune activation and cardiac function. In this study, C57BL/6 mice were operated to develop into early and late sepsis phases, and miR-155 mimic was injected through the tail vein 48 h after cecal ligation and puncture (CLP)...
May 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28506231/optogenetic-interrogation-reveals-separable-g-protein-dependent-and-independent-signalling-linking-g-protein-coupled-receptors-to-the-circadian-oscillator
#6
Helena J Bailes, Nina Milosavljevic, Ling-Yu Zhuang, Elliot J Gerrard, Tomoki Nishiguchi, Takeaki Ozawa, Robert J Lucas
BACKGROUND: Endogenous circadian oscillators distributed across the mammalian body are synchronised among themselves and with external time via a variety of signalling molecules, some of which interact with G-protein-coupled receptors (GPCRs). GPCRs can regulate cell physiology via pathways originating with heterotrimeric G-proteins or β-arrestins. We applied an optogenetic approach to determine the contribution of these two signalling modes on circadian phase. RESULTS: We employed a photopigment (JellyOp) that activates Gαs signalling with better selectivity and higher sensitivity than available alternatives, and a point mutant of this pigment (F112A) biased towards β-arrestin signalling...
May 15, 2017: BMC Biology
https://www.readbyqxmd.com/read/28502792/drug-binding-poses-relate-structure-with-efficacy-in-the-%C3%AE-opioid-receptor
#7
Katy J Sutcliffe, Graeme Henderson, Eamonn Kelly, Richard B Sessions
The μ-opioid receptor (MOPr) is a clinically important G protein-coupled receptor (GPCR) which couples to Gi/o proteins and arrestins. At present the receptor conformational changes that occur following agonist binding and activation are poorly understood. This study has employed molecular dynamics simulations to investigate the binding mode and receptor conformational changes induced by structurally similar opioid ligands of widely differing intrinsic agonist efficacy, norbuprenorphine, buprenorphine and diprenorphine...
May 11, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28499989/melanocortin-receptor-accessory-proteins-mraps-functions-in-the-melanocortin-system-and-beyond
#8
REVIEW
Alix A J Rouault, Dinesh K Srinivasan, Terry C Yin, Abigail A Lee, Julien A Sebag
G-protein coupled receptors (GPCRs) are regulated by numerous proteins including kinases, G-proteins, β-arrestins and accessory proteins. Several families of GPCR accessory proteins like Receptor Activity Modifying Proteins, Receptor Transporting Proteins and Melanocortin Receptor Accessory Proteins (MRAPs) have been identified as regulator of receptor trafficking, signaling and ligand specificity. The MRAP family contains two members, MRAP1 and MRAP2, responsible for the formation of a functional ACTH receptor and for the regulation of energy homeostasis respectively...
May 9, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28495999/%C3%AE-arrestin-mediated-regulation-of-the-human-ether-a-go-go-related-gene-herg-potassium-channel
#9
Matthew G Sangoi, Shawn M Lamothe, Jun Guo, Tonghua Yang, Wentao Li, Ellen G Avery, John T Fisher, Shetuan Zhang
The rapidly activating delayed rectifier K(+) channel (IKr) is encoded by the human ether-a-go-go-related gene (hERG), which is important for the repolarization of the cardiac action potential. Mutations in hERG or drugs can impair the function or decrease the expression level of hERG channels, leading to long QT syndrome (LQTS). Thus, it is important to understand hERG channel trafficking and its regulation. For this purpose, G protein-coupled receptors (GPCRs), which regulate a vast array of cellular processes, represent a useful route...
May 11, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28495495/translating-in-vitro-ligand-bias-into-in-vivo-efficacy
#10
REVIEW
Louis M Luttrell, Stuart Maudsley, Diane Gesty-Palmer
It is increasingly apparent that ligand structure influences both the efficiency with which G protein-coupled receptors (GPCRs) engage their downstream effectors and the manner in which they are activated. Thus, 'biased' agonists, synthetic ligands whose intrinsic efficacy differs from the native ligand, afford a strategy for manipulating GPCR signaling in ways that promote beneficial signals while blocking potentially deleterious ones. Still, there are significant challenges in relating in vitro ligand efficacy, which is typically measured in heterologous expression systems, to the biological response in vivo, where the ligand is acting on natively expressed receptors and in the presence of the endogenous ligand...
May 7, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28493341/design-and-validation-of-the-first-cell-impermeant-melatonin-receptor-agonist
#11
Florence Gbahou, Erika Cecon, Guillaume Viault, Romain Gerbier, Frederic Jean-Alphonse, Angeliki Karamitri, Gérald Guillaumet, Philippe Delagrange, Robert M Friedlander, Jean-Pierre Vilardaga, Franck Suzenet, Ralf Jockers
BACKGROUND AND PURPOSE: The paradigm that G protein-coupled receptors are able to prolong or initiate cellular signaling through intracellular receptors recently emerged. Melatonin binds to G protein-coupled MT1 and MT2 receptors. Different from most other hormones targeting GPCRs, melatonin and its synthetic analogs are amphiphilic molecules easily penetrating into cells, but the existence of intracellular receptors is still unclear mainly due to a lack of appropriate tools. EXPERIMENTAL APPROACH: We therefore designed and synthesized a series of hydrophilic melatonin receptor ligands coupled to the Cy3 cyanin fluorophore to reliably monitor its inability of cellular penetration...
May 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28489379/hydroxy-substituted-heteroarylpiperazines-novel-scaffolds-for-%C3%AE-arrestin-biased-d2r-agonists
#12
Barbara Männel, Daniela Dengler, Jeremy Shonberg, Harald Hübner, Dorothee Möller, Peter Gmeiner
By means of a formal structural hybridization of the antipsychotic drug aripiprazole and the heterocyclic catecholamine surrogates present in the β2-adrenoceptor agonists procaterol and BI-167107 (4), we designed and synthesized a collection of novel hydroxy-substituted heteroarylpiperazines and heteroarylhomopiperazines with high dopamine D2 receptor (D2R) affinity. In contrast to the weak agonistic behavior of aripiprazole, these ligands are capable of effectively mimicking those interactions of dopamine and the D2R that are crucial for an active state, leading to the recruitment of β-arrestin-2...
May 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28484426/structural-functional-features-of-the-thyrotropin-receptor-a-class-a-g-protein-coupled-receptor-at-work
#13
REVIEW
Gunnar Kleinau, Catherine L Worth, Annika Kreuchwig, Heike Biebermann, Patrick Marcinkowski, Patrick Scheerer, Gerd Krause
The thyroid-stimulating hormone receptor (TSHR) is a member of the glycoprotein hormone receptors, a sub-group of class A G-protein-coupled receptors (GPCRs). TSHR and its endogenous ligand thyrotropin (TSH) are of essential importance for growth and function of the thyroid gland and proper function of the TSH/TSHR system is pivotal for production and release of thyroid hormones. This receptor is also important with respect to pathophysiology, such as autoimmune (including ophthalmopathy) or non-autoimmune thyroid dysfunctions and cancer development...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28482214/active-state-structures-of-g-protein-coupled-receptors-highlight-the-similarities-and-differences-in-the-g-protein-and-arrestin-coupling-interfaces
#14
REVIEW
Byron Carpenter, Christopher G Tate
G protein-coupled receptors (GPCRs) regulate cellular signalling through heterotrimeric G proteins and arrestins in response to an array of extracellular stimuli. Structure determination of GPCRs in an active conformation bound to intracellular signalling proteins has proved to be highly challenging. Nonetheless, three new structures of GPCRs in an active state have been published during the last year, namely the adenosine A2A receptor (A2AR) bound to an engineered G protein, opsin bound to visual arrestin and the μ opioid receptor (μOR) bound to a G protein-mimicking nanobody...
May 5, 2017: Current Opinion in Structural Biology
https://www.readbyqxmd.com/read/28478994/emerging-paradigms-of-g-protein-coupled-receptor-dephosphorylation
#15
REVIEW
Andrea Kliewer, Rainer K Reinscheid, Stefan Schulz
Elucidation of the molecular mechanisms underlying G protein-coupled receptor (GPCR) dephosphorylation remains a major challenge. While specific GPCR phosphatases (GRPs) have eluded identification, prevailing models propose that receptors must first internalize into acidic endosomes to become dephosphorylated in a housekeeping-like process. Recently, phosphosite-specific antibodies, combined with siRNAs targeting specific phosphatase transcripts, have facilitated the identification of distinct protein phosphatase 1 (PP1) and PP2 catalytic subunits as bona fide GRPs...
May 4, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28476928/the-selexipag-active-metabolite-act-333679-displays-strong-anti-contractile-and-anti-remodeling-effects-but-low-%C3%AE-arrestin-recruitment-and-desensitization-potential
#16
John Gatfield, Katalin Menyhart, Daniel Wanner, Carmela Gnerre, Lucile Monnier, Keith Morrison, Patrick Hess, Marc Iglarz, Martine Clozel, Oliver Nayler
Prostacyclin (PGI2) receptor (IP receptor) agonists, which are indicated for the treatment of pulmonary arterial hypertension (PAH), increase cytosolic cAMP levels and thereby inhibit pulmonary vasoconstriction, pulmonary arterial smooth muscle cell (PASMC) proliferation and extracellular matrix synthesis. Selexipag (Uptravi(®)) is the first non-prostanoid IP receptor agonist, it is available orally and was recently approved for the treatment of PAH. In this study we show that the active metabolite of selexipag and the main contributor to clinical efficacy, ACT-333679 (previously known as MRE-269), behaved as full agonist in multiple PAH-relevant receptor-distal - or downstream - cellular readouts with a maximal efficacy comparable to that of the prototypic PGI2 analog iloprost: In PASMC, ACT-333679 potently induced cellular relaxation (EC50=4...
May 5, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28473212/hepatocellular-adenoma-in-a-european-flatfish-limanda-limanda-genetic-alterations-in-laser-capture-micro-dissected-tissue-and-global-transcriptomic-approach
#17
Adélaïde Lerebours, Emma Chapman, Brett P Lyons, John P Bignell, Grant D Stentiford, Jeanette M Rotchell
Liver tumours in flatfish have been diagnosed using histopathology for decades to monitor the impacts of marine pollution. Here we describe the application of specific gene (retinoblastoma, Rb) profiling in laser capture micro-dissected samples, and a suppression subtractive hybridization (SSH) approach to isolate differentially expressed genes in hepatocellular adenoma (HCA) samples from dab, Limanda limanda. The Rb profiles from apparently normal and HCA micro-dissected samples of fish from the North Sea showed no significant difference, and genotypic heterogeneity within defined histological phenotypes was observed...
May 1, 2017: Marine Pollution Bulletin
https://www.readbyqxmd.com/read/28472170/two-serines-in-the-distal-c-terminus-of-the-human-%C3%A3-1-adrenoceptor-determine-%C3%A3-arrestin2-recruitment
#18
Laura Hinz, Andrea Ahles, Benjamin Ruprecht, Bernhard Küster, Stefan Engelhardt
G protein-coupled receptors (GPCRs) undergo phosphorylation at several intracellular residues by G protein-coupled receptor kinases. The resulting phosphorylation pattern triggers arrestin recruitment and receptor desensitization. The exact sites of phosphorylation and their function remained largely unknown for the human β1-adrenoceptor (ADRB1), a key GPCR in adrenergic signal transduction and the target of widely used drugs such as β-blockers. The present study aimed to identify the intracellular phosphorylation sites in the ADRB1 and to delineate their function...
2017: PloS One
https://www.readbyqxmd.com/read/28468964/luminal-angiotensin-ii-is-internalized-as-a-complex-with-at1r-at2r-heterodimers-to-target-endoplasmic-reticulum-in-llc-pk1-cells
#19
Fernanda M Ferrão, Luiza H D Cardoso, Heather A Drummond, Xiao C Li, Jia L Zhuo, Dayene S Gomes, Lucienne S Lara, Adalberto Vieyra, Jennifer Lowe
Angiotensin II (ANG II) has many biological effects in renal physiology, particularly in Ca(2+) handling in the regulation of fluid and solute reabsorption. It involves the systemic endocrine renin-angiotensin system (RAS), but tissue and intracrine ANG II are also known. We have shown that ANG II induces heterodimerization of its AT1 and AT2 receptors (AT1R and AT2R) to stimulate sarco(endo)plasmic reticulum Ca(2+)-ATPase (SERCA) activity. Thus, we investigated whether ANG II-AT1R/AT2R complex is formed and internalized, and also looked at the intracellular localization of this complex to determine how its effect might be exerted on renal intracrine RAS...
May 3, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28468835/multilevel-regulation-of-an-%C3%AE-arrestin-by-glucose-depletion-controls-hexose-transporter-endocytosis
#20
Junie Hovsepian, Quentin Defenouillère, Véronique Albanèse, Libuše Váchová, Camille Garcia, Zdena Palková, Sébastien Léon
Nutrient availability controls the landscape of nutrient transporters present at the plasma membrane, notably by regulating their ubiquitylation and subsequent endocytosis. In yeast, this involves the Nedd4 ubiquitin ligase Rsp5 and arrestin-related trafficking adaptors (ARTs). ARTs are targeted by signaling pathways and warrant that cargo ubiquitylation and endocytosis appropriately respond to nutritional inputs. Here, we show that glucose deprivation regulates the ART protein Csr2/Art8 at multiple levels to trigger high-affinity glucose transporter endocytosis...
May 3, 2017: Journal of Cell Biology
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