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https://www.readbyqxmd.com/read/28440799/corrigendum-kif3a-binds-to-%C3%AE-arrestin-for-suppressing-wnt-%C3%AE-catenin-signalling-independently-of-primary-cilia-in-lung-cancer
#1
Minsuh Kim, Young-Ah Suh, Ju-Hee Oh, Bo Ra Lee, Joon Kim, Se Jin Jang
No abstract text is available yet for this article.
April 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28431242/structural-and-functional-analysis-of-a-%C3%AE-2-adrenergic-receptor-complex-with-grk5
#2
Konstantin E Komolov, Yang Du, Nguyen Minh Duc, Robin M Betz, João P G L M Rodrigues, Ryan D Leib, Dhabaleswar Patra, Georgios Skiniotis, Christopher M Adams, Ron O Dror, Ka Young Chung, Brian K Kobilka, Jeffrey L Benovic
The phosphorylation of agonist-occupied G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) functions to turn off G-protein signaling and turn on arrestin-mediated signaling. While a structural understanding of GPCR/G-protein and GPCR/arrestin complexes has emerged in recent years, the molecular architecture of a GPCR/GRK complex remains poorly defined. We used a comprehensive integrated approach of cross-linking, hydrogen-deuterium exchange mass spectrometry (MS), electron microscopy, mutagenesis, molecular dynamics simulations, and computational docking to analyze GRK5 interaction with the β2-adrenergic receptor (β2AR)...
April 20, 2017: Cell
https://www.readbyqxmd.com/read/28427767/%C3%AE-arrestins-negatively-control-human-adrenomedullin-type-1-receptor-internalization
#3
Kenji Kuwasako, Kazuo Kitamura, Sayaka Nagata, Toshio Sekiguchi, Jiang Danfeng, Manabu Murakami, Yuichi Hattori, Johji Kato
Adrenomedullin (AM) is a potent hypotensive peptide that exerts a powerful variety of protective effects against multiorgan damage through the AM type 1 receptor (AM1 receptor), which consists of the calcitonin receptor-like receptor (CLR) and receptor activity-modifying protein 2 (RAMP2). Two β-arrestin (β-arr) isoforms, β-arr-1 and β-arr-2, play a central role in the agonist-induced internalization of many receptors for receptor resensitization. Notably, β-arr-biased agonists are now being tested in phase II clinical trials, targeting acute pain and acute heart failure...
April 17, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28424471/human-luteinizing-hormone-and-chorionic-gonadotropin-display-biased-agonism-at-the-lh-and-lh-cg-receptors
#4
Laura Riccetti, Romain Yvinec, Danièle Klett, Nathalie Gallay, Yves Combarnous, Eric Reiter, Manuela Simoni, Livio Casarini, Mohammed Akli Ayoub
Human luteinizing hormone (LH) and chorionic gonadotropin (hCG) have been considered biologically equivalent because of their structural similarities and their binding to the same receptor; the LH/CGR. However, accumulating evidence suggest that LH/CGR differentially responds to the two hormones triggering differential intracellular signaling and steroidogenesis. The mechanistic basis of such differential responses remains mostly unknown. Here, we compared the abilities of recombinant rhLH and rhCG to elicit cAMP, β-arrestin 2 activation, and steroidogenesis in HEK293 cells and mouse Leydig tumor cells (mLTC-1)...
April 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28424266/disease-associated-extracellular-loop-mutations-in-the-adhesion-g-protein-coupled-receptor-g1-adgrg1-gpr56-differentially-regulate-downstream-signaling
#5
Ayush Kishore, Randy A Hall
Mutations to the adhesion G protein-coupled receptor ADGRG1 (G1; also known as GPR56) underlie the neurological disorder bilateral frontoparietal polymicrogyria (BFPP). Disease-associated mutations in G1 studied to date are believed to induce complete loss of receptor function, either through disruption of receptor trafficking or signaling activity. Given that N-terminal truncation of G1 and other adhesion G protein-coupled receptors has been shown to significantly increase the receptors' constitutive signaling, we examined two different BFPP-inducing extracellular loop mutations (R565W and L640R) in the context of both full-length and N-terminally truncated (deltaNT) G1...
April 19, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28419873/arrestin-2-and-arrestin-3-differentially-modulate-locomotor-responses-and-sensitization-to-amphetamine
#6
Lilia Zurkovsky, Katayoun Sedaghat, M Rafiuddin Ahmed, Vsevolod V Gurevich, Eugenia V Gurevich
Arrestins play a prominent role in shutting down signaling via G protein-coupled receptors. In recent years, a signaling role for arrestins independent of their function in receptor desensitization has been discovered. Two ubiquitously expressed arrestin isoforms, arrestin-2 and arrestin-3, perform similarly in the desensitization process and share many signaling functions, enabling them to substitute for one another. However, signaling roles specific to each isoform have also been described. Mice lacking arrestin-3 (ARR3KO) were reported to show blunted acute responsiveness to the locomotor stimulatory effect of amphetamine (AMPH)...
April 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28416805/a-new-inhibitor-of-the-%C3%AE-arrestin-ap2-endocytic-complex-reveals-interplay-between-gpcr-internalization-and-signalling
#7
Alexandre Beautrait, Justine S Paradis, Brandon Zimmerman, Jenna Giubilaro, Ljiljana Nikolajev, Sylvain Armando, Hiroyuki Kobayashi, Lama Yamani, Yoon Namkung, Franziska M Heydenreich, Etienne Khoury, Martin Audet, Philippe P Roux, Dmitry B Veprintsev, Stéphane A Laporte, Michel Bouvier
In addition to G protein-coupled receptor (GPCR) desensitization and endocytosis, β-arrestin recruitment to ligand-stimulated GPCRs promotes non-canonical signalling cascades. Distinguishing the respective contributions of β-arrestin recruitment to the receptor and β-arrestin-promoted endocytosis in propagating receptor signalling has been limited by the lack of selective analytical tools. Here, using a combination of virtual screening and cell-based assays, we have identified a small molecule that selectively inhibits the interaction between β-arrestin and the β2-adaptin subunit of the clathrin adaptor protein AP2 without interfering with the formation of receptor/β-arrestin complexes...
April 18, 2017: Nature Communications
https://www.readbyqxmd.com/read/28406627/diindolylmethane-derivatives-potent-agonists-of-the-immunostimulatory-orphan-g-protein-coupled-receptor-gpr84
#8
Thanigaimalai Pillaiyar, Meryem Köse, Katharina Sylvester, Heike Weighardt, Dominik Thimm, Gleice Borges, Irmgard Förster, Ivar von Kügelgen, Christa E Müller
The Gi protein-coupled receptor GPR84, which is activated by (hydroxy)fatty acids, is highly expressed on immune cells. Recently 3,3'-diindolylmethane was identified as a heterocyclic, non-lipid-like GPR84 agonist. We synthesized a broad range of diindolylmethane derivatives by condensation of indoles with formaldehyde in water under microwave irradiation. The products were evaluated at the human GPR84 in cAMP and β-arrestin assays. Structure-activity relationships (SARs) were steep. 3,3'-Diindolylmethanes bearing small lipophilic residues at the 5- and/or 7-position of the indole rings displayed the highest activity in cAMP assays, the most potent agonists being di-(5-fluoro-1H-indole-3-yl)methane (38, PSB-15160, EC50 80...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28400916/angiotensin-receptor-blocker-drugs-and-inhibition-of-adrenal-beta-arrestin-1-dependent-aldosterone-production-implications-for-heart-failure-therapy
#9
EDITORIAL
Anastasios Lymperopoulos, Beatrix Aukszi
Aldosterone mediates many of the physiological and pathophysiological/cardio-toxic effects of angiotensin II (AngII). Its synthesis and secretion from the zona glomerulosa cells of the adrenal cortex, elevated in chronic heart failure (HF), is induced by AngII type 1 receptors (AT1Rs). The AT1R is a G protein-coupled receptor, mainly coupling to Gq/11 proteins. However, it can also signal through β-arrestin-1 (βarr1) or -2 (βarr2), both of which mediate G protein-independent signaling. Over the past decade, a second, Gq/11 protein-independent but βarr1-dependent signaling pathway emanating from the adrenocortical AT1R and leading to aldosterone production has become appreciated...
March 26, 2017: World Journal of Cardiology
https://www.readbyqxmd.com/read/28399904/separation-of-photoreceptor-cell-compartments-in-mouse-retina-for-protein-analysis
#10
Kasey Rose, Steven T Walston, Jeannie Chen
BACKGROUND: Light exposure triggers movement of certain signaling proteins within the cellular compartments of the highly polarized rod photoreceptor cell. This redistribution of proteins between the inner and outer segment compartments affects the performance and physiology of the rod cell. In addition, newly synthesized phototransduction proteins traverse from the site of their synthesis in the inner segment, through the thin connecting cilium, to reach their destination in the outer segment...
April 11, 2017: Molecular Neurodegeneration
https://www.readbyqxmd.com/read/28394950/generation-and-characterization-of-an-antagonistic-monoclonal-antibody-against-an-extracellular-domain-of-mouse-dp2-crth2-gpr44-receptors-for-prostaglandin-d2
#11
Nanae Nagata, Hiroko Iwanari, Hidetoshi Kumagai, Osamu Kusano-Arai, Yuichi Ikeda, Kosuke Aritake, Takao Hamakubo, Yoshihiro Urade
Prostaglandin D2 (PGD2) is a lipid mediator involved in sleep regulation and inflammation. PGD2 interacts with 2 types of G protein-coupled receptors, DP1 and DP2/CRTH2 (chemoattractant receptor homologous molecule expressed on T helper type 2 cells)/GPR44 to show a variety of biological effects. DP1 activation leads to Gs-mediated elevation of the intracellular cAMP level, whereas activation of DP2 decreases this level via the Gi pathway; and it also induces G protein-independent, arrestin-mediated cellular responses...
2017: PloS One
https://www.readbyqxmd.com/read/28384160/a-wnt-planar-polarity-pathway-instructs-neurite-branching-by-restricting-f-actin-assembly-through-endosomal-signaling
#12
Chun-Hao Chen, Chun-Wei He, Chien-Po Liao, Chun-Liang Pan
Spatial arrangement of neurite branching is instructed by both attractive and repulsive cues. Here we show that in C. elegans, the Wnt family of secreted glycoproteins specify neurite branching sites in the PLM mechanosensory neurons. Wnts function through MIG-1/Frizzled and the planar cell polarity protein (PCP) VANG-1/Strabismus/Vangl2 to restrict the formation of F-actin patches, which mark branching sites in nascent neurites. We find that VANG-1 promotes Wnt signaling by facilitating Frizzled endocytosis and genetically acts in a common pathway with arr-1/β-arrestin, whose mutation results in defective PLM branching and F-actin patterns similar to those in the Wnt, mig-1 or vang-1 mutants...
April 2017: PLoS Genetics
https://www.readbyqxmd.com/read/28379944/structural-basis-for-selectivity-and-diversity-in-angiotensin-ii-receptors
#13
Haitao Zhang, Gye Won Han, Alexander Batyuk, Andrii Ishchenko, Kate L White, Nilkanth Patel, Anastasiia Sadybekov, Beata Zamlynny, Michael T Rudd, Kaspar Hollenstein, Alexandra Tolstikova, Thomas A White, Mark S Hunter, Uwe Weierstall, Wei Liu, Kerim Babaoglu, Eric L Moore, Ryan D Katz, Jennifer M Shipman, Margarita Garcia-Calvo, Sujata Sharma, Payal Sheth, Stephen M Soisson, Raymond C Stevens, Vsevolod Katritch, Vadim Cherezov
The angiotensin II receptors AT1R and AT2R serve as key components of the renin-angiotensin-aldosterone system. AT1R has a central role in the regulation of blood pressure, but the function of AT2R is unclear and it has a variety of reported effects. To identify the mechanisms that underlie the differences in function and ligand selectivity between these receptors, here we report crystal structures of human AT2R bound to an AT2R-selective ligand and to an AT1R/AT2R dual ligand, capturing the receptor in an active-like conformation...
April 20, 2017: Nature
https://www.readbyqxmd.com/read/28369721/biased-agonism-and-allosteric-modulation-of-gpr183-a-7tm-receptor-also-known-as-ebv-induced-ebi2
#14
Viktorija Daugvilaite, Christian Medom Madsen, Michael Lückmann, Clara Castello Echeverria, Andreas Walter Sailer, Thomas Michael Frimurer, Mette Marie Rosenkilde, Tau Benned-Jensen
BACKGROUND AND PURPOSE: The G protein-coupled receptor Epstein Barr virus-induced gene 2 (EBI2, also known as GPR183) is activated by oxysterols and plays a pivotal role for proper B cell migration during immune responses. While the molecular basis of agonist binding has been addressed in several studies, the concept of biased agonism of EBI2 has not been explored. EXPERIMENTAL APPROACH: We investigated the effects of the EBI2 endogenous agonist 7α,25-OHC on G protein-dependent and -independent pathways as well as sodium ion allosterism using site-directed mutagenesis and functional studies...
March 29, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28364251/allosteric-modulation-model-of-the-mu-opioid-receptor-by-herkinorin-a-potent-not-alkaloidal-agonist
#15
A F Marmolejo-Valencia, K Martínez-Mayorga
Modulation of opioid receptors is the primary choice for pain management and structural information studies have gained new horizons with the recently available X-ray crystal structures. Herkinorin is one of the most remarkable salvinorin A derivative with high affinity for the mu opioid receptor, moderate selectivity and lack of nitrogen atoms on its structure. Surprisingly, binding models for herkinorin are lacking. In this work, we explore binding models of herkinorin using automated docking, molecular dynamics simulations, free energy calculations and available experimental information...
March 31, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28363772/characterization-of-signal-bias-at-the-glp-1-receptor-induced-by-backbone-modification-of-glp-1
#16
Marlies V Hager, Lachlan Clydesdale, Samuel H Gellman, Patrick M Sexton, Denise Wootten
The glucagon-like peptide-1 receptor (GLP-1R) is a cla B G protein-coupled receptor that is a major therapeutic target for the treatment of type 2 diabetes. Activation of this receptor promotes insulin secretion and blood glucose regulation. The GLP-1R can initiate signaling through several intracellular pathways upon activation by GLP-1. GLP-1R ligands that preferentially stimulate subsets among the natural signaling pathways ("biased agonists") could be useful as tools for elucidating the consequences of specific pathways and might engender therapeutic agents with tailored effects...
March 28, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28356352/rearrangement-of-a-polar-core-provides-a-conserved-mechanism-for-constitutive-activation-of-class-b-g-protein-coupled-receptors
#17
Yanting Yin, Parker de Waal, Yuanzheng He, Li-Hua Zhao, Dehua Yang, Xiaoqing Cai, Yi Jiang, Karsten Melcher, Ming-Wei Wang, H Eric Xu
The glucagon receptor (GCGR) belongs to the secretin-like (class B) family of G protein-coupled receptors (GPCRs) and is activated by the peptide hormone, glucagon. The structures of an activated class B GPCR have remained unsolved, preventing a mechanistic understanding of how these receptors are activated. Using a combination of structural modeling and mutagenesis studies, we present here two modes of ligand-independent activation of GCGR. First, we identified a GCGR-specific hydrophobic lock comprising M338 and F345 within the IC3 loop and transmembrane helix 6 (TM6) and found that this lock stabilizes the TM6 helix in the inactive conformation...
March 29, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28346440/endocytic-proteins-are-partitioned-at-the-edge-of-the-clathrin-lattice-in-mammalian-cells
#18
Kem A Sochacki, Andrea M Dickey, Marie-Paule Strub, Justin W Taraska
Dozens of proteins capture, polymerize and reshape the clathrin lattice during clathrin-mediated endocytosis (CME). How or if this ensemble of proteins is organized in relation to the clathrin coat is unknown. Here, we map key molecules involved in CME at the nanoscale using correlative super-resolution light and transmission electron microscopy. We localize 19 different endocytic proteins (amphiphysin1, AP2, β2-arrestin, CALM, clathrin, DAB2, dynamin2, EPS15, epsin1, epsin2, FCHO2, HIP1R, intersectin, NECAP, SNX9, stonin2, syndapin2, transferrin receptor, VAMP2) on thousands of individual clathrin structures, generating a comprehensive molecular architecture of endocytosis with nanoscale precision...
April 2017: Nature Cell Biology
https://www.readbyqxmd.com/read/28345900/fluorescence-and-radiolabeling-of-lys-4-nle-17-30-hpp-yields-molecular-tools-for-the-npy-y4-receptor
#19
Stefanie Dukorn, Timo Littmann, Max Keller, Kilian Kuhn, Chiara Cabrele, Paul Baumeister, Günther Bernhardt, Armin Buschauer
The neuropeptide Y (NPY) Y4 receptor (Y4R) is involved in energy homeostasis and considered a potential drug target for the treatment of obesity. Only a few molecular tools, i.e., radiolabeled and fluorescent ligands, for the investigation of the Y4R were reported. Previously, [Lys(4)]hPP proved to be an appropriate full-length PP analog to prepare a fluorescent ligand by derivatization at the ε-amino group. To preclude oxidation upon long-term storage, we replaced the two methionine residues in [Lys(4)]hPP by norleucine and prepared the corresponding [(3)H]propionylated ([(3)H]12) and cyanine labeled (13) peptides, which were characterized and compared with a set of reference compounds in binding (Y1, Y2, Y4, and Y5 receptors) and functional (luciferase gene reporter, beta-arrestin-1,2) Y4R assays...
April 5, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28345375/the-chemo-prophylactic-efficacy-of-an-ethanol-moringa-oleifera-leaf-extract-against-hepatocellular-carcinoma-in-rats
#20
Kadry M Sadek, Tarek K Abouzed, Reham Abouelkhair, Sherif Nasr
CONTEXT: Hepatocellular carcinoma (HCC) is among the most well-known threatening tumours around the world, and the outlook remains bleak. Moringa oleifera Lam. (Moringaceae) exhibits antitumor, antioxidant and hepatoprotective properties. OBJECTIVES: To assess the chemo-prophylactic proficiency and other likely activities of Moringa oleifera leaf ethanol extract (MOLEE) against diethyl nitrosamine (DEN)-induced HCC. MATERIALS AND METHODS: Wistar rats were gastrogavaged with MOLEE (500 mg/kg) for one week and then gastrogavaged with MOLEE and DEN (10 mg/kg) for the following 16 weeks...
December 2017: Pharmaceutical Biology
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