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GPCR signaling

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https://www.readbyqxmd.com/read/28216047/serotonin-2a-homodimers-are-needed-for-signalling-via-both-phospholipase-a2-and-phospholipase-c-in-transfected-cho-cells
#1
Alba Iglesias, Marta Cimadevila, María Isabel Cadavid, María Isabel Loza, José Brea
Different ligands differentially activate phospholipase A2 (PLA2) and phospholipase C (PLC) signalling pathways that are coupled to the serotonin 2A (5-HT2A) receptor, a class-A G-protein coupled receptor (GPCR). The serotonin 5-HT2A receptor has been shown to be expressed as a homodimer displaying some ligands negative cooperativity between protomers in the PLA2 signalling pathway. We hypothesized that the homodimeric complex is the minimum functional unit required for activation of the PLA2 and PLC pathways by the serotonin 5-HT2A receptor...
February 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28215292/emergent-role-of-coronin-1a-in-neuronal-signaling
#2
M Martorella, K Barford, B Winkler, C D Deppmann
The Coronin family of proteins were first noted for their role in pathogen-host interactions and for modulating actin dynamics. Recently, however, Coronins have been found in a greater variety of cell types, and novel roles for the Coronins within the nervous system have been discovered. In the immune system, Coronin-1a enables Mycobacterium tuberculosis to evade lysosomal destruction. This activity appears to be analogous to protection of the NGF-TrkA signaling endosome during sympathetic nervous system development that is required for survival signaling...
2017: Vitamins and Hormones
https://www.readbyqxmd.com/read/28213525/conformational-profiling-of-the-at1-angiotensin-ii-receptor-reflects-biased-agonism-g-protein-coupling-and-cellular-context
#3
Dominic Devost, Rory Sleno, Darlaine Petrin, Alice Zhang, Yuji Shinjo, Rakan Okde, Junken Aoki, Asuka Inoue, Terence E Hebert
Here, we report the design and use of GPCR-based biosensors to monitor ligand-mediated conformational changes in receptors in intact cells. These biosensors use Bioluminescence Resonance Energy Transfer (BRET) with Renilla luciferase (RlucII) as an energy donor, placed at the distal end of the receptor C-tail and the small fluorescent molecule FlAsH, as an energy acceptor, its binding site inserted at different positions throughout the intracellular loops and carboxy-terminal tail of the angiotensin II type I receptor (AT1R)...
February 17, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28213524/g-protein-coupled-receptor-kinase-2-grk-2-regulates-serotonin-metabolism-through-the-monoamine-oxidase-amx-2-in-caenorhabditis-elegans
#4
Jianjun Wang, Jiansong Luo, Dipendra K Aryal, William C Wetzel, Richard Nass, Jeffrey L Benovic
G protein-coupled receptors (GPCRs) regulate many animal behaviors. GPCR signaling is mediated by agonist-promoted interactions of GPCRs with heterotrimeric G proteins, GPCR kinases (GRKs) and arrestins. To further elucidate the role of GRKs in regulating GPCR-mediated behaviors, we utilized the genetic model system Caenorhabditis elegans. Our studies demonstrate that grk-2 loss-of-function strains are egg-laying defective and contain low levels of serotonin (5-HT) and high levels of the 5-HT metabolite 5-hydroxyindole acetic acid (5-HIAA)...
February 17, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28209512/n-glycan-dependent-cell-surface-expression-of-the-p2y2-receptor-and-n-glycan-independent-distribution-to-lipid-rafts
#5
Tetsuto Nakagawa, Chihiro Takahashi, Hitomi Matsuzaki, Shohei Takeyama, Shinpei Sato, Ayaka Sato, Yoshiyuki Kuroda, Hideyoshi Higashi
P2Y2 receptor (P2Y2R) is a G-protein-coupled receptor (GPCR) that couples with Gαq/11 and is stimulated by ATP and UTP. P2Y2R is involved in pain, proinflammatory changes, and blood pressure control. Some GPCRs are localized in lipid rafts for interaction with other signaling molecules. In this study, we prepared N-glycan-deficient mutants by mutating the two consensus Asn residues for N-glycosylation to Gln to examine intracellular localization and association with lipid rafts. Western blotting of the wild type (WT) protein and mutants (N9Q, N13Q, N9Q/N13Q) in COS-7 cells showed that both Asn residues were glycosylated in the WT...
February 14, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28195946/g-protein-coupled-receptor-mediated-transactivation-of-extracellular-proteases
#6
Allison E Schafer, Burns C Blaxall
G protein-coupled receptors (GPCRs) comprise the largest family of receptors in humans. Traditional activation of GPCRs involves binding of a ligand to the receptor, activation of heterotrimeric G proteins and induction of subsequent signaling molecules. It is now known that GPCR signaling occurs through G protein-independent pathways including signaling through β-arrestin as well as transactivation of other receptor types. Generally, transactivation occurs when activation of one receptor leads to the activation of another receptor(s)...
February 13, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28195188/sumo-regulates-the-activity-of-smoothened-and-costal-2-in-drosophila-hedgehog-signaling
#7
Jie Zhang, Yajuan Liu, Kai Jiang, Jianhang Jia
In Hedgehog (Hh) signaling, the GPCR-family protein Smoothened (Smo) acts as a signal transducer that is regulated by phosphorylation and ubiquitination, which ultimately change the cell surface accumulation of Smo. However, it is not clear whether Smo is regulated by other post-translational modifications, such as sumoylation. Here, we demonstrate that knockdown of the small ubiquitin-related modifier (SUMO) pathway components Ubc9 (a SUMO-conjugating enzyme E2), PIAS (a SUMO-protein ligase E3), and Smt3 (the SUMO isoform in Drosophila) by RNAi prevents Smo accumulation and alters Smo activity in the wing...
February 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28188824/the-g-protein-coupled-receptor-n-terminus-and-receptor-signalling-n-tering-a-new-era
#8
REVIEW
James L J Coleman, Tony Ngo, Nicola J Smith
G protein-coupled receptors (GPCRs) are a vast family of membrane-traversing proteins, essential to the ability of eukaryotic life to detect, and mount an intracellular response to, a diverse range of extracellular stimuli. GPCRs have evolved with archetypal features including an extracellular N-terminus and intracellular C-terminus that flank a transmembrane structure of seven sequential helices joined by intracellular and extracellular loops. These structural domains contribute to the ability of a GPCR to be correctly synthesised and inserted into the cell membrane, to interact with its cognate ligand(s) and to couple with signal-transducing heterotrimeric G proteins, allowing the activated receptor to selectively modulate a number of signalling cascades...
February 8, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28182309/propagation-of-the-allosteric-modulation-induced-by-sodium-in-the-%C3%AE-opioid-receptor
#9
Xianqiang Sun, Genevieve Laroche, Xu Wang, Hans Ågren, Greg Bowman, Patrick M Giguère, Yaoquan Tu
Allosteric sodium in the helix bundle of a G protein-coupled receptor (GPCR) can modulate the receptor activation on the intracellular side. This phenomenon has confounded the GPCR community for decades. In this work, we present a theoretical model that reveals the mechanism of the allosteric modulation induced by sodium in the δ opioid receptor. We found that the allosteric sodium ion exploits a distinct conformation of the key residue Trp2746.48 to propagate the modulation to helixes 5 and 6, which further transmits along the helixes and regulates their positions on the intracellular side...
February 9, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28181555/determination-of-biological-activity-of-gonadotropins-hcg-and-fsh-by-f%C3%A3-rster-resonance-energy-transfer-based-biosensors
#10
Olga Mazina, Anni Allikalt, Juha S Tapanainen, Andres Salumets, Ago Rinken
Determination of biological activity of gonadotropin hormones is essential in reproductive medicine and pharmaceutical manufacturing of the hormonal preparations. The aim of the study was to adopt a G-protein coupled receptor (GPCR)-mediated signal transduction pathway based assay for quantification of biological activity of gonadotropins. We focussed on studying human chorionic gonadotropin (hCG) and follicle-stimulating hormone (FSH), as these hormones are widely used in clinical practice. Receptor-specific changes in cellular cyclic adenosine monophosphate (cAMP, second messenger in GPCR signalling) were monitored by a Förster resonance energy transfer (FRET) biosensor protein (T)Epac(VV) in living cells upon activation of the relevant gonadotropin receptor...
February 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28181498/arrestin-biased-at1r-agonism-induces-acute-catecholamine-secretion-through-trpc3-coupling
#11
Chun-Hua Liu, Zheng Gong, Zong-Lai Liang, Zhi-Xin Liu, Fan Yang, Yu-Jing Sun, Ming-Liang Ma, Yi-Jing Wang, Chao-Ran Ji, Yu-Hong Wang, Mei-Jie Wang, Fu-Ai Cui, Amy Lin, Wen-Shuai Zheng, Dong-Fang He, Chang-Xiu Qu, Peng Xiao, Chuan-Yong Liu, Alex R B Thomsen, Thomas Joseph Cahill, Alem W Kahsai, Fan Yi, Kun-Hong Xiao, Tian Xue, Zhuan Zhou, Xiao Yu, Jin-Peng Sun
Acute hormone secretion triggered by G protein-coupled receptor (GPCR) activation underlies many fundamental physiological processes. GPCR signalling is negatively regulated by β-arrestins, adaptor molecules that also activate different intracellular signalling pathways. Here we reveal that TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), stimulates acute catecholamine secretion through coupling with the transient receptor potential cation channel subfamily C 3 (TRPC3)...
February 9, 2017: Nature Communications
https://www.readbyqxmd.com/read/28174684/sucralose-activates-an-erk1-2-ribosomal-protein-s6-signaling-axis
#12
Marcy L Guerra, Michael A Kalwat, Kathleen McGlynn, Melanie H Cobb
The sweetener sucralose can signal through its GPCR receptor to induce insulin secretion from pancreatic β cells, but the downstream signaling pathways involved are not well-understood. Here we measure responses to sucralose, glucagon-like peptide 1, and amino acids in MIN6 β cells. Our data suggest a signaling axis, whereby sucralose induces calcium and cAMP, activation of ERK1/2, and site-specific phosphorylation of ribosomal protein S6. Interestingly, sucralose acted independently of mTORC1 or ribosomal S6 kinase (RSK)...
February 2017: FEBS Open Bio
https://www.readbyqxmd.com/read/28174517/a-practical-guide-to-approaching-biased-agonism-at-g-protein-coupled-receptors
#13
Jaimee Gundry, Rachel Glenn, Priya Alagesan, Sudarshan Rajagopal
Biased agonism, the ability of a receptor to differentially activate downstream signaling pathways depending on binding of a "biased" agonist compared to a "balanced" agonist, is a well-established paradigm for G protein-coupled receptor (GPCR) signaling. Biased agonists have the promise to act as smarter drugs by specifically targeting pathogenic or therapeutic signaling pathways while avoiding others that could lead to side effects. A number of biased agonists targeting a wide array of GPCRs have been described, primarily based on their signaling in pharmacological assays...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28174117/%C3%AE-arrestin-signalling-and-bias-in-hormone-responsive-gpcrs
#14
Eric Reiter, Mohammed Akli Ayoub, Lucie P Pellissier, Flavie Landomiel, Astrid Musnier, Aurélie Tréfier, Jorge Gandia, Francesco De Pascali, Shifa Tahir, Romain Yvinec, Gilles Bruneau, Anne Poupon, Pascale Crépieux
G protein-coupled receptors (GPCRs) play crucial roles in the ability of target organs to respond to hormonal cues. GPCRs' activation mechanisms have long been considered as a two-state process connecting the agonist-bound receptor to heterotrimeric G proteins. This view is now challenged as mounting evidence point to GPCRs being connected to large arrays of transduction mechanisms involving heterotrimeric G proteins as well as other players. Amongst the G protein-independent transduction mechanisms, those elicited by β-arrestins upon their recruitment to the active receptors are by far the best characterized and apply to most GPCRs...
February 4, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28169830/phosphorylation-of-%C3%AE-arrestin-2-at-thr-383-by-mek-underlies-%C3%AE-arrestin-dependent-activation-of-erk1-2-by-gpcrs
#15
Elisabeth Cassier, Nathalie Gallay, Thomas Bourquard, Sylvie Claeysen, Joël Bockaert, Pascale Crépieux, Anne Poupon, Eric Reiter, Philippe Marin, Franck Vandermoere
In addition to their role in desensitization and internalization of G protein-coupled receptors (GPCRs), β-arrestins are essential scaffolds linking GPCRs to Erk1/2 signaling. However, their role in GPCR-operated Erk1/2 activation differs between GPCRs and the underlying mechanism remains poorly characterized. Here, we show that activation of serotonin 5-HT2C receptors, which engage Erk1/2 pathway via a β-arrestin-dependent mechanism, promotes MEK-dependent β-arrestin 2 phosphorylation at Thr(383), a necessary step for Erk recruitment to the receptor/β-arrestin complex and Erk activation...
February 7, 2017: ELife
https://www.readbyqxmd.com/read/28168348/insights-into-cellular-signalling-by-g-protein-coupled-receptor-transactivation-of-cell-surface-protein-kinase-receptors
#16
REVIEW
Rebecca Chaplin, Lyna Thach, Morley D Hollenberg, Yingnan Cao, Peter J Little, Danielle Kamato
G protein coupled receptor (GPCR) signalling is mediated by transactivation independent and transactivation dependent pathways. GPCRs transactivate protein tyrosine kinase receptors (PTKRs) and protein serine/threonine kinase receptors (PS/TKR). Since the initial observations of transactivation dependent signalling, there has been an effort to understand the mechanisms behind this phenomena. GPCR signalling has evolved to include biased signalling. Biased signalling, whereby selected ligands can activate the same GPCR that can generate multiple signals, but drive only a unique response...
February 6, 2017: Journal of Cell Communication and Signaling
https://www.readbyqxmd.com/read/28167604/gs-dreadd-knock-in-mice-for-tissue-specific-temporal-stimulation-of-camp-signaling
#17
Dmitry Akhmedov, Maria G Mendoza-Rodriguez, Kavitha Rajendran, Mario Rossi, Jürgen Wess, Rebecca Berdeaux
Hundreds of hormones and ligands stimulate cAMP signaling in different tissues through activation of G protein-coupled receptors (GPCRs). Although functions and individual effectors of cAMP signaling are well characterized in many tissues, pleiotropic effects of GPCR agonists limit investigation of physiologic functions of cAMP signaling in individual cell types at different developmental stages in vivo To facilitate studies of cAMP signaling in specific cell populations in vivo, we harnessed the power of DREADD (Designer Receptors Exclusively Activated by Designer Drugs) technology by creating ROSA26-based knock-in mice for conditional expression of a Gs-coupled DREADD (rM3Ds-GFP, or "GsD")...
February 6, 2017: Molecular and Cellular Biology
https://www.readbyqxmd.com/read/28167537/site-specific-o-glycosylation-by-polypeptide-galnac-transferase-t2-co-regulates-beta1-adrenergic-receptor-n-terminal-cleavage
#18
Christoffer K Goth, Hanna E Tuhkanen, Hamayun Khan, Jarkko J Lackman, Shengjun Wang, Yoshiki Narimatsu, Lasse Holst Hansen, Christopher Overall, Henrik Clausen, Katrine T Schjoldager, Ulla E Petäjä-Repo
The β1-adrenergic receptor (β1AR) is a G protein-coupled receptor (GPCR) and the predominant adrenergic receptor subtype in the heart, where it mediates cardiac contractility and the force of contraction. Although it is the most important target for β-adrenergic antagonists, such as beta-blockers, relatively little is still known about its regulation. We have previously shown that β1AR undergoes constitutive and regulated N-terminal cleavage participating in receptor down-regulation, and moreover that the receptor is modified by O-glycosylation...
February 6, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28163240/cardiomyopathy-an-approach-to-the-autoimmune-background
#19
REVIEW
Niels-Peter Becker, Johannes Müller, Gerd Wallukat, Ingolf Schimke
Autoimmunity is increasingly accepted as the origin or amplifier of various diseases. In contrast to classic autoantibodies (AABs), which induce immune responses resulting in the destruction of the affected tissue, an additional class of AABs is directed against G-protein-coupled receptors (GPCRs; GPCR-AABs). GPCR-AABs functionally affect their related GPCRs for activation of receptor mediated signal cascades. Diseases which are characterized by the presence of GPCR-AABs with evidence for disease-specific pathogenic activity could be named "functional autoantibody disease"...
February 2, 2017: Autoimmunity Reviews
https://www.readbyqxmd.com/read/28159877/g-protein-coupled-receptor-signaling-in-cilia
#20
Kirk Mykytyn, Candice Askwith
G-protein-coupled receptors (GPCRs) are the largest and most versatile family of signaling receptors in humans. They respond to diverse external signals, such as photons, proteins, peptides, chemicals, hormones, lipids, and sugars, and mediate a myriad of functions in the human body. Signaling through GPCRs can be optimized by enriching receptors and downstream effectors in discrete cellular domains. Many GPCRs have been found to be selectively targeted to cilia on numerous mammalian cell types. Moreover, investigations into the pathophysiology of human ciliopathies have implicated GPCR ciliary signaling in a number of developmental and cellular pathways...
February 3, 2017: Cold Spring Harbor Perspectives in Biology
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