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https://www.readbyqxmd.com/read/29346437/tissue-specific-transcriptome-analyses-provide-new-insights-into-gpcr-signalling-in-adult-schistosoma-mansoni
#1
REVIEW
Steffen Hahnel, Nic Wheeler, Zhigang Lu, Arporn Wangwiwatsin, Paul McVeigh, Aaron Maule, Matthew Berriman, Timothy Day, Paula Ribeiro, Christoph G Grevelding
Schistosomes are blood-dwelling trematodes with global impact on human and animal health. Because medical treatment is currently based on a single drug, praziquantel, there is urgent need for the development of alternative control strategies. The Schistosoma mansoni genome project provides a platform to study and connect the genetic repertoire of schistosomes to specific biological functions essential for successful parasitism. G protein-coupled receptors (GPCRs) form the largest superfamily of transmembrane receptors throughout the Eumetazoan phyla, including platyhelminths...
January 2018: PLoS Pathogens
https://www.readbyqxmd.com/read/29345311/calcium-sensing-receptor-activates-the-nlrp3-inflammasome-in-ls14-preadipocytes-mediated-by-erk1-2-signaling
#2
Amanda D'Espessailles, Yuly A Mora, Cecilia Fuentes, Mariana Cifuentes
The study of the mechanisms that trigger inflammation in adipose tissue is key to understanding and preventing the cardiometabolic consequences of obesity. We have proposed a model where activation of the G protein-coupled calcium sensing receptor (CaSR) leads to inflammation and dysfunction in adipose cells. Upon activation, CaSR can mediate the expression and secretion of proinflammatory factors in human preadipocytes, adipocytes and adipose tissue explants. One possible pathway involved in CaSR-induced inflammation is the activation of the NLR family, pyrin domain-containing 3 (NLRP3) inflammasome, that promotes maturation and secretion of interleukin (IL)-1β...
January 18, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29343833/dopamine-d3-receptor-antagonist-reveals-a-cryptic-pocket-in-aminergic-gpcrs
#3
Noelia Ferruz, Stefan Doerr, Michelle A Vanase-Frawley, Yaozhong Zou, Xiaomin Chen, Eric S Marr, Robin T Nelson, Bethany L Kormos, Travis T Wager, Xinjun Hou, Anabella Villalobos, Simone Sciabola, Gianni De Fabritiis
The recent increase in the number of X-ray crystal structures of G-protein coupled receptors (GPCRs) has been enabling for structure-based drug design (SBDD) efforts. These structures have revealed that GPCRs are highly dynamic macromolecules whose function is dependent on their intrinsic flexibility. Unfortunately, the use of static structures to understand ligand binding can potentially be misleading, especially in systems with an inherently high degree of conformational flexibility. Here, we show that docking a set of dopamine D3 receptor compounds into the existing eticlopride-bound dopamine D3 receptor (D3R) X-ray crystal structure resulted in poses that were not consistent with results obtained from site-directed mutagenesis experiments...
January 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29343553/molecular-mechanisms-of-biased-and-probe-dependent-signaling-at-cxcr3-induced-by-negative-allosteric-modulators
#4
Regine Brox, Lampros Milanos, Noureldin Saleh, Paul Baumeister, Armin Buschauer, Dagmar Hofmann, Markus R Heinrich, Timothy Clark, Nuska Tschammer
Our recent explorations of allosteric modulators (AMs) with improved properties resulted in the identification of two biased negative AMs, N-1-{[3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimi-din2yl]ethyl}-4-(4-fluorobutoxy)-N-[(1-methylpiperidin-4-yl)me-thyl}]butanamide (BD103) and {5-[(N-{1-[3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl]ethyl-2-[4-fluoro-3-(trifluoromethyl)phenyl]acetamido)methyl]-2-fluorophenyl}boronic acid (BD064), that exhibited probe-dependent inhibition of the chemokine receptor CXCR3 signaling...
January 17, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29343498/the-gpr120-agonist-tug-891-promotes-metabolic-health-by-stimulating-mitochondrial-respiration-in-brown-fat
#5
Maaike Schilperoort, Andrea D van Dam, Geerte Hoeke, Irina G Shabalina, Anthony Okolo, Aylin C Hanyaloglu, Lea H Dib, Isabel M Mol, Natarin Caengprasath, Yi-Wah Chan, Sami Damak, Anne Reifel Miller, Tamer Coskun, Bharat Shimpukade, Trond Ulven, Sander Kooijman, Patrick Cn Rensen, Mark Christian
Brown adipose tissue (BAT) activation stimulates energy expenditure in human adults, which makes it an attractive target to combat obesity and related disorders. Recent studies demonstrated a role for G protein-coupled receptor 120 (GPR120) in BAT thermogenesis. Here, we investigated the therapeutic potential of GPR120 agonism and addressed GPR120-mediated signaling in BAT We found that activation of GPR120 by the selective agonist TUG-891 acutely increases fat oxidation and reduces body weight and fat mass in C57Bl/6J mice...
January 17, 2018: EMBO Molecular Medicine
https://www.readbyqxmd.com/read/29343433/oxysterol-sensing-through-the-receptor-gpr183-promotes-the-lymphoid-tissue-inducing-function-of-innate-lymphoid-cells-and-colonic-inflammation
#6
Johanna Emgård, Hana Kammoun, Bethania García-Cassani, Julie Chesné, Sara M Parigi, Jean-Marie Jacob, Hung-Wei Cheng, Elza Evren, Srustidhar Das, Paulo Czarnewski, Natalie Sleiers, Felipe Melo-Gonzalez, Egle Kvedaraite, Mattias Svensson, Elke Scandella, Matthew R Hepworth, Samuel Huber, Burkhard Ludewig, Lucie Peduto, Eduardo J Villablanca, Henrique Veiga-Fernandes, João P Pereira, Richard A Flavell, Tim Willinger
Group 3 innate lymphoid cells (ILC3s) sense environmental signals and are critical for tissue integrity in the intestine. Yet, which signals are sensed and what receptors control ILC3 function remain poorly understood. Here, we show that ILC3s with a lymphoid-tissue-inducer (LTi) phenotype expressed G-protein-coupled receptor 183 (GPR183) and migrated to its oxysterol ligand 7α,25-hydroxycholesterol (7α,25-OHC). In mice lacking Gpr183 or 7α,25-OHC, ILC3s failed to localize to cryptopatches (CPs) and isolated lymphoid follicles (ILFs)...
January 16, 2018: Immunity
https://www.readbyqxmd.com/read/29342984/amaranthus-caudatus-stimulates-insulin-secretion-in-goto-kakizaki-rats-a-model-of-diabetes-mellitus-type-2
#7
Silvia Zambrana, Lena C E Lundqvist, Virginia Veliz, Sergiu-Bogdan Catrina, Eduardo Gonzales, Claes-Göran Östenson
Diabetes Mellitus Type 2 prevalence is increasing worldwide; thus efforts to develop novel therapeutic strategies are required. Amaranthus caudatus (AC) is a pseudo-cereal with reported anti-diabetic effects that is usually consumed in food preparations in Bolivia. This study evaluated the anti-diabetic nutraceutical property of an AC hydroethanolic extract that contains mainly sugars and traces of polyphenols and amino acids (as shown by nalysis with liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR)), in type 2 diabetic Goto-Kakizaki (GK) rats and healthy Wistar (W) rats...
January 15, 2018: Nutrients
https://www.readbyqxmd.com/read/29342363/differential-effects-of-inhibitory-g-protein-isoforms-on-g-protein-gated-inwardly-rectifying-k-currents-in-adult-murine-atria
#8
Muriel Nobles, David Montaigne, Sonia Sebastian, Lutz Birnbaumer, Andrew Tinker
G-protein gated inwardly rectifying K+ (GIRK) channels are the major inwardly rectifying K+ currents in cardiac atrial myocytes and an important determinant of atrial electrophysiology. Inhibitory G-protein alpha subunits can both mediate activation via acetylcholine but can also supress basal currents in the absence of agonist. We studied this phenomenon using whole cell patch clamping in murine atria from mice with global genetic deletion of Gαi2, combined deletion of Gαi1/Gαi3 and littermate controls...
January 17, 2018: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29342245/structure-function-relationships-of-olfactory-and-taste-receptors
#9
Maik Behrens, Loïc Briand, Claire A de March, Hiroaki Matsunami, Atsuko Yamashita, Wolfgang Meyerhof, Simone Weyand
The field of chemical senses has made major progress in understanding the cellular mechanisms of olfaction and taste in the past two decades. However, the molecular understanding of odour and taste recognition is still lagging far behind and will require solving multiple structures of the relevant full-length receptors in complex with native ligands to achieve this goal. However, the development of multiple complimentary strategies for the structure determination of G protein-coupled receptors (GPCRs) makes this goal realistic...
January 12, 2018: Chemical Senses
https://www.readbyqxmd.com/read/29341826/mu-opioid-receptors-inhibit-the-exercise-pressor-reflex-by-closing-n-type-calcium-channels-but-not-by-opening-girk-channels-in-rats
#10
Juan A Estrada, Marc P Kaufman
Mu opioid G-protein coupled receptors (MOR) interact with ion channels to decrease neuronal excitability. In humans, intrathecal administration of the MOR agonist, fentanyl, inhibits the exercise pressor reflex, an effect that can be attributed to either the opening of inward rectifying potassium channels (GIRK) or the closing of N-type calcium channels. The purpose of this study was to determine if the highly selective MOR agonist DAMGO attenuates the exercise pressor reflex, and which of these two channels are responsible for this effect...
January 17, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/29341465/p2y12-deficiency-in-mouse-impairs-noradrenergic-system-in-brain-and-alters-anxiety-like-neurobehavior-and-memory
#11
Fang Zheng, Qiang Zhou, Yin Cao, Hailian Shi, Hui Wu, Beibei Zhang, Fei Huang, Xiaojun Wu
Purinergic receptor P2Y12 (P2Y12 ), a G protein-coupled (GPCR) purinergic receptor, is widely distributed in nervous system and involved in the progression of neurological diseases such as multiple sclerosis and neuropathic pain. The central noradrenergic system actively participates in a number of neurophysiological processes. Nevertheless, whether there is any direct relevance between P2Y12 and noradrenergic signal transduction remains unknown. In the present study, we tested the hypothesis that lack of P2Y12 impaired noradrenergic signal transduction in mouse brain...
January 17, 2018: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/29340786/in-silico-identification-and-experimental-validation-of-amino-acid-motifs-required-for-the-rho-of-plants-gtpase-mediated-activation-of-receptor-like-cytoplasmic-kinases
#12
Dézi Bianka Lajkó, Ildikó Valkai, Mónika Domoki, Dalma Ménesi, Györgyi Ferenc, Ferhan Ayaydin, Attila Fehér
Several amino acid motifs required for Rop-dependent activity were found to form a common surface on RLCKVI_A kinases. This indicates a unique mechanism for Rho-type GTPase-mediated kinase activation in plants. Rho-of-plants (Rop) G-proteins are implicated in the regulation of various cellular processes, including cell growth, cell polarity, hormonal and pathogen responses. Our knowledge about the signalling pathways downstream of Rops is continuously increasing. However, there are still substantial gaps in this knowledge...
January 16, 2018: Plant Cell Reports
https://www.readbyqxmd.com/read/29339457/curcumin-acts-as-a-positive-allosteric-modulator-of-%C3%AE-7-nicotinic-acetylcholine-receptors-and-reverses-nociception-in-mouse-models-of-inflammatory-pain
#13
Eslam Gaber El Nebrisi, Deniz Bagdas, Wisam Toma, Halima Al Samri, Anna Brodzik, Yasmin Alkhlaif, Keun-Hang Susan Yang, Frank C Howarth, Imad M Damaj, Murat Oz
Effects of curcumin, a major ingredient of turmeric, were tested on the function of α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes and on nociception in mouse models of tonic and visceral pain. Curcumin caused a significant potentiation of ACh (100 μM)-induced currents with an EC50 value of 0.2 µM. The effect of curcumin was not dependent on the activation of G-proteins and protein kinases and did not involve Ca2+-dependent Cl- channels expressed endogenously in oocytes...
January 16, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29339445/bile-acids-in-glucose-metabolism-in-health-and-disease
#14
REVIEW
Hagit Shapiro, Aleksandra A Kolodziejczyk, Daniel Halstuch, Eran Elinav
Bile acids (BAs) are cholesterol-derived metabolites that facilitate the intestinal absorption and transport of dietary lipids. Recently, BAs also emerged as pivotal signaling molecules controlling glucose, lipid, and energy metabolism by binding to the nuclear hormone farnesoid X receptor (FXR) and Takeda G protein receptor 5 (TGR5) in multiple organs, leading to regulation of intestinal incretin secretion, hepatic gluconeogenesis, glycogen synthesis, energy expenditure, inflammation, and gut microbiome configuration...
January 16, 2018: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/29338718/a-live-cell-assay-of-gpcr-coupling-allows-identification-of-optogenetic-tools-for-controlling-go-and-gi-signaling
#15
Edward R Ballister, Jessica Rodgers, Franck Martial, Robert J Lucas
BACKGROUND: Animal opsins are light-sensitive G-protein-coupled receptors (GPCRs) that enable optogenetic control over the major heterotrimeric G-protein signaling pathways in animal cells. As such, opsins have potential applications in both biomedical research and therapy. Selecting the opsin with the best balance of activity and selectivity for a given application requires knowing their ability to couple to a full range of relevant Gα subunits. We present the GsX assay, a set of tools based on chimeric Gs subunits that transduce coupling of opsins to diverse G proteins into increases in cAMP levels,  measured with a real-time reporter in living cells...
January 16, 2018: BMC Biology
https://www.readbyqxmd.com/read/29338045/protection-induced-by-virus-like-particle-vaccine-containing-tandem-repeat-gene-of-respiratory-syncytial-virus-g-protein
#16
Ah-Ra Kim, Dong-Hun Lee, Su-Hwa Lee, Ilaria Rubino, Hyo-Jick Choi, Fu-Shi Quan
Respiratory syncytial virus (RSV) is the leading cause of lower respiratory tract illness in infants, young children and the elderly. However, there is no licensed vaccine available against RSV infection. In this study, we generated virus-like particle (VLP) vaccine and investigated the vaccine efficacy in a mouse model. For VLP vaccines, tandem gene (1-780 bp) for V1 VLPs and tandem repeat gene (repeated 450-780 bp) for V5 VLPs were constructed in pFastBacTM vectors, respectively. Influenza matrix protein 1 (M1) was used as a core protein in the VLPs...
2018: PloS One
https://www.readbyqxmd.com/read/29337301/hepatic-gi-signaling-regulates-whole-body-glucose-homeostasis
#17
Mario Rossi, Lu Zhu, Sara M McMillin, Sai Prasad Pydi, Shanu Jain, Lei Wang, Yinghong Cui, Regina J Lee, Amanda H Cohen, Hideaki Kaneto, Morris J Birnbaum, Yanling Ma, Yaron Rotman, Jie Liu, Travis J Cyphert, Toren Finkel, Owen P McGuinness, Jürgen Wess
An increase in hepatic glucose production (HGP) is a key feature of type 2 diabetes. Excessive signaling through hepatic Gs-linked glucagon receptors critically contributes to pathologically elevated HGP. Here, we tested the hypothesis that this metabolic impairment can be counteracted by enhancing hepatic Gi signaling. Specifically, we used a chemogenetic approach to selectively activate Gi-type G proteins in mouse hepatocytes in vivo. Unexpectedly, activation of hepatic Gi signaling triggered a pronounced increase in HGP and severely impaired glucose homeostasis...
January 16, 2018: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/29337260/modelling-and-simulation-of-biased-agonism-dynamics-at-a-g%C3%A2-protein-coupled-receptor
#18
L J Bridge, J Mead, E Frattini, I Winfield, G Ladds
Theoretical models of G protein-coupled receptor (GPCR) concentration-response relationships often assume an agonist producing a single functional response via a single active state of the receptor. These models have largely been analysed assuming steady-state conditions. There is now much experimental evidence to suggest that many GPCRs can exist in multiple receptor conformations and elicit numerous functional responses, with ligands having the potential to activate different signalling pathways to varying extents - a concept referred to as biased agonism, functional selectivity or pluri-dimensional efficacy...
January 11, 2018: Journal of Theoretical Biology
https://www.readbyqxmd.com/read/29336473/usefulness-of-identifying-g-protein-coupled-receptor-dimers-for-diagnosis-and-therapy-of-neurodegenerative-diseases-and-of-gliomas
#19
REVIEW
Irene Reyes-Resina, David Aguinaga, José Luis Labandeira-García, José Luis Lanciego, Gemma Navarro, Rafael Franco
Immunochemical detection of G-protein-coupled receptors (GPCRs) in cells and tissues was a technical challenge for years. After the discovery of formation of GPCR dimers/trimers/tetramers in transfected cells, a most recent challenge has been to confirm receptor-receptor interactions in natural sources. The occurrence of dimers or higher order oligomers is important from a therapeutic point of view, mainly because their physiology/pharmacology is different from those of individual receptors. On the one hand, pathophysiological factors need to count more on GPCR dimers than on individual receptors...
January 16, 2018: Histology and Histopathology
https://www.readbyqxmd.com/read/29336307/activation-of-g-protein-coupled-estrogen-receptor-signaling-inhibits-melanoma-and-improves-response-to-immune-checkpoint-blockade
#20
Christopher A Natale, Jinyang Li, Junqian Zhang, Ankit Dahal, Tzvete Dentchev, Ben Z Stanger, Todd W Ridky
Female sex and history of prior pregnancies are associated with favorable melanoma outcomes. Here, we show that much of the melanoma protective effect likely results from estrogen signaling through the G protein-coupled estrogen receptor (GPER) on melanocytes. Selective GPER activation in primary melanocytes and melanoma cells induced long-term changes that maintained a more differentiated cell state as defined by increased expression of well-established melanocyte differentiation antigens, increased pigment production, decreased proliferative capacity, and decreased expression of the oncodriver and stem cell marker c-Myc...
January 16, 2018: ELife
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