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G protein coupled receptor

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https://www.readbyqxmd.com/read/29355732/the-quest-for-endothelial-atypical-cannabinoid-receptor-bkca-channels-act-as-cellular-sensors-for-cannabinoids-in-in-vitro-and-in-situ-endothelial-cells
#1
Alexander I Bondarenko, Olga Panasiuk, Konstantin Drachuk, Fabrizio Montecucco, Karim J Brandt, François Mach
Endothelium-dependent component of cannabinoid-induced vasodilation has been postulated to require G-protein-coupled non-CB1/CB2 endothelial cannabinoid (eCB) receptor. GPR18 was proposed as a candidate for eCBR. To address the hypothesis that the effects attributed to eCBR are mediated by G-protein-coupled receptor (GPCR)-independent targets, we studied the electrical responses in endothelial cells, focusing on BKCa channels. In patches excised from endothelial-derived EA.hy926 cells, N-arachydonoyl glycine (NAGly) and abnormal cannabidiol (abn-cbd), prototypical agonists for eCB receptor, stimulate single BKCa activity in a concentration- and Ca2+-dependent manner...
January 17, 2018: Vascular Pharmacology
https://www.readbyqxmd.com/read/29355558/-epicatechin-stimulates-mitochondrial-biogenesis-and-cell-growth-in-c2c12-myotubes-via-the-g-protein-coupled-estrogen-receptor
#2
Aldo Moreno-Ulloa, Adriana Miranda-Cervantes, Alexei Licea-Navarro, Christina Mansour, Ernesto Beltrán-Partida, Luis Donis-Maturano, Hilda Carolina Delgado De la Herrán, Francisco Villarreal, Carolina Álvarez-Delgado
We have reported on the capacity of (-)-epicatechin ((-)-EPI) to stimulate mitochondrial biogenesis (MiB) in mouse skeletal muscle (SkM). However, the mechanisms mediating the effects of (-)-EPI are not fully understood. We previously identified a role of the G-protein coupled estrogen receptor (GPER) in modulating the vascular effects of (-)-EPI. We therefore tested the hypothesis that GPER mediates (at least in part) the stimulatory effects of (-)-EPI on MiB in SkM cells. As an in vitro model, we employed mouse SkM-derived C2C12 myoblasts differentiated into myotubes...
January 16, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29355483/plasticity-of-the-ligand-binding-pocket-in-the-bitter-taste-receptor-t2r7
#3
Kun Liu, Appalaraju Jaggupilli, Dhanaraj Premnath, Prashen Chelikani
Bitter taste receptors (T2Rs) are a group of 25 G protein-coupled receptors (GPCRs) in humans. The cognate agonists and the mechanism of ligand binding to the majority of the T2Rs remain unknown. Here we report the first structure-function analysis of T2R7 and study the ability of this receptor to bind to different agonists by site-directed mutagenesis. Screening of ligands for T2R7 in calcium based assays lead to the identification of novel compounds that activate this receptor. Quinine, diphenidol, dextromethorphan and diphenhydramine showed substantial activation of T2R7...
January 18, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29355372/m-4-muscarinic-receptors-and-locomotor-activity-regulation
#4
J Myslivecek, V Farar, P Valuskova
M(4) muscarinic receptors (M(4) MR) represent a subfamily of G-protein coupled receptors serving a substantial role in spontaneous locomotor activity regulation, cognition and modulation of cholinergic system. With increasing body of literature discussing the role of M(4) MR some controversies arose. Thus, we try here to summarize the current evidence regarding the M(4) MR, with the special focus on their role in Locomotor activity control. We review the molecular function of M(4) MR in specific brain areas implicated in locomotor regulation, and shortly in other CNS processes that could be connected to locomotor activity...
December 30, 2017: Physiological Research
https://www.readbyqxmd.com/read/29355030/allosteric-modulators-of-cannabinoid-receptor-1-developing-compounds-for-improved-specificity
#5
Rachel Dopart, Dai Lu, Aron H Lichtman, Debra A Kendall
The cannabinoid receptor 1 (CB1) is a G protein-coupled receptor (GPCR) that is located primarily in the central nervous system. CB1 is a therapeutic target which may impact pathways to mediate pain, neurodegenerative disorders, hunger, and drug-seeking behavior. Despite these benefits, development of orthosteric therapeutic compounds, which target the endogenous ligand-binding site of CB1, has been challenging due to detrimental side effects including psychoactivity, depression, and suicidal thoughts. However, CB1 also has an allosteric binding site(s), which is topographically distinct from the orthosteric site...
January 21, 2018: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/29354237/novel-genetic-variants-associated-with-lumbar-spondylosis-in-koreans-a-genome-wide-association-study
#6
Hyun Ah Kim, Seong Gu Heo, Ji Wan Park, Young Ok Jung
Objective: The aim of this study was to identify the susceptibility genes responsible for lumbar spondylosis (LS) in Korean patients. Methods: Data from 1427 subjects were made available for radiographic grading and genome wide association studies (GWAS) analysis. Lateral lumbar spine radiographs were obtained and the various degrees of degenerative change were semi-quantitatively scored. A pilot GWAS was performed using the AffymetrixGenome-Wide Human single-nucleotide polymorphisms (SNPs), 500K array...
January 2018: Journal of Korean Neurosurgical Society
https://www.readbyqxmd.com/read/29353414/oral-administration-of-compound-probiotics-ameliorates-hfd-induced-gut-microbe-dysbiosis-and-chronic-metabolic-inflammation-via-the-g-protein-coupled-receptor-43-in-non-alcoholic-fatty-liver-disease-rats
#7
Yinji Liang, Shu Liang, Yupei Zhang, Yuanjun Deng, Yifang He, Yanning Chen, Chan Liu, Chenli Lin, Qinhe Yang
The aim of this study was to investigate how the effects of compound probiotics modulate the gut microbiota, short-chain fatty acid (SCFA), body composition, serum and liver lipids, and inflammatory markers in non-alcoholic fatty liver disease (NAFLD) rats. Twenty-four male SD rats were randomly divided into 3 groups: normal control group (standard feed), high-fat diet (HFD) feeding group (83% standard feed + 10% lard oil + 1.5% cholesterol + 0.5% cholate + 5% sucrose), and compound probiotics intervention group (HFD + 0...
January 20, 2018: Probiotics and Antimicrobial Proteins
https://www.readbyqxmd.com/read/29352161/the-action-of-a-negative-allosteric-modulator-at-the-dopamine-d2-receptor-is-dependent-upon-sodium-ions
#8
Christopher J Draper-Joyce, Ravi Kumar Verma, Mayako Michino, Jeremy Shonberg, Anitha Kopinathan, Carmen Klein Herenbrink, Peter J Scammells, Ben Capuano, Ara M Abramyan, David M Thal, Jonathan A Javitch, Arthur Christopoulos, Lei Shi, J Robert Lane
Sodium ions (Na+) allosterically modulate the binding of orthosteric agonists and antagonists to many class A G protein-coupled receptors, including the dopamine D2 receptor (D2R). Experimental and computational evidences have revealed that this effect is mediated by the binding of Na+ to a conserved site located beneath the orthosteric binding site (OBS). SB269652 acts as a negative allosteric modulator (NAM) of the D2R that adopts an extended bitopic pose, in which the tetrahydroisoquinoline moiety interacts with the OBS and the indole-2-carboxamide moiety occupies a secondary binding pocket (SBP)...
January 19, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29351614/a-membrane-g-protein-coupled-estrogen-receptor-is-necessary-but-not-sufficient-for-sex-differences-in-zebra-finch-auditory-coding
#9
Amanda A Krentzel, Matheus Macedo-Lima, Maaya Z Ikeda, Luke Remage-Healey
Estradiol acts as a neuromodulator in brain regions important for cognition and sensory processing. Estradiol also shapes brain sex differences, but rarely have these concepts been considered simultaneously. In male and female songbirds, estradiol rapidly increases within the auditory forebrain during song exposure and enhances local auditory processing. We tested whether GPER1, a membrane bound estrogen receptor, is necessary and sufficient for neuroestrogen regulation of forebrain auditory processing in male and female zebra finches (Taeniopygia guttata)...
January 17, 2018: Endocrinology
https://www.readbyqxmd.com/read/29351511/chemogenetic-tools-for-causal-cellular-and-neuronal-biology
#10
Deniz Atasoy, Scott M Sternson
Chemogenetic technologies enable selective pharmacological control of specific cell populations. An increasing number of approaches have been developed that modulate different signaling pathways. Selective pharmacological control over G protein-coupled receptor signaling, ion channel conductances, protein association, protein stability, and small molecule targeting allows modulation of cellular processes in distinct cell types. Here, we review these chemogenetic technologies and instances of their applications in complex tissues in vivo and ex vivo...
January 1, 2018: Physiological Reviews
https://www.readbyqxmd.com/read/29351497/screen-targeting-lung-and-prostate-cancer-oncogene-identifies-novel-inhibitors-of-rgs17-and-problematic-chemical-substructures
#11
Christopher R Bodle, Josephine H Schamp, Joseph B O'Brien, Michael P Hayes, Meng Wu, Jonathan A Doorn, David L Roman
Regulator of G protein signaling (RGS) proteins temporally regulate heterotrimeric G protein signaling cascades elicited by G protein-coupled receptor activation and thus are essential for cell homeostasis. The dysregulation of RGS protein expression has been linked to several pathologies, spurring discovery efforts to identify small-molecule inhibitors of these proteins. Presented here are the results of a high-throughput screening (HTS) campaign targeting RGS17, an RGS protein reported to be inappropriately upregulated in several cancers...
January 1, 2018: SLAS Discovery
https://www.readbyqxmd.com/read/29350995/a-review-of-analytical-methods-for-the-determination-of-clopidogrel-in-pharmaceuticals-and-biological-matrices
#12
Kavitha J, K S Kokilambigai, R Seetharaman, Harini R R, A A Kaaviya, Sowndaravel P, Lakshmi K S
P2Y12 belongs to a group of G protein - coupled (GPCR) purinergic receptors and is a receptor for adenosine diphosphate (ADP). The P2Y12 receptor is involved in platelet aggregation and acts as a biological target for treating thromboembolisms and other clotting disorders. The use of Clopidogrel (CLO) has improved the morbidity and mortality endpoints including cardiovascular death, recurrent myocardial infarction (MI) and stroke at 30 days after percutaneous coronary intervention (PCI). CLO is one such drug that specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor...
January 19, 2018: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/29350399/biological-functions-of-elabela-a-novel-endogenous-ligand-of-apj-receptor
#13
REVIEW
Jin Xu, Linxi Chen, Zhisheng Jiang, Lanfang Li
The G protein-coupled receptor APJ and its cognate ligand, apelin, are widely expressed throughout human body. They are implicated in different key physiological processes such as angiogenesis, cardiovascular functions, fluid homeostasis and energy metabolism regulation. Recently, a new endogenous peptidic ligand of APJ, named Elabela, has been identified and shown to play a crucial role in embryonic development. In addition, increasing evidences show that Elabela is also intimate associated with a large number of physiological processes in adulthood...
January 19, 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29350282/neutrophil-chemotaxis
#14
REVIEW
Björn Petri, Maria-Jesús Sanz
Neutrophils are the primary cells recruited to inflamed sites during an innate immune response to tissue damage and/or infection. They are finely sensitive to inciting stimuli to reach in great numbers and within minutes areas of inflammation and tissue insult. For this effective response, they can detect extracellular chemical gradients and move towards higher concentrations, the so-called chemotaxis process or guided cell migration. This directed neutrophil recruitment is orchestrated by chemoattractants, a chemically diverse group of molecular guidance cues (e...
January 19, 2018: Cell and Tissue Research
https://www.readbyqxmd.com/read/29349610/ligand-binding-dynamics-for-pre-dimerised-g-protein-coupled-receptor-homodimers-linear-models-and-analytical-solutions
#15
Carla White, Lloyd J Bridge
Evidence suggests that many G protein-coupled receptors (GPCRs) are bound together forming dimers. The implications of dimerisation for cellular signalling outcomes, and ultimately drug discovery and therapeutics, remain unclear. Consideration of ligand binding and signalling via receptor dimers is therefore required as an addition to classical receptor theory, which is largely built on assumptions of monomeric receptors. A key factor in developing theoretical models of dimer signalling is cooperativity across the dimer, whereby binding of a ligand to one protomer affects the binding of a ligand to the other protomer...
January 18, 2018: Bulletin of Mathematical Biology
https://www.readbyqxmd.com/read/29348172/-the-a-arrestin-arrdc3-suppresses-breast-carcinoma-invasion-by-regulating-g-protein-coupled-receptor-lysosomal-sorting-and-signaling
#16
Aleena K S Arakaki, Wen-An Pan, Huilan Lin, JoAnn Trejo
Aberrant G protein-coupled receptor (GPCR) expression and activation has been linked to tumor initiation, progression, invasion and metastasis. However, compared with other cancer drivers, the exploitation of GPCRs as potential therapeutic targets has been largely ignored, despite the fact that GPCRs are highly druggable. Therefore, to advance the potential status of GPCRs as therapeutic targets, it is important to understand how GPCRs function together with other cancer drivers during tumor progression. We now report that the alpha-arrestin domain-containing protein-3 (ARRDC3) acts as a tumor suppressor in part by controlling signaling and trafficking of the GPCR, protease-activated receptor-1 (PAR1)...
January 18, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29347925/alarm-pheromone-and-kairomone-detection-via-bitter-taste-receptors-in-the-mouse-grueneberg-ganglion
#17
Fabian Moine, Julien Brechbühl, Monique Nenniger Tosato, Manon Beaumann, Marie-Christine Broillet
BACKGROUND: The mouse Grueneberg ganglion (GG) is an olfactory subsystem specialized in the detection of volatile heterocyclic compounds signalling danger. The signalling pathways transducing the danger signals are only beginning to be characterized. RESULTS: Screening chemical libraries for compounds structurally resembling the already-identified GG ligands, we found a new category of chemicals previously identified as bitter tastants that initiated fear-related behaviours in mice depending on their volatility and evoked neuronal responses in mouse GG neurons...
January 18, 2018: BMC Biology
https://www.readbyqxmd.com/read/29346437/tissue-specific-transcriptome-analyses-provide-new-insights-into-gpcr-signalling-in-adult-schistosoma-mansoni
#18
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
#19
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
#20
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
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