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https://www.readbyqxmd.com/read/28698140/n-arachidonoyl-glycine-another-endogenous-agonist-of-gpr55
#1
Linda Console-Bram, Sandra M Ciuciu, Pingwei Zhao, Robert E Zipkin, Eugen Brailoiu, Mary E Abood
Interest in lipoamino acids as endogenous modulators of G-protein coupled receptors has escalated due to their involvement in a variety of physiologic processes. In particular, a role for these amino acid conjugates has emerged in the endocannabinoid system. The study presented herein investigated the effects of N-arachidonoyl glycine (NAGly) on a candidate endocannabinoid receptor, GPR55. Our novel findings reveal that NAGly induces concentration dependent increases in calcium mobilization and mitogen-activated protein kinase activities in HAGPR55/CHO cells...
July 8, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28673732/design-synthesis-and-biological-evaluation-of-gpr55-agonists
#2
Lara Fakhouri, Christopher D Cook, Mohammed H Al-Huniti, Linda M Console-Bram, Dow P Hurst, Michael B S Spano, Daniel J Nasrallah, Marc G Caron, Larry S Barak, Patricia H Reggio, Mary E Abood, Mitchell P Croatt
GPR55, a G protein-coupled receptor, is an attractive target to alleviate inflammatory and neuropathic pain and treat osteoporosis and cancer. Identifying a potent and selective ligand will aid to further establish the specific physiological roles and pharmacology of the receptor. Towards this goal, a targeted library of 22 compounds was synthesized in a modular fashion to obtain structure-activity relationship information. The general route consisted of coupling a variety of p-aminophenyl sulfonamides to isothiocyanates to form acylthioureas...
June 13, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28653801/a-putative-lysophosphatidylinositol-receptor-gpr55-modulates-hippocampal-synaptic-plasticity
#3
Katrina Hurst, Corinne Badgley, Tanner Ellsworth, Spencer Bell, Lindsey Friend, Brad Prince, Jacob Welch, Zack Cowan, Ryan Williamson, Chris Lyon, Brandon Anderson, Brian Poole, Michael Christensen, Michael McNeil, Jarrod Call, Jeffrey G Edwards
GPR55, an orphan G-protein coupled receptor, is activated by lysophosphatidylinositol (LPI) and the endocannabinoid anandamide, as well as by other compounds including THC. LPI is a potent endogenous ligand of GPR55 and neither GPR55 nor LPIs' functions in the brain are well understood. While endocannabinoids are well known to modulate brain synaptic plasticity, the potential role LPI could have on brain plasticity has never been demonstrated. Therefore, we examined not only GPR55 expression, but also the role its endogenous ligand could play in long-term potentiation, a common form of synaptic plasticity...
June 8, 2017: Hippocampus
https://www.readbyqxmd.com/read/28638091/the-cannabinoid-ligand-lh-21-reduces-anxiety-and-improves-glucose-handling-in-diet-induced-obese-pre-diabetic-mice
#4
Silvana Y Romero-Zerbo, Inmaculada Ruz-Maldonado, Vanesa Espinosa-Jiménez, Alex Rafacho, Ana I Gómez-Conde, Lourdes Sánchez-Salido, Nadia Cobo-Vuilleumier, Benoit R Gauthier, Francisco J Tinahones, Shanta J Persaud, Francisco J Bermúdez-Silva
LH-21 is a triazol derivative that has been described as a low-permeant neutral CB1 antagonist, though its pharmacology is still unclear. It has been associated with anti-obesity actions in obese rats. However, its role in preventing type 2 diabetes (T2D) onset have not been studied yet. Given CB1 receptors remain as potential pharmacological targets to fight against obesity and T2D, we wanted to explore the metabolic impact of this compound in an animal model of obesity and pre-diabetes as well as the lack of relevant actions in related central processes such as anxiety...
June 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28552522/lysophosphatidylcholine-elicits-intracellular-calcium-signaling-in-a-gpr55-dependent-manner
#5
Anna Drzazga, Agata Sowinska, Agnieszka Krzeminska, Przemysław Rytczak, Maria Koziolkiewicz, Edyta Gendaszewska-Darmach
The GPR55 signaling is fertile ground for drug discovery, however despite considerable research progress during the past 10 years, many open questions remain. The GPR55 pharmacology remains controversial, as many ligands have been reported with inconsistent results. Here, we show that various molecular species of lysophosphatidylcholine (LPC) elicit intracellular Ca(2+) mobilization in GPR55-expressing PC-3 human prostate carcinoma cells. The response was even stronger than [Ca(2+)]i flux evoked by endogenous (OEA) and synthetic (Abn-CBD) agonists...
July 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28534260/pharmacogenetics-of-cannabinoids
#6
Szymon Hryhorowicz, Michal Walczak, Oliwia Zakerska-Banaszak, Ryszard Słomski, Marzena Skrzypczak-Zielińska
Although the application of medical marijuana and cannabinoid drugs is controversial, it is a part of modern-day medicine. The list of diseases in which cannabinoids are promoted as a treatment is constantly expanding. Cases of significant improvement in patients with a very poor prognosis of glioma or epilepsy have already been described. However, the occurrence of side effects is still difficult to estimate, and the current knowledge of the therapeutic effects of cannabinoids is still insufficient. In our opinion, the answers to many questions and concerns regarding the medical use of cannabis can be provided by pharmacogenetics...
May 22, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28533434/lysophosphatidylinositol-induced-activation-of-the-cation-channel-trpv2-triggers-glucagon-like-peptide-1-secretion-in-enteroendocrine-l-cells
#7
Kazuki Harada, Tetsuya Kitaguchi, Taichi Kamiya, Kyaw Htet Aung, Kazuaki Nakamura, Kunihiro Ohta, Takashi Tsuboi
The lysophosphatidylinositol (LPI) has crucial roles in multiple physiological processes, including insulin exocytosis from pancreatic islets. However, the role of LPI in secretion of glucagon-like peptide-1 (GLP-1), a hormone that enhances glucose-induced insulin secretion, is unclear. Here, we used the murine enteroendocrine L cell line GLUTag and primary murine small intestinal cells to elucidate the mechanism of LPI-induced GLP-1 secretion. Exogenous LPI addition increased intracellular Ca(2+) concentrations ([Ca(2+)] i ) in GLUTag cells and induced GLP-1 secretion from both GLUTag and acutely prepared primary intestinal cells...
June 30, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28495590/concurrent-activation-of-%C3%AE-2-adrenergic-receptor-and-blockage-of-gpr55-disrupts-pro-oncogenic-signaling-in-glioma-cells
#8
Artur Wnorowski, Justyna Such, Rajib K Paul, Robert P Wersto, Fred E Indig, Krzysztof Jozwiak, Michel Bernier, Irving W Wainer
Activation of β2-adrenergic receptor (β2AR) and deorphanized GPR55 has been shown to modulate cancer growth in diverse tumor types in vitro and in xenograft models in vivo. (R,R')-4'-methoxy-1-naphthylfenoterol [(R,R')-MNF] is a bivalent compound that agonizes β2AR but inhibits GPR55-mediated pro-oncogenic responses. Here, we investigated the molecular mechanisms underlying the anti-tumorigenic effects of concurrent β2AR activation and GPR55 blockade in C6 glioma cells using (R,R')-MNF as a marker ligand...
August 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28457969/gpr55-and-the-regulation-of-glucose-homeostasis
#9
Eva Tudurí, Miguel López, Carlos Diéguez, Angel Nadal, Ruben Nogueiras
Pathophysiological conditions such as obesity and type 2 diabetes (T2D) are reportedly associated to over-activation of the endocannabinoid system (ECS). Therefore, modulation of the ECS offers potential therapeutic benefits on those diseases. GPR55, the receptor for L-α-lysophosphatidylinositol (LPI) that has also affinity for various cannabinoid ligands, is distributed at the central and peripheral level and it is involved in several physiological processes. This review summarizes the localization and role of GPR55 in tissues that are crucial for the regulation of glucose metabolism, and provides an update on its contribution in obesity and insulin resistance...
July 2017: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/28428628/inflammatory-and-neuropathic-nociception-is-preserved-in-gpr55-knockout-mice
#10
Lawrence M Carey, Tannia Gutierrez, Liting Deng, Wan-Hung Lee, Ken Mackie, Andrea G Hohmann
The G-protein coupled receptor GPR55 has been postulated to serve as a novel cannabinoid receptor. A previous report indicated that GPR55 knockout mice fail to develop mechanical hyperalgesia, suggesting a pro-nociceptive role for GPR55 in the control of nociceptive responding. However, GPR55 knockout mice remain incompletely characterized in models of pathological pain. Here we provide a comprehensive assessment of responses of GPR55 knockout and wild-type mice to mechanical and thermal (heat, cold) stimulation in multiple, mechanistically distinct models of inflammatory and neuropathic pain...
April 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28373843/antihyperalgesic-activities-of-endocannabinoids-in-a-mouse-model-of-antiretroviral-induced-neuropathic-pain
#11
Neha Munawar, Mabayoje A Oriowo, Willias Masocha
Background: Nucleoside reverse transcriptase inhibitors (NRTIs) are the cornerstone of the antiretroviral therapy for human immunodeficiency virus/acquired immune deficiency syndrome (HIV/AIDS). However, their use is sometimes limited by the development of a painful sensory neuropathy, which does not respond well to drugs. Smoked cannabis has been reported in clinical trials to have efficacy in relieving painful HIV-associated sensory neuropathy. Objectives: The aim of this study was to evaluate whether the expression of endocannabinoid system molecules is altered during NRTI-induced painful neuropathy, and also whether endocannabinoids can attenuate NRTI-induced painful neuropathy...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28289782/neuro-psychopharmacological-perspective-of-orphan-receptors-of-rhodopsin-class-a-family-of-g-protein-coupled-receptors
#12
REVIEW
Muhammad Zahid Khan, Ling He
BACKGROUND: In the central nervous system (CNS), G protein-coupled receptors (GPCRs) are the most fruitful targets for neuropsychopharmacological drug development. Rhodopsin (class A) is the most studied class of GPCR and includes orphan receptors for which the endogenous ligand is not known or is unclear. Characterization of orphan GPCRs has proven to be challenging, and the production pace of GPCR-based drugs has been incredibly slow. OBJECTIVE: Determination of the functions of these receptors may provide unexpected insight into physiological and neuropathological processes...
April 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28272905/g-protein-coupled-receptor-55-gpr55-expresses-differently-in-patients-with-crohn-s-disease-and-ulcerative-colitis
#13
Marcin Włodarczyk, Aleksandra Sobolewska-Włodarczyk, Adam I Cygankiewicz, Damian Jacenik, Wanda M Krajewska, Krystyna Stec-Michalska, Aleksandra Piechota-Polańczyk, Maria Wiśniewska-Jarosińska, Jakub Fichna
AIM: To investigate the levels of G protein-coupled receptor 55 (GPR55) expression in colonic tissue of inflammatory bowel disease (IBD) patients and healthy controls, and its potential implication in IBD treatment. METHODS: Fifty patients were enrolled in our prospective study: n = 21 with Crohn's disease (CD) and n = 16 with ulcerative colitis (UC); 19 women and 18 men. Control consisted of 13 non-IBD patients. In each subject, two biopsies were taken from different colonic locations...
June 2017: Scandinavian Journal of Gastroenterology
https://www.readbyqxmd.com/read/28237711/pharmacological-inhibition-of-faah-modulates-tlr-induced-neuroinflammation-but-not-sickness-behaviour-an-effect-partially-mediated-by-central-trpv1
#14
Rebecca J Henry, Daniel M Kerr, Lisa E Flannery, Marykate Killilea, Edel M Hughes, Louise Corcoran, David P Finn, Michelle Roche
Aberrant activation of toll-like receptors (TLRs), key components of the innate immune system, has been proposed to underlie and exacerbate a range of central nervous system disorders. Increasing evidence supports a role for the endocannabinoid system in modulating inflammatory responses including those mediated by TLRs, and thus this system may provide an important treatment target for neuroinflammatory disorders. However, the effect of modulating endocannabinoid tone on TLR-induced neuroinflammation in vivo and associated behavioural changes is largely unknown...
February 22, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28196832/gpr55-a-new-promising-target-for-metabolism
#15
REVIEW
Eva Tudurí, Monica Imbernon, Rene Javier Hernández-Bautista, Marta Tojo, Johan Fernø, Carlos Diéguez, Rubén Nogueiras
GPR55 is a G-protein-coupled receptor (GPCR) that has been identified as a new cannabinoid receptor. Given the wide localization of GPR55 in brain and peripheral tissues, this receptor has emerged as a regulator of multiple biological actions. Lysophosphatidylinositol (LPI) is generally accepted as the endogenous ligand of GPR55. In this review, we will focus on the role of GPR55 in energy balance and glucose metabolism. We will summarize its actions on feeding, nutrient partitioning, gastrointestinal motility and insulin secretion in preclinical models and the scarce data available in humans...
April 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28194850/cannabidiol-reduces-ethanol-consumption-motivation-and-relapse-in-mice
#16
Adrián Viudez-Martínez, María S García-Gutiérrez, Carmen María Navarrón, María Isabel Morales-Calero, Francisco Navarrete, Ana Isabel Torres-Suárez, Jorge Manzanares
This study evaluated the effects of cannabidiol (CBD) on ethanol reinforcement, motivation and relapse in C57BL/6 J mice. The effects of CBD (60 mg/kg, i.p.) on blood ethanol concentration, hypothermia and handling-induced convulsions associated to acute ethanol administration were evaluated. The two-bottle choice paradigm was performed to assess the effects of CBD (30, 60 and 120 mg/kg/day, i.p.) on ethanol intake and preference. In addition, an oral ethanol self-administration experiment was carried out to evaluate the effects of CBD [a single s...
February 13, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28168010/rutin-as-a-mediator-of-lipid-metabolism-and-cellular-signaling-pathways-interactions-in-fibroblasts-altered-by-uva-and-uvb-radiation
#17
Agnieszka Gęgotek, Paula Rybałtowska-Kawałko, Elżbieta Skrzydlewska
Background. Rutin is a natural nutraceutical that is a promising compound for the prevention of UV-induced metabolic changes in skin cells. The aim of this study was to examine the effects of rutin on redox and endocannabinoid systems, as well as proinflammatory and proapoptotic processes, in UV-irradiated fibroblasts. Methods. Fibroblasts exposed to UVA and UVB radiation were treated with rutin. The activities and levels of oxidants/antioxidants and endocannabinoid system components, as well as lipid, DNA, and protein oxidation products, and the proinflammatory and pro/antiapoptotic proteins expression were measured...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28087250/pharmacology-of-cannabinoids-in-the-treatment-of-epilepsy
#18
REVIEW
Tyler E Gaston, Daniel Friedman
The use of cannabis products in the treatment of epilepsy has long been of interest to researchers and clinicians alike; however, until recently very little published data were available to support its use. This article summarizes the available scientific data of pharmacology from human and animal studies on the major cannabinoids which have been of interest in the treatment of epilepsy, including ∆9-tetrahydrocannabinol (∆9-THC), cannabidiol (CBD), ∆9-tetrahydrocannabivarin (∆9-THCV), cannabidivarin (CBDV), and ∆9-tetrahydrocannabinolic acid (Δ9-THCA)...
May 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28064014/gpr55-agonist-lysophosphatidylinositol-and-lysophosphatidylcholine-inhibit-endothelial-cell-hyperpolarization-via-gpr-independent-suppression-of-na-ca-2-exchanger-and-endoplasmic-reticulum-ca-2-refilling
#19
Alexander I Bondarenko, Fabrizio Montecucco, Olga Panasiuk, Vadim Sagach, Nataliya Sidoryak, Karim J Brandt, François Mach
Lysophosphatidylinositol (LPI) and lysophosphatidylcholine (LPC) are lipid signaling molecules that induce endothelium-dependent vasodilation. In addition, LPC suppresses acetylcholine (Ach)-induced responses. We aimed to determine the influence of LPC and LPI on hyperpolarizing responses in vitro and in situ endothelial cells (EC) and identify the underlying mechanisms. Using patch-clamp method, we show that LPI and LPC inhibit EC hyperpolarization to histamine and suppress Na(+)/Ca(2+) exchanged (NCX) currents in a concentration-dependent manner...
January 5, 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28029647/peptide-guided-targeting-of-gpr55-for-anti-cancer-therapy
#20
Maria Mangini, Enrico Iaccino, Maria Giovanna Mosca, Selena Mimmi, Rosa D'Angelo, Ileana Quinto, Giuseppe Scala, Stefania Mariggiò
Expression of the lysophosphatidylinositol receptor GPR55 correlates with invasive potential of metastatic cells and bone metastasis formation of different types of tumors. These findings suggest a role for GPR55 signaling in cancer progression, including in lymphoproliferative diseases. Here, we screened a M13-phage-displayed random library using the bait of HEK293 cells that heterologously expressed full-length HA-GPR55. We selected a set of phagotopes that carried 7-mer insert peptides flanked by a pair of cysteine residues, which resulted in cyclized peptides...
January 17, 2017: Oncotarget
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