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https://www.readbyqxmd.com/read/28875496/g-protein-coupled-receptor-gpr55-promotes-colorectal-cancer-and-has-opposing-effects-to-cannabinoid-receptor-1
#1
Carina Hasenoehrl, David Feuersinger, Eva M Sturm, Thomas Bärnthaler, Ellen Heitzer, Ricarda Graf, Magdalena Grill, Martin Pichler, Stephan Beck, Lee Butcher, Dominique Thomas, Nerea Ferreirós, Rufina Schuligoi, Caroline Schweiger, Johannes Haybaeck, Rudolf Schicho
The putative cannabinoid receptor GPR55 has been shown to play a tumor-promoting role in various cancers, and is involved in many physiological and pathological processes of the gastrointestinal (GI) tract. While the cannabinoid receptor 1 (CB1 ) has been reported to suppress intestinal tumor growth, the role of GPR55 in the development of GI cancers is unclear. We, therefore, aimed at elucidating the role of GPR55 in colorectal cancer (CRC), the third most common cancer worldwide. Using azoxymethane (AOM)- and dextran sulfate sodium (DSS)-driven CRC mouse models, we found that GPR55 plays a tumor-promoting role that involves alterations of leukocyte populations, i...
September 5, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28867485/mechanisms-of-action-of-cannabidiol-in-adoptively-transferred-experimental-autoimmune-encephalomyelitis
#2
Coral González-García, Irene Moreno Torres, Ruth García-Hernández, Lucía Campos-Ruíz, Luis Rodríguez Esparragoza, María José Coronado, Aranzazu García Grande, Antonio García-Merino, Antonio J Sánchez López
Cannabidiol (CBD) is one of the most important compounds in Cannabis sativa, lacks psychotropic effects, and possesses a high number of therapeutic properties including the amelioration of experimental autoimmune encephalomyelitis (EAE). The aim of this study was to analyse the relative efficacy of CBD in adoptively transferred EAE (at-EAE), a model that allows better delineation of the effector phase of EAE. Splenocytes and lymph nodes from mice with actively induced EAE were cultured in the presence of MOG35-55 and IL-12 and inoculated intraperitoneally in recipient female C57BL/6J mice...
September 1, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28861501/palmitoylethanolamide-modulates-gpr55-receptor-signaling-in-the-ventral-hippocampus-to-regulate-mesolimbic-dopamine-activity-social-interaction-and-memory-processing
#3
Cecilia Kramar, Michael Loureiro, Justine Renard, Steven R Laviolette
Introduction: The GPR55 receptor has been identified as an atypical cannabinoid receptor and is implicated in various physiological processes. However, its functional role in the central nervous system is not currently understood. The presence of GPR55 receptor in neural regions such as the ventral hippocampus (vHipp), which is critical for cognition, recognition memory, and affective processing, led us to hypothesize that intra-vHipp GPR55 transmission may modulate mesolimbic activity states and related behavioral phenomena...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/28826543/cannabinoids-and-pain-sites-and-mechanisms-of-action
#4
Katarzyna Starowicz, David P Finn
The endocannabinoid system, consisting of the cannabinoid1 receptor (CB1R) and cannabinoid2 receptor (CB2R), endogenous cannabinoid ligands (endocannabinoids), and metabolizing enzymes, is present throughout the pain pathways. Endocannabinoids, phytocannabinoids, and synthetic cannabinoid receptor agonists have antinociceptive effects in animal models of acute, inflammatory, and neuropathic pain. CB1R and CB2R located at peripheral, spinal, or supraspinal sites are important targets mediating these antinociceptive effects...
2017: Advances in Pharmacology
https://www.readbyqxmd.com/read/28826536/cannabinoid-receptor-related-orphan-g-protein-coupled-receptors
#5
Andrew Irving, Ghayth Abdulrazzaq, Sue L F Chan, June Penman, Jenni Harvey, Stephen P H Alexander
Of the druggable group of G protein-coupled receptors in the human genome, a number remain which have yet to be paired with an endogenous ligand-orphan GPCRs. Among these 100 or so entities, 3 have been linked to the cannabinoid system. GPR18, GPR55, and GPR119 exhibit limited sequence homology with the established CB1 and CB2 cannabinoid receptors. However, the pharmacology of these orphan receptors displays overlap with CB1 and CB2 receptors, particularly for GPR18 and GPR55. The linking of GPR119 to the cannabinoid receptors is less convincing and emanates from structural similarities of endogenous ligands active at these GPCRs, but which do not cross-react...
2017: Advances in Pharmacology
https://www.readbyqxmd.com/read/28807673/gpr55-a-therapeutic-target-for-parkinson-s-disease
#6
Marta Celorrio, Estefanía Rojo-Bustamante, Diana Fernández-Suárez, Elena Sáez, Ander Estella-Hermoso de Mendoza, Christa E Müller, María J Ramírez, Julen Oyarzábal, Rafael Franco, María S Aymerich
The GPR55 receptor is expressed abundantly in the brain, especially in the striatum, suggesting it might fulfill a role in motor function. Indeed, motor behavior is impaired in mice lacking GPR55, which also display dampened inflammatory responses. Abnormal-cannabidiol (Abn-CBD), a synthetic cannabidiol (CBD) isomer, is a GPR55 agonist that may serve as a therapeutic agent in the treatment of inflammatory diseases. In this study, we explored whether modulating GPR55 could also represent a therapeutic approach for the treatment of Parkinson's disease (PD)...
August 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28800762/the-novel-cannabinoid-receptor-gpr55-mediates-anxiolytic-like-effects-in-the-medial-orbital-cortex-of-mice-with-acute-stress
#7
Qi-Xin Shi, Liu-Kun Yang, Wen-Long Shi, Lu Wang, Shi-Meng Zhou, Shao-Yu Guan, Ming-Gao Zhao, Qi Yang
The G protein-coupled receptor 55 (GPR55) is a novel cannabinoid receptor, whose exact role in anxiety remains unknown. The present study was conducted to explore the possible mechanisms by which GPR55 regulates anxiety and to evaluate the effectiveness of O-1602 in the treatment of anxiety-like symptoms. Mice were exposed to two types of acute stressors: restraint and forced swimming. Anxiety behavior was evaluated using the elevated plus maze and the open field test. We found that O-1602 alleviated anxiety-like behavior in acutely stressed mice...
August 11, 2017: Molecular Brain
https://www.readbyqxmd.com/read/28767505/age-dependent-plasticity-in-endocannabinoid-modulation-of-pain-processing-through-postnatal-development
#8
Charlie H-T Kwok, Ian M Devonshire, Amer Imraish, Charles M Greenspon, Stevie Lockwood, Catherine Fielden, Andrew Cooper, Stephen Woodhams, Sarir Sarmad, Catherine A Ortori, David A Barrett, David Kendall, Andrew J Bennett, Victoria Chapman, Gareth J Hathway
Significant age and experience-dependent remodelling of spinal and supraspinal neural networks occur resulting in altered pain responses in early life. In adults endogenous opioid peptide and endocannabinoid (ECs) pain control systems exist which modify pain responses but the role they play in acute responses to pain and postnatal neurodevelopment is unknown. Here we have studied the changing role of the ECs in brainstem nuclei essential for the control of nociception from birth to adulthood in both rat and human...
August 1, 2017: Pain
https://www.readbyqxmd.com/read/28750813/methods-for-the-development-of-in-silico-gpcr-models
#9
Paula Morales, Dow P Hurst, Patricia H Reggio
The Reggio group has constructed computer models of the inactive and G-protein-activated states of the cannabinoid CB1 and CB2 receptors, as well as, several orphan receptors that recognize a subset of cannabinoid compounds, including GPR55 and GPR18. These models have been used to design ligands, mutations, and covalent labeling studies. The resultant second-generation models have been used to design ligands with improved affinity, efficacy, and subtype selectivity. Herein, we provide a guide for the development of GPCR models using the most recent orphan receptor studied in our lab, GPR3...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28741686/gpr55-receptor-antagonist-decreases-glycolytic-activity-in-panc-1-pancreatic-cancer-cell-line-and-tumor-xenografts
#10
Michel Bernier, Jonathan Catazaro, Nagendra S Singh, Artur Wnorowski, Anna Boguszewska-Czubara, Krzysztof Jozwiak, Robert Powers, Irving W Wainer
The Warburg effect is a predominant metabolic pathway in cancer cells characterized by enhanced glucose uptake and its conversion to l-lactate and is associated with upregulated expression of HIF-1α and activation of the EGFR-MEK-ERK, Wnt-β-catenin, and PI3K-AKT signaling pathways. (R,R')-4'-methoxy-1-naphthylfenoterol ((R,R')-MNF) significantly reduces proliferation, survival, and motility of PANC-1 pancreatic cancer cells through inhibition of the GPR55 receptor. We examined (R,R')-MNF's effect on glycolysis in PANC-1 cells and tumors...
July 25, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28726104/n-acyl-dopamines-induce-apoptosis-in-pc12-cell-line-via-the-gpr55-receptor-activation
#11
M G Akimov, A M Ashba, N M Gretskaya, V V Bezuglov
Dopamine amides of arachidonic, docosahexaenoic, and oleic acids were found to induce apoptosis in PC12 cells, which was blocked exclusively by antagonists and preincubation agonists of the receptor GPR55, belonging to the group of non-CB1/CB2 receptors.
May 2017: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28698140/n-arachidonoyl-glycine-another-endogenous-agonist-of-gpr55
#12
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...
September 2, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28673732/design-synthesis-and-biological-evaluation-of-gpr55-agonists
#13
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...
August 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28653801/a-putative-lysophosphatidylinositol-receptor-gpr55-modulates-hippocampal-synaptic-plasticity
#14
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...
September 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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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