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Adenosine A2B receptor

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https://www.readbyqxmd.com/read/29125553/structure-based-design-of-potent-and-selective-ligands-at-the-four-adenosine-receptors
#1
Willem Jespers, Ana Oliveira, Rubén Prieto-Díaz, María Majellaro, Johan Åqvist, Eddy Sotelo, Hugo Gutiérrez-de-Terán
The four receptors that signal for adenosine, A₁, A2A, A2B and A₃ ARs, belong to the superfamily of G protein-coupled receptors (GPCRs). They mediate a number of (patho)physiological functions and have attracted the interest of the biopharmaceutical sector for decades as potential drug targets. The many crystal structures of the A2A, and lately the A₁ ARs, allow for the use of advanced computational, structure-based ligand design methodologies. Over the last decade, we have assessed the efficient synthesis of novel ligands specifically addressed to each of the four ARs...
November 10, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29119938/adenosine-receptor-ligands-on-cancer-therapy-a-review-of-patent-literature
#2
Carmen Diniz, Joana Beatriz Sousa, Paula Fresco, Jorge Goncalves
BACKGROUND: Adenosine is a purine, with an adenine group and a ribose sugar, formed endogenously by ATP catabolism both intracellularly and extracellularly. Among the medicinal features of adenosine and of its receptors (A1, A2A, A2B and A3), anticancer activity has been an intense field of research. The anticancer potential of adenosine receptor ligands has been brought forefront of research and evidenced in innumerous research articles and patents. OBJECTIVE: The present review focuses on the patent literature from 2002 onwards (2002-2017)...
November 7, 2017: Recent Patents on Anti-cancer Drug Discovery
https://www.readbyqxmd.com/read/29116551/anti-inflammatory-effect-of-a-novel-locally-acting-a2a-receptor-agonist-in-a-rat-model-of-oxazolone-induced-colitis
#3
L Antonioli, A El-Tayeb, C Pellegrini, M Fornai, O Awwad, G Giustarini, G Natale, L Ryskalin, Z H Németh, C E Müller, C Blandizzi, R Colucci
Adenosine represents a powerful modulating factor, which has been shown to orchestrate the scope, duration, and remission of the inflammatory response through the activation of four specific receptors, classified as A1, A2A, A2B, and A3, all being widely expressed in a variety of immune cells. Several selective A2A receptor agonists have displayed anti-inflammatory effects, through the suppression of IL-12, TNF, and IFN-γ production by monocytes and lymphocytes, in the setting of chronic intestinal inflammation...
November 8, 2017: Purinergic Signalling
https://www.readbyqxmd.com/read/29106905/characterisation-of-endogenous-a2a-and-a2b-receptor-mediated-cyclic-amp-responses-in-hek-293-cells-using-the-glosensor%C3%A2-biosensor-evidence-for-an-allosteric-mechanism-of-action-for-the-a2b-selective-antagonist-psb-603
#4
Joelle Goulding, Lauren T May, Stephen J Hill
Endogenous adenosine A2B receptors (A2BAR) mediate cAMP accumulation in HEK 293 cells. Here we have used a biosensor to investigate the mechanism of action of the A2BAR antagonist PSB 603 in HEK 293 cells. The A2A agonist CGS 21680 elicited a small response in these cells (circa 20% of that obtained with NECA), suggesting that they also contain a small population of A2A receptors. The responses to NECA and adenosine were antagonised by PSB 603, but not by the selective A2AAR antagonist SCH 58261. In contrast, CGS 21680 responses were not antagonised by high concentrations of PSB 603, but were sensitive to inhibition by SCH 58261...
October 26, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29099770/adenosine-a2b-receptors-an-optional-target-for-the-management-of-irritable-bowel-syndrome-with-diarrhea
#5
REVIEW
Teita Asano, Mitsuko Takenaga
Irritable bowel syndrome (IBS) is a functional gastrointestinal disorder, with the characteristic symptoms of chronic abdominal pain and altered bowel habits (diarrhea, constipation, or both). IBS is a highly prevalent condition, which negatively affects quality of life and is a significant burden on global healthcare costs. Although many pharmacological medicines have been proposed to treat IBS, including those targeting receptors, channels, and chemical mediators related to visceral hypersensitivity, successful pharmacotherapy for the disease has not been established...
November 3, 2017: Journal of Clinical Medicine
https://www.readbyqxmd.com/read/29047264/the-inactivation-of-erk1-2-p38-and-nf-kb-is-involved-in-the-down-regulation-of-osteoclastogenesis-and-function-by-a2b-adenosine-receptor-stimulation
#6
Bo Hyun Kim, Ju Hee Oh, Na Kyung Lee
A2B adenosine receptor (A2BAR) is known to be the regulator of bone homeostasis, but its regulatory mechanisms in osteoclast formation are less well-defined. Here, we demonstrate the effect of A2BAR stimulation on osteoclast differentiation and activity by RANKL. A2BAR was expressed in bone marrow-derived monocyte/macrophage (BMM) and RANKL increased A2BAR expression during osteoclastogenesis. A2BAR stimulation with its specific agonist BAY 60-6583 was sufficient to inhibit the activation of ERK1/2, p38 MAP kinases and NF-κB by RANKL as well as it abrogated cell-cell fusion in the late stage of osteoclast differentiation...
October 2017: Molecules and Cells
https://www.readbyqxmd.com/read/29018360/adenosine-direct-and-indirect-actions-on-gastric-acid-secretion
#7
REVIEW
Rosa M Arin, Adriana Gorostidi, Hiart Navarro-Imaz, Yuri Rueda, Olatz Fresnedo, Begoña Ochoa
Composed by a molecule of adenine and a molecule of ribose, adenosine is a paradigm of recyclable nucleoside with a multiplicity of functions that occupies a privileged position in the metabolic and regulatory contexts. Adenosine is formed continuously in intracellular and extracellular locations of all tissues. Extracellular adenosine is a signaling molecule, able to modulate a vast range of physiologic responses in many cells and organs, including digestive organs. The adenosine A1, A2A, A2B, and A3 receptors are P1 purinergic receptors, G protein-coupled proteins implicated in tissue protection...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28990513/protective-effects-of-the-caffeine-against-neurodegenerative-diseases
#8
Ester Tellone, Antonio Galtieri, Annamaria Russo, Silvana Ficarra
Caffeine is one of the most consumed stimulant of the central nervous system. Similar to those of other stimulants, its effects are to improve brain activity and stimulate cognition learning and memory. Caffeine affects the brain by acting mainly as a non-selective blocker of the adenosine receptors (A1, A2A, A2B, and A3). The purpose of this review article is to provide an overview on the neurobiochemical impact of caffeine, focusing on the ability of the drug to effectively counteract several neurodegenerative disorders such as Alzheimer's, Parkinson's, Huntington's diseases, Multiple sclerosis and Amyotrophic lateral sclerosis and Epilepsy...
October 9, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28988061/nanolayered-hybrid-mediates-synergistic-co-delivery-of-ligand-and-ligation-activator-for-inducing-stem-cell-differentiation-and-tissue-healing
#9
Heemin Kang, Minkyu Kim, Qian Feng, Sien Lin, Kongchang Wei, Rui Li, Chan Ju Choi, Tae-Hyun Kim, Gang Li, Jae-Min Oh, Liming Bian
Cellular behaviors, such as differentiation, are regulated by complex ligation processes involving cell surface receptors, which can be activated by various divalent metal cations. The design of nanoparticle for co-delivery of ligand and ligation activator can offer a novel strategy to synergistically stimulate ligation processes in vivo. Here, we present a novel layered double hydroxide (LDH)-based nanohybrid (MgFe-Ado-LDH), composed of layered MgFe hydroxide nanocarriers sandwiching the adenosine cargo molecule, maintained through an electrostatic balance, to co-deliver the adenosine (Ado) ligand from the interlayer spacing and the Mg(2+) ion (ligation activator) through the dissolution of the MgFe nanocarrier itself...
September 29, 2017: Biomaterials
https://www.readbyqxmd.com/read/28982732/adenosine-receptors-differentially-regulate-type-2-cytokine-production-by-il-33-activated-bone-marrow-cells-ilc2s-and-macrophages
#10
Balázs Csóka, Zoltán H Németh, Claudia U Duerr, Jörg H Fritz, Pál Pacher, György Haskó
Group 2 innate lymphoid cells (ILC2s) represent a rapid source of type 2 cytokines, such as IL-5 and IL-13, and play an important role in orchestrating type 2 immune response. Adenosine is an endogenous purine nucleoside, a catabolite of ATP that binds and activates ≥1 of 4 transmembrane G protein-coupled cell-surface adenosine receptors (ARs)-A1, A2A, A2B, and A3 Here, we studied the role of ARs in the regulation of cytokine production by ILC2s. We found that A2BARs suppress the production of both IL-5 and IL-13 by ILC2s, whereas A2AARs augment IL-5 production and fail to affect IL-13 release...
October 5, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28921456/blood-brain-barrier-in-a-haemophilus-influenzae-type-a-in-vitro-infection-role-of-adenosine-receptors-a2a-and-a2b
#11
N Caporarello, M Olivieri, M Cristaldi, M Scalia, M A Toscano, C Genovese, A Addamo, M Salmeri, G Lupo, C D Anfuso
The blood-brain barrier (BBB) is mainly made up of tightly connected microvascular endothelial cells (BMECs), surrounded by pericytes (BMPCs) which regulate BBB tightness by providing soluble factors that control endothelial proliferation. Haemophilus influenzae type a (Hia) is able to reach the BBB, crossing it, thus causing meningitis. In this study, by using an in vitro model of BBB, performed with human BMECs and human BMPCs in co-culture, we demonstrated that, after Hia infection, the number of hBMPCs decreased whereas the number of hBMECs increased in comparison with non-infected cells...
September 18, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28893553/caffeine-has-no-effect-on-eyeblink-conditioning-in-mice
#12
Anders Rasmussen, Anna C H G Ijpelaar, Chris I De Zeeuw, Henk-Jan Boele
Caffeine is one of the most widely used drugs in the world. In the brain, caffeine acts as an antagonist for the adenosine A1 and A2B receptors. Since A1 receptors are highly concentrated in the cortex of the cerebellum, we hypothesized that caffeine could potentially affect learning tasks that require the cerebellar cortex, such as eyeblink conditioning. To test this hypothesis, we examined the effect of low (5mg/kg) and high (50mg/kg) doses of caffeine, injected intraperitoneally before training, on eyeblink conditioning in mice...
January 30, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/28893353/the-cholangiocyte-adenosine-il6-axis-regulates-survival-during-biliary-cirrhosis
#13
Elise Lavoie, Michel Fausther, Jessica Goree, Jonathan Dranoff
BACKGROUND AND AIMSEpithelial response to injury is critical to the pathogenesis of biliary cirrhosis, and IL6 has been suggested as a mediator of this phenomenon. Several liver cell types can secrete IL6 following activation by various signaling molecules including circulating adenosine. The aims of this study are to assess whether adenosine can induce IL6 secretion by cholangiocytes via the A2b adenosine receptor (A2bAR) and determine the effect of A2bAR-sensitive IL6 release on injury response in biliary cirrhosis...
September 11, 2017: Gene Expression
https://www.readbyqxmd.com/read/28835798/discovery-of-potent-and-selective-a2a-antagonists-with-efficacy-in-animal-models-of-parkinson-s-disease-and-depression
#14
Sujay Basu, Dinesh A Barawkar, Vidya Ramdas, Minakshi Naykodi, Yogesh D Shejul, Meena Patel, Sachin Thorat, Anil Panmand, K Kashinath, Rajesh Bonagiri, Vandna Prasad, Ganesh Bhat, Azfar Quraishi, Sumit Chaudhary, Amol Magdum, Ashwinkumar V Meru, Indraneel Ghosh, Ravi K Bhamidipati, Amol A Raje, Vamsi L M Madgula, Siddhartha De, Sreekanth R Rouduri, Venkata P Palle, Anita Chugh, Narayanan Hariharan, Kasim A Mookhtiar
Adenosine A2A receptor (A2AAdoR) antagonism is a nondopaminergic approach to Parkinson's disease treatment that is under development. Earlier we had reported the therapeutic potential of 7-methoxy-4-morpholino-benzothiazole derivatives as A2AAdoR antagonists. We herein described a novel series of [1,2,4]triazolo[5,1-f]purin-2-one derivatives that displays functional antagonism of the A2A receptor with a high degree of selectivity over A1, A2B, and A3 receptors. Compounds from this new scaffold resulted in the discovery of highly potent, selective, stable, and moderate brain penetrating compound 33...
August 10, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28830843/inhibition-of-tpa-induced-hemorrhagic-transformation-involves-adenosine-a2b-receptor-activation-after-cerebral-ischemia
#15
Qiang Li, Xiaoning Han, Xi Lan, Xiaohua Hong, Qian Li, Yufeng Gao, Tianqi Luo, Qingwu Yang, Raymond C Koehler, Yu Zhai, Jinyuan Zhou, Jian Wang
Tissue plasminogen activator (tPA) is administered after ischemic stroke to dissolve intravascular clots, but its use can lead to hemorrhagic transformation (HT). Therapeutic strategies to reduce hemorrhagic complications of tPA might be of benefit for stroke patients. Adenosine A2b receptor (A2bR) plays pivotal roles in regulating vascular protection in peripheral organs. This study explored whether A2bR agonist BAY 60-6583 reduces hemorrhage risk after tPA usage. Using a rat transient middle cerebral artery occlusion model, we showed that mRNA and protein expression of A2bR increased to a greater extent after ischemia-reperfusion than did expression of the other three adenosine receptors (A1, A2a, and A3)...
December 2017: Neurobiology of Disease
https://www.readbyqxmd.com/read/28827387/retraction-hypoxia-inducible-factor-1%C3%AE-dependent-protection-from-intestinal-ischemia-reperfusion-injury-involves-ecto-5-nucleotidase-cd73-and-the-a2b-adenosine-receptor
#16
Melanie L Hart, Iris C Gorzolla, Jens Schittenhelm, Julee H Dalton, Holger K Eltzschig
No abstract text is available yet for this article.
September 1, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28808842/colonic-motor-dysfunctions-in-a-mouse-model-of-high-fat-diet-induced-obesity-an-involvement-of-a2b-adenosine-receptors
#17
Luca Antonioli, Carolina Pellegrini, Matteo Fornai, Erika Tirotta, Daniela Gentile, Laura Benvenuti, Maria Cecilia Giron, Valentina Caputi, Ilaria Marsilio, Genny Orso, Nunzia Bernardini, Cristina Segnani, Chiara Ippolito, Balázs Csóka, Zoltán H Németh, György Haskó, Carmelo Scarpignato, Corrado Blandizzi, Rocchina Colucci
Adenosine A2B receptors (A2BR) regulate several enteric functions. However, their implication in the pathophysiology of intestinal dysmotility associated with high-fat diet (HFD)-induced obesity has not been elucidated. We investigated the expression of A2BR in mouse colon and their role in the mechanisms underlying the development of enteric dysmotility associated with obesity. Wild-type C57BL/6J mice were fed with HFD (60% kcal from fat) or normocaloric diet (NCD; 18% kcal from fat) for 8 weeks. Colonic A2BR localization was examined by immunofluorescence...
August 14, 2017: Purinergic Signalling
https://www.readbyqxmd.com/read/28791011/leishmania-amazonensis-induced-camp-triggered-by-adenosine-a2b-receptor-is-important-to-inhibit-dendritic-cell-activation-and-evade-immune-response-in-infected-mice
#18
Amanda Braga Figueiredo, Míriam Conceição Souza-Testasicca, Tiago Wilson Patriarca Mineo, Luís Carlos Crocco Afonso
Differently from others Leishmania species, infection by the protozoan parasite L. amazonensis is associated with a lack of antigen-specific T-cell responses. Dendritic cells (DC) are essential for the innate immune response and for directing the differentiation of T-helper lymphocytes. Previously, we showed that L. amazonensis infection impairs DC activation through the activation of adenosine A2B receptor, and here, we evaluated the intracellular events triggered by this receptor in infected cells. To this aim, bone marrow-derived DC from C57BL/6J mice were infected with metacyclic promastigotes of L...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28765173/a2a-adenosine-receptors-control-pancreatic-dysfunction-in-high-fat-diet-induced-obesity
#19
Balázs Csóka, Gábor Törő, Joana Vindeirinho, Zoltán V Varga, Balázs Koscsó, Zoltán H Németh, Endre Kókai, Luca Antonioli, Mara Suleiman, Piero Marchetti, Karolina Cseri, Ádám Deák, László Virág, Pál Pacher, Péter Bai, György Haskó
Adenosine, a key extracellular signaling mediator, regulates several aspects of metabolism by activating 4 G protein-coupled receptors, the A1, A2A, A2B, and A3 adenosine receptors (ARs). The role of A2AARs in regulating high-fat-diet (HFD)-induced metabolic derangements is unknown. To evaluate the role of A2AARs in regulating glucose and insulin homeostasis in obesity, we fed A2AAR knockout (KO) and control mice an HFD for 16 wk to initiate HFD-induced metabolic disorder. We found that genetic deletion of A2AARs caused impaired glucose tolerance in mice fed an HFD...
August 1, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28734062/coumarins-and-adenosine-receptors-new-perceptions-in-structure-affinity-relationships
#20
André Fonseca, Maria João Matos, Santiago Vilar, Sonja Kachler, Karl-Norbert Klotz, Eugenio Uriarte, Fernanda Borges
Adenosine receptors (ARs) subtypes are involved in several physiological and pharmacological processes. Ligands able to selectively modulate one receptor subtype can delay or slow down the progression of diverse diseases. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective ARs ligands based on coumarin scaffold. Therefore, a series 3-phenylcarboxamidocoumarins were synthesised and their affinity for the human ARs subtypes was screened by radioligand binding assays for A1 , A2A and A3 receptors and for A2B by adenylyl cyclase assay...
July 22, 2017: Chemical Biology & Drug Design
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