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Adenosine A2B receptor

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https://www.readbyqxmd.com/read/29329032/targeting-expression-of-adenosine-receptors-during-hypoxia-induced-angiogenesis-a-study-using-zebrafish-model
#1
Navina Panneerselvan, Malathi Ragunathan
Hypoxia is known to be a major player during pathological angiogenesis and adenosine as a negative feedback signaling to maintain oxygen delivery in pathological ischemic condition. We mimicked hypoxic condition and studied angiogenesis by inducing adenosine receptors using forskolin, a plant compound and NECA analogue of adenosine using zebrafish model. Vascular endothelial growth factor (VEGF) is known to play a key role during pathological angiogenesis and regulated by the factors HIF1a under hypoxic condition and recently Notch is proposed to play a negative feedback loop mechanism along with VEGF signaling but the role of adenosine receptor during the process is not known...
January 9, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29322373/epac-is-required-for-exogenous-and-endogenous-stimulation-of-adenosine-a2b-receptor-for-inhibition-of-angiotensin-ii-induced-collagen-synthesis-and-myofibroblast-differentiation
#2
Sarawuth Phosri, Kwanchai Bunrukchai, Warisara Parichatikanond, Vilasinee H Sato, Supachoke Mangmool
Angiotensin II (Ang II) plays an important role on the pathogenesis of cardiac fibrosis. Prolong and overstimulation of angiotensin II type 1 receptor with Ang II-induced collagen synthesis and myofibroblast differentiation in cardiac fibroblasts, leading to cardiac fibrosis. Although adenosine and its analogues are known to have cardioprotective effects, the mechanistic by which adenosine A2 receptors (A2Rs) inhibit Ang II-induced cardiac fibrosis is not clearly understood. In the present study, we examined the effects of exogenous adenosine and endogenous adenosine on Ang II-induced collagen and myofibroblast differentiation determined by α-smooth muscle action (α-SMA) overexpression and their underlying signal transduction...
January 10, 2018: Purinergic Signalling
https://www.readbyqxmd.com/read/29315226/unfolding-role-of-a-danger-molecule-adenosine-signaling-in-modulation-of-microbial-infection-and-host-cell-response
#3
REVIEW
Jaden S Lee, Özlem Yilmaz
Ectonucleotidases CD39 and CD73, specific nucleotide metabolizing enzymes located on the surface of the host, can convert a pro-inflammatory environment driven by a danger molecule extracellular-ATP to an adenosine-mediated anti-inflammatory milieu. Accordingly, CD39/CD73 signaling have has strongly implicated in modulating the intensity, duration, and composition of purinergic danger signals delivered to host. Recent studies have eluted potential roles for CD39 and CD73 in selective triggering of a variety of host immune cells and molecules in the presence of pathogenic microorganisms or microbial virulence molecules...
January 9, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29249971/inhibition-of-a2a-adenosine-receptor-signaling-in-cancer-cells-proliferation-by-the-novel-antagonist-tp455
#4
Stefania Gessi, Serena Bencivenni, Enrica Battistello, Fabrizio Vincenzi, Vittoria Colotta, Daniela Catarzi, Flavia Varano, Stefania Merighi, Pier Andrea Borea, Katia Varani
Several evidences indicate that the ubiquitous nucleoside adenosine, acting through A1, A2A, A2B, and A3 receptor (AR) subtypes, plays crucial roles in tumor development. Adenosine has contrasting effects on cell proliferation depending on the engagement of different receptor subtypes in various tumors. The involvement of A2AARs in human A375 melanoma, as well as in human A549 lung and rat MRMT1 breast carcinoma proliferation has been evaluated in view of the availability of a novel A2AAR antagonist, with high affinity and selectivity, named as 2-(2-furanyl)-N5-(2-methoxybenzyl)[1,3]thiazolo[5,4-d]pyrimidine-5,7-diammine (TP455)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29225130/on-the-g-protein-coupling-selectivity-of-the-native-a2b-adenosine-receptor
#5
Zhan-Guo Gao, Asuka Inoue, Kenneth A Jacobson
A2B adenosine receptor (A2BAR) activation induces Gs-dependent cyclic AMP accumulation. However, A2BAR G protein-coupling to other signaling events, e.g. ERK1/2 and calcium, is not well documented. We explored Gi, Gq/11 and Gs coupling in 1321N1 astrocytoma, HEK293, and T24 bladder cancer cells endogenously expressing human A2BAR, using NECA or nonnucleoside BAY60-6583 as agonist, selective Gi, Gs and Gq/11 blockers, and CRISPR/Cas9-based Gq- and Gs-null HEK293 cells. In HEK293 cells, A2BAR-mediated ERK1/2 activity occurred via both Gi and Gs, but not Gq/11...
December 7, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29218545/a2b-adenosine-receptor-agonist-induces-cell-cycle-arrest-and-apoptosis-in-breast-cancer-stem-cells-via-erk1-2-phosphorylation
#6
Seyyed Mehdi Jafari, Hamid Reza Joshaghani, Mojtaba Panjehpour, Mahmoud Aghaei
PURPOSE: It has been reported that cancer stem cells (CSCs) may play a crucial role in the development, recurrence and metastasis of breast cancer. Targeting signaling pathways in CSCs is considered to be a promising strategy for the treatment of cancer. Here, we investigated the role of the A2B adenosine receptor (A2BAR) and its associated signaling pathways in governing the proliferation and viability of breast cancer cell line derived CSCs. METHODS: CSCs were isolated from the breast cancer cell lines MCF-7 and MDA-MB-231 using a mammosphere assay...
December 7, 2017: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/29203139/structural-mapping-of-adenosine-receptor-mutations-ligand-binding-and-signaling-mechanisms
#7
REVIEW
Willem Jespers, Anke C Schiedel, Laura H Heitman, Robert M Cooke, Lisa Kleene, Gerard J P van Westen, David E Gloriam, Christa E Müller, Eddy Sotelo, Hugo Gutiérrez-de-Terán
The four adenosine receptors (ARs), A1, A2A, A2B, and A3, constitute a subfamily of G protein-coupled receptors (GPCRs) with exceptional foundations for structure-based ligand design. The vast amount of mutagenesis data, accumulated in the literature since the 1990s, has been recently supplemented with structural information, currently consisting of several inactive and active structures of the A2A and inactive conformations of the A1 ARs. We provide the first integrated view of the pharmacological, biochemical, and structural data available for this receptor family, by mapping onto the relevant crystal structures all site-directed mutagenesis data, curated and deposited at the GPCR database (available through http://www...
December 1, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/29163164/lassbio-897-reduces-lung-injury-induced-by-silica-particles-in-mice-potential-interaction-with-the-a2a-receptor
#8
Vinicius F Carvalho, Tatiana P T Ferreira, Ana C S de Arantes, François Noël, Roberta Tesch, Carlos M R Sant'Anna, Eliezer J L Barreiro, Carlos A M Fraga, Patrícia M Rodrigues E Silva, Marco A Martins
Silicosis is a lethal fibro-granulomatous pulmonary disease highly prevalent in developing countries, for which no proper therapy is available. Among a small series of N-acylhydrazones, the safrole-derived compound LASSBio-897 (3-thienylidene-3, 4-methylenedioxybenzoylhydrazide) raised interest due to its ability to bind to the adenosine A2A receptor. Here, we evaluated the anti-inflammatory and anti-fibrotic potential of LASSBio-897, exploring translation to a mouse model of silicosis and the A2A receptor as a site of action...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29125553/structure-based-design-of-potent-and-selective-ligands-at-the-four-adenosine-receptors
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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