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https://www.readbyqxmd.com/read/29681156/fluorescent-labeled-selective-adenosine-a2b-receptor-antagonist-enables-competition-binding-assay-by-flow-cytometry
#1
Meryem Köse, Sabrina Gollos, Tadeusz Karcz, Amelie Fiene, Fabian Heisig, Andrea Behrenswerth, Katarzyna J Kiec-Kononowicz, Vigneshwaran Namasivayam, Christa E Müller
Fluorescent ligands represent powerful tools for biological studies and are considered as attractive alternatives to radioligands. In this study, we developed fluorescent antagonists for A2B adenosine receptors (A2BARs), which are targeted by anti-asthmatic xanthines and were proposed as novel targets in immuno-oncology. Our approach was to merge a small BODIPY derivative with the pharmacophore of 8-substituted xanthine derivatives. Based on the design, synthesis and evaluation of model compounds several fluorescent ligands were synthesized...
April 22, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29473361/-effects-of-electroacupuncture-on-the-expression-of-adenosine-receptors-in-the-heart-tissue-of-myocardial-ischemia-rats
#2
Shengfeng Lu, Yuexia Tang, Yajuan Ding, Meiling Yu, Shuping Fu, Bingmei Zhu
OBJECTIVE: To explore the impact of electroacupuncture (EA) on the protein expression of adenosine receptors in the heart of the rats with myocardial ischemia (MI). METHODS: Thirty healthy male SD rats were divided randomly into a control group ( n =6), a model group ( n =12) and an EA group ( n =12). We ligated the left anterior descending artery (LAD) for MI model in the model group and EA group, and exposed the heart after opening the chest without ligation in the control group...
February 12, 2018: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
https://www.readbyqxmd.com/read/29387112/estrogen-stimulates-adenosine-receptor-expression-subtypes-in-human-breast-cancer-mcf-7-cell-line
#3
Azam Mohamadi, Mahmoud Aghaei, Mojtaba Panjehpour
Estrogen is a steroid hormone that plays a key role in the development and regulation of reproductive system. It has been shown that estrogen is related to breast cancer development through binding to its receptors. In order to uncover the estrogen effects on adenosine receptor expression, estrogen-positive MCF-7 cells were used to treat with agonist and antagonist of estrogen and then the mRNA expression of adenosine receptor subtypes were evaluated. Estrogen-positive MCF-7 cells were treated with various concentrations of 17β estradiol (E2) as an estrogen agonist, and ICI 182,780 as an estrogen antagonist...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29225130/on-the-g-protein-coupling-selectivity-of-the-native-a-2b-adenosine-receptor
#4
Zhan-Guo Gao, Asuka Inoue, Kenneth A Jacobson
A2B adenosine receptor (A2B AR) activation induces Gs-dependent cyclic AMP accumulation. However, A2B AR 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 1321 N1 astrocytoma, HEK293, and T24 bladder cancer cells endogenously expressing human A2B AR, 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, A2B AR-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
#5
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...
February 2018: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/29149731/purinergic-drug-targets-for-gastrointestinal-disorders
#6
REVIEW
Geoffrey Burnstock, Kenneth A Jacobson, Fievos L Christofi
Purinergic receptors are implicated in the pathogenesis of gastrointestinal disorders and are being explored as potential therapeutic targets. Gut inflammation releases ATP that acts on neuronal, glial, epithelial and immune cells. Purinergic signalling in glia and neurons is implicated in enteric neuropathies. Inflammation activates glia to increase ATP release and alter purinergic signalling. ATP release causes neuron death and gut motor dysfunction in colitis via a P2X7-dependent neural-glial pathway and a glial purinergic-connexin-43 pathway...
December 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/29125553/structure-based-design-of-potent-and-selective-ligands-at-the-four-adenosine-receptors
#7
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/29108754/extracellular-adenosine-produced-by-ecto-5-nucleotidase-cd73-regulates-macrophage-pro-inflammatory-responses-nitric-oxide-production-and-favors-salmonella-persistence
#8
Matthew G Costales, Mohammad Samiul Alam, Christopher Cavanaugh, Kristina M Williams
Surface enzymes CD39 (nucleoside triphosphate dephosphorylase) and CD73 (ecto-5'-nucleotidase) mediate the synthesis of extracellular adenosine that can regulate immune responses. Adenosine produced by CD39/CD73 acts via adenosine receptors (ARs). CD73 is expressed by a variety of cell types and mediates anti-inflammatory responses. Because efficient innate immune responses are required for clearance of Salmonella infection, we investigated the role of CD73 in macrophage function, including phagocytosis, intracellular killing of Salmonella, and anti-bacterial pro-inflammatory responses to Salmonella-whole cell lysate (ST-WCL) or Salmonella infection...
January 30, 2018: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/29106905/characterisation-of-endogenous-a-2a-and-a-2b-receptor-mediated-cyclic-amp-responses-in-hek-293-cells-using-the-glosensor%C3%A2-biosensor-evidence-for-an-allosteric-mechanism-of-action-for-the-a-2b-selective-antagonist-psb-603
#9
Joelle Goulding, Lauren T May, Stephen J Hill
Endogenous adenosine A2B receptors (A2B AR) mediate cAMP accumulation in HEK 293 cells. Here we have used a biosensor to investigate the mechanism of action of the A2B AR 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 A2A AR 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...
January 2018: Biochemical Pharmacology
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
#10
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/28982732/adenosine-receptors-differentially-regulate-type-2-cytokine-production-by-il-33-activated-bone-marrow-cells-ilc2s-and-macrophages
#11
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 A2B ARs suppress the production of both IL-5 and IL-13 by ILC2s, whereas A2A ARs augment IL-5 production and fail to affect IL-13 release...
February 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28893353/the-cholangiocyte-adenosine-il-6-axis-regulates-survival-during-biliary-cirrhosis
#12
Elise G Lavoie, Michel Fausther, Jessica R Goree, Jonathan A Dranoff
Epithelial response to injury is critical to the pathogenesis of biliary cirrhosis, and IL-6 has been suggested as a mediator of this phenomenon. Several liver cell types can secrete IL-6 following activation by various signaling molecules including circulating adenosine. The aims of this study were to assess whether adenosine can induce IL-6 secretion by cholangiocytes via the A2b adenosine receptor (A2bAR) and to determine the effect of A2bAR-sensitive IL-6 release on injury response in biliary cirrhosis...
November 27, 2017: Gene Expression
https://www.readbyqxmd.com/read/28529484/targeting-adenosine-receptors-for-the-treatment-of-cardiac-fibrosis
#13
REVIEW
Elizabeth A Vecchio, Paul J White, Lauren T May
Adenosine is a ubiquitous molecule with key regulatory and cytoprotective mechanisms at times of metabolic imbalance in the body. Among a plethora of physiological actions, adenosine has an important role in attenuating ischaemia-reperfusion injury and modulating the ensuing fibrosis and tissue remodeling following myocardial damage. Adenosine exerts these actions through interaction with four adenosine G protein-coupled receptors expressed in the heart. The adenosine A2B receptor (A2BAR) is the most abundant adenosine receptor (AR) in cardiac fibroblasts and is largely responsible for the influence of adenosine on cardiac fibrosis...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28368607/enantiospecific-recognition-at-the-a2b-adenosine-receptor-by-alkyl-2-cyanoimino-4-substituted-6-methyl-1-2-3-4-tetrahydropyrimidine-5-carboxylates
#14
Carlos Carbajales, Jhonny Azuaje, Ana Oliveira, María I Loza, José Brea, María I Cadavid, Christian F Masaguer, Xerardo García-Mera, Hugo Gutiérrez-de-Terán, Eddy Sotelo
A novel family of structurally simple, potent, and selective nonxanthine A2BAR ligands was identified, and its antagonistic behavior confirmed through functional experiments. The reported alkyl 2-cyanoimino-4-substituted-6-methyl-1,2,3,4-tetrahy-dropyrimidine-5-carboxylates (16) were designed by bioisosteric replacement of the carbonyl group at position 2 in a series of 3,4-dihydropyrimidin-2-ones. The scaffold (16) documented herein contains a chiral center at the heterocycle. Accordingly, the most attractive ligand of the series [(±)16b, Ki = 24...
April 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28344125/capadenoson-a-clinically-trialed-partial-adenosine-a-1-receptor-agonist-can-stimulate-adenosine-a-2b-receptor-biased-agonism
#15
Jo-Anne Baltos, Elizabeth A Vecchio, Matthew A Harris, Cheng Xue Qin, Rebecca H Ritchie, Arthur Christopoulos, Paul J White, Lauren T May
The adenosine A2B receptor (A2B AR) has been identified as an important therapeutic target in cardiovascular disease, however in vitro and in vivo targeting has been limited by the paucity of pharmacological tools, particularly potent agonists. Interestingly, 2-((6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)-2-pyridinyl)thio)acetamide (BAY60-6583), a potent and subtype-selective A2B AR agonist, has the same core structure as 2-amino-6-[[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methylsulfanyl]-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitril (capadenoson)...
July 1, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28266889/lung-injury-pathways-adenosine-receptor-2b-signaling-limits-development-of-ischemic-bronchiolitis-obliterans-organizing-pneumonia
#16
John C Densmore, Terry R Schaid, Paul M Jeziorczak, Meetha Medhora, Said Audi, Shraddha Nayak, John Auchampach, Melinda R Dwinell, Aron M Geurts, Elizabeth R Jacobs
Purpose/Aim of the Study: Adenosine signaling was studied in bronchiolitis obliterans organizing pneumonia (BOOP) resulting from unilateral lung ischemia. MATERIALS AND METHODS: Ischemia was achieved by either left main pulmonary artery or complete hilar ligation. Sprague-Dawley (SD) rats, Dahl salt sensitive (SS) rats and SS mutant rat strains containing a mutation in the A2B adenosine receptor gene (Adora2b) were studied. Adenosine concentrations were measured in bronchoalveolar lavage (BAL) by HPLC...
February 2017: Experimental Lung Research
https://www.readbyqxmd.com/read/28137910/osteogenesis-is-improved-by-low-tumor-necrosis-factor-alpha-concentration-through-the-modulation-of-gs-coupled-receptor-signals
#17
Simona Daniele, Letizia Natali, Chiara Giacomelli, Pietro Campiglia, Ettore Novellino, Claudia Martini, Maria Letizia Trincavelli
In the early phase of bone damage, low concentrations of the cytokine tumor necrosis factor alpha (TNF-α) favor osteoblast differentiation. In contrast, chronic high doses of the same cytokine contribute to bone loss, demonstrating opposite effects depending on its concentration and on the time of exposure. In the bone microenvironment, TNF-α modulates the expression/function of different G protein-coupled receptors (GPCRs) and of their regulatory proteins, GPCR-regulated kinases (GRKs), thus dictating their final biological outcome in controlling bone anabolic processes...
April 15, 2017: Molecular and Cellular Biology
https://www.readbyqxmd.com/read/28054654/aminophylline-suppresses-stress-induced-visceral-hypersensitivity-and-defecation-in-irritable-bowel-syndrome
#18
Teita Asano, Ken-Ichiro Tanaka, Arisa Tada, Hikaru Shimamura, Rikako Tanaka, Hiroki Maruoka, Mitsuko Takenaga, Tohru Mizushima
Pharmacological therapy for irritable bowel syndrome (IBS) has not been established. In order to find candidate drugs for IBS with diarrhea (IBS-D), we screened a compound library of drugs clinically used for their ability to prevent stress-induced defecation and visceral hypersensitivity in rats. We selected the bronchodilator aminophylline from this library. Using a specific inhibitor for each subtype of adenosine receptors (ARs) and phosphodiesterases (PDEs), we found that both A2BARs and PDE4 are probably mediated the inhibitory effect of aminophylline on wrap restraint stress (WRS)-induced defecation...
January 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/27974241/a-2b-adenosine-receptors-stimulate-il-6-production-in-primary-murine-microglia-through-p38-mapk-kinase-pathway
#19
Stefania Merighi, Serena Bencivenni, Fabrizio Vincenzi, Katia Varani, Pier Andrea Borea, Stefania Gessi
The hallmark of neuroinflammation is the activation of microglia, the immunocompetent cells of the CNS, releasing a number of proinflammatory mediators implicated in the pathogenesis of neuronal diseases. Adenosine is an ubiquitous autacoid regulating several microglia functions through four receptor subtypes named A1 , A2A , A2B and A3 (ARs), that represent good targets to suppress inflammation occurring in CNS. Here we investigated the potential role of ARs in the modulation of IL-6 secretion and cell proliferation in primary microglial cells...
March 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27871900/insulin-adenosine-axis-linked-signalling
#20
REVIEW
Luis Silva, Mario Subiabre, Joaquín Araos, Tamara Sáez, Rocío Salsoso, Fabián Pardo, Andrea Leiva, Rody San Martín, Fernando Toledo, Luis Sobrevia
Regulation of blood flow depends on systemic and local release of vasoactive molecules such as insulin and adenosine. These molecules cause vasodilation by activation of plasma membrane receptors at the vascular endothelium. Adenosine activates at least four subtypes of adenosine receptors (A1AR, A2AAR, A2BAR, A3AR), of which A2AAR and A2BAR activation leads to increased cAMP level, generation of nitric oxide, and relaxation of the underlying smooth muscle cell layer. Vasodilation caused by adenosine also depends on plasma membrane hyperpolarization due to either activation of intermediate-conductance Ca(2+)-activated K(+) channels in vascular smooth muscle or activation of ATP-activated K(+) channels in the endothelium...
November 19, 2016: Molecular Aspects of Medicine
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