keyword
MENU ▼
Read by QxMD icon Read
search

Adenosine A2B receptor

keyword
https://www.readbyqxmd.com/read/29771006/the-anti-fibrotic-effect-of-adenosine-a2b-receptor-antagonism-in-a-mouse-model-of-dermal-fibrosis
#1
Harry Karmouty-Quintana, Jose G Molina, Kemly Philip, Chiara Bellocchi, Brent Gudenkauf, Minghua Wu, Ning-Yuan Chen, Scott D Collum, Junsuk Ko, Sandeep K Agarwal, Shervin Assassi, Hongyan Zhong, Michael R Blackburn, Tingting Weng
OBJECTIVE: Systemic sclerosis (SSc - scleroderma) is a chronic disease that affects the skin and various internal organs. Dermal fibrosis is a major component of this disease. The mechanisms that promote dermal fibrosis remain elusive. Elevations in tissue adenosine levels and the subsequent engagement of the pro-fibrotic A2B adenosine receptor (ADORA2B) have been shown to regulate fibrosis in multiple organs including the lung, kidney and penis; however, the role of the ADORA2B in dermal fibrosis has not been investigated...
May 17, 2018: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/29769005/adenosine-synthetic-methods-of-its-derivatives-and-antitumor-activity
#2
Margarita Gutierrez, Francisco Valdes, Victor Luna, Barbara Arevalo, Nelson Brown
Since 1929, several researchers have conducted studies in relation the nucleoside of adenosine (1) mainly distribution identifying, characterizing their biological importance and synthetic chemistry to which this type of molecule has been subjected to obtain multiple of its derivatives. The receptors that interact with adenosine and its derivatives, called purinergic receptors, are classified as A1, A2A, A2B and A3. In the presence of agonists and antagonists, these receptors are involved in various physiological processes and diseases...
May 16, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29752618/tritium-labeled-agonists-as-tools-for-studying-adenosine-a-2b-receptors
#3
Sonja Hinz, Wessam M Alnouri, Ulrich Pleiss, Christa E Müller
A selective agonist radioligand for A2B adenosine receptors (A2B ARs) is currently not available. Such a tool would be useful for labeling the active conformation of the receptors. Therefore, we prepared BAY 60-6583, a potent and functionally selective A2B AR (partial) agonist, in a tritium-labeled form. Despite extensive efforts, however, we have not been able to establish a radioligand binding assay using [3 H]BAY 60-6583. This is probably due to its high non-specific binding and its moderate affinity, which had previously been overestimated based on functional data...
May 11, 2018: Purinergic Signalling
https://www.readbyqxmd.com/read/29747005/is-the-adenosine-a-2b-biased-receptor-a-valuable-target-for-the-treatment-of-pulmonary-arterial-hypertension
#4
REVIEW
Mafalda Bessa-Gonçalves, Bruno Bragança, Eduardo Martins-Dias, Paulo Correia-de-Sá, Ana Patrícia Fontes-Sousa
Pulmonary arterial hypertension (PAH) is a maladaptive disorder characterized by increased pulmonary vascular resistance leading to right ventricular failure and death. Adenosine released by injured tissues, such as the lung and heart, influences tissue remodeling through the activation of adenosine receptors. Evidence regarding activation of the low-affinity A2B AR by adenosine points towards pivotal roles of this receptor in processes associated with both acute and chronic lung diseases. Conflicting results exist concerning the beneficial or detrimental roles of the A2B 'biased' receptor in right ventricular failure secondary to PAH...
May 7, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29740323/the-selective-antagonism-of-adenosine-a-2b-receptors-reduces-the-synaptic-failure-and-neuronal-death-induced-by-oxygen-and-glucose-deprivation-in-rat-ca1-hippocampus-in-vitro
#5
Irene Fusco, Filippo Ugolini, Daniele Lana, Elisabetta Coppi, Ilaria Dettori, Lisa Gaviano, Daniele Nosi, Federica Cherchi, Felicita Pedata, Maria G Giovannini, Anna M Pugliese
Ischemia is a multifactorial pathology characterized by different events evolving in time. Immediately after the ischemic insult, primary brain damage is due to the massive increase of extracellular glutamate. Adenosine in the brain increases dramatically during ischemia in concentrations able to stimulate all its receptors, A1 , A2A , A2B , and A3 . Although adenosine exerts clear neuroprotective effects through A1 receptors during ischemia, the use of selective A1 receptor agonists is hampered by their undesirable peripheral side effects...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29733889/adenosine-promotes-endplate-nachr-channel-activity-in-adult-mouse-skeletal-muscle-fibres-via-low-affinity-p1-receptors
#6
Annalisa Bernareggi, Elisa Ren, Arthur Giniatullin, Elisa Luin, Marina Sciancalepore, Rashid Giniatullin, Paola Lorenzon
Adenosine is a powerful modulator of skeletal neuromuscular transmission, operating via inhibitory or facilitatory purinergic-type P1 receptors. To date, studies have been focused mainly on the effect of adenosine on presynaptic P1 receptors controlling transmitter release. In this study, using two-microelectrode voltage clamp and single channel patch-clamp recording techniques, we have explored potential postsynaptic targets of adenosine and their modulatory effect on nicotinic acetylcholine receptor (nAChR)-mediated synaptic responses in adult mouse skeletal muscle fibres in vitro...
May 4, 2018: Neuroscience
https://www.readbyqxmd.com/read/29731713/cytokine-induced-killer-cells-express-cd39-cd38-cd203a-cd73-ectoenzymes-and-p1-adenosinergic-receptors
#7
Alberto L Horenstein, Antonella Chillemi, Roberta Zini, Valeria Quarona, Nicoletta Bianchi, Rossella Manfredini, Roberto Gambari, Fabio Malavasi, Davide Ferrari
Cytokine-induced killer (CIK) cells, a heterogeneous T cell population obtained by in vitro differentiation of peripheral blood mononuclear cells (PBMC), represent a promising immunological approach in cancer. Numerous studies have explored the role of CD38, CD39, CD203a/PC-1, and CD73 in generating extracellular adenosine (ADO) and thus in shaping the tumor niche in favor of proliferation. The findings shown here reveal that CIK cells are able to produce extracellular ADO via traditional (CD39/CD73) and/or alternative (CD38/CD203a/CD73 or CD203a/CD73) pathways...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29702147/adenosine-signalling-and-the-immune-system-when-a-lot-could-be-too-much
#8
REVIEW
Luca Antonioli, Matteo Fornai, Corrado Blandizzi, Pál Pacher, György Haskó
Adenosine is increasingly recognized as a key mediator of the immune response. Signals delivered by extracellular adenosine are detected and transduced by G-protein-coupled cell-surface receptors, classified into four subtypes: A1 , A2A , A2B and A3 . These receptors, expressed virtually on all immune cells, modulate all aspects of immune/inflammatory responses. These immunoregulatory effects, which are mostly anti-inflammatory, contribute to the general tissue protective effects of adenosine and its receptors...
April 24, 2018: Immunology Letters
https://www.readbyqxmd.com/read/29692248/a2a-adenosine-receptor-antagonists-as-therapeutic-candidates-are-they-still-an-interesting-challenge
#9
Barbara Cacciari, Stephanie Federico, Giampiero Spalluto
In the past decades, many efforts were done to develope ligands for the adenosine receptors, with the purpose to individuate agonists and antagonists affine and selective for each subtypes , named A1, A2A, A2B, and A3. These intense studies allowed a deeper and deeper knowledge of the nature and, moreover, of the pathophysiological roles of all the adenosine receptor subtypes. In particular, the involvment of the A2A adenosine receptor subtype in some physiological mechanisms in the brain, that could be related to important diseases such as the Parkinson's disease, encouraged the research in this field...
April 22, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29681156/fluorescent-labeled-selective-adenosine-a2b-receptor-antagonist-enables-competition-binding-assay-by-flow-cytometry
#10
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/29679502/new-paradigms-in-adenosine-receptor-pharmacology-allostery-oligomerization-and-biased-agonism
#11
REVIEW
Elizabeth A Vecchio, Jo-Anne Baltos, Anh T N Nguyen, Arthur Christopoulos, Paul J White, Lauren T May
Adenosine receptors (ARs) are a family of G protein-coupled receptors (GPCRs) containing four subtypes (A1 AR, A2A AR, A2B AR and A3 AR), all of which bind the ubiquitous nucleoside adenosine. ARs play an important role in physiology and pathophysiology and therefore represent attractive drug targets for a range of conditions. The theoretical framework surrounding AR drug action now extends beyond the notion of prototypical agonism and antagonism to encompass more complex pharmacological concepts. New paradigms include allostery, whereby ligands bind a topographically distinct receptor site from that of the endogenous agonist, homomeric or heteromeric interactions across receptor oligomers and biased agonism; that is, ligand-dependent differential intracellular signalling...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29674631/orally-active-species-independent-novel-a-3-adenosine-receptor-antagonist-protects-against-kidney-injury-in-db-db-mice
#12
Debra Dorotea, Ahreum Cho, Gayoung Lee, Guideock Kwon, Junghwa Lee, Pramod K Sahu, Lak Shin Jeong, Dae Ryong Cha, Hunjoo Ha
Diabetic kidney disease (DKD) is the leading cause of end-stage kidney disease, and the current pharmacological treatment for DKD is limited to renin-angiotensin system (RAS) inhibitors. Adenosine is detectable in the kidney and is significantly elevated in response to cellular damage. While all 4 known subtypes of adenosine receptors, namely, A1 AR, A2a AR, A2b AR, and A3 AR, are expressed in the kidney, our previous study has demonstrated that a novel, orally active, species-independent, and selective A3 AR antagonist, LJ-1888, ameliorates unilateral ureteral obstruction-induced tubulointerstitial fibrosis...
April 20, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29670529/adenosine-receptor-mediated-cardioprotection-current-limitations-and-future-directions
#13
Robert D Lasley
Since the seminal reports of adenosine receptor-mediated cardioprotection in the early 1990s, there have been a multitude of such reports in various species and preparations. Original observations of the beneficial effects of A1 receptor agonists have been followed up with numerous reports also implicating A2A , A3 , and most recently A2B , receptor agonists as cardioprotective agents. Although adenosine has been approved for clinical use in the United States for the treatment of supraventricular tachycardia and coronary artery imaging, and the selective A2A agonist, regadenoson, for the latter, clinical use of adenosine receptor agonists for protecting the ischemic heart has not advanced beyond early trials...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29649498/the-wakefulness-promoting-drug-modafinil-causes-adenosine-receptor-mediated-upregulation-of-receptor-activator-of-nuclear-factor-%C3%AE%C2%BAb-ligand-in-osteoblasts-negative-impact-of-the-drug-on-peak-bone-accrual-in-rats
#14
Shyamsundar Pal China, Subhashis Pal, Sourav Chattopadhyay, Konica Porwal, Monika Mittal, Sabyasachi Sanyal, Naibedya Chattopadhyay
Modafinil is primarily prescribed for treatment of narcolepsy and other sleep-associated disorders. However, its off-prescription use as a cognition enhancer increased considerably, specially among youths. Given its increasing use in young adults the effect of modafinil on peak bone accrual is an important issue but has never been investigated. Modafinil treatment to young male rats caused trabecular and cortical bone loss in tibia and femur, and reduction in biomechanical strength. Co-treatment of modafinil with alendronate (a drug that suppresses bone resorption) reversed the trabecular bone loss but failed to prevent cortical loss...
April 9, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29626279/activation-of-adenosine-a2b-receptor-attenuates-high-glucose-induced-apoptosis-in-h9c2-cells-via-pi3k-akt-signaling
#15
Yi Shen, Gang Tang, Pan Gao, Bin Zhang, Hang Xiao, Liang-Yi Si
High glucose plays a vital role in apoptosis in H9C2 cells. However, the exact molecular mechanism remains unclear. In this study, we aimed to evaluate the cardio-protective role of A2b receptor in high glucose-induced cardiomyocyte apoptosis via PI3K/Akt pathway. Adenosine A2b receptor agonist (Bay506583), antagonist (MRS1754), and Akt inhibitor (LY294002) were applied respectively to H9C2 cells before exposed to high glucose for 12 h. Apoptosis of H9C2 cells was determined by TUNEL assay and the apoptosis rate by flow cytometry...
April 6, 2018: In Vitro Cellular & Developmental Biology. Animal
https://www.readbyqxmd.com/read/29587249/activation-of-adenylyl-cyclase-causes-stimulation-of-adenosine-receptors
#16
Thomas Pleli, Antonia Mondorf, Nerea Ferreiros, Dominique Thomas, Karel Dvorak, Ricardo M Biondi, Dagmar Meyer Zu Heringdorf, Stefan Zeuzem, Gerd Geisslinger, Herbert Zimmermann, Oliver Waidmann, Albrecht Piiper
BACKGROUND/AIMS: Signaling of Gs protein-coupled receptors (GsPCRs) is accomplished by stimulation of adenylyl cyclase, causing an increase of the intracellular cAMP concentration, activation of the intracellular cAMP effectors protein kinase A (PKA) and Epac, and an efflux of cAMP, the function of which is still unclear. METHODS: Activation of adenylyl cyclase by GsPCR agonists or cholera toxin was monitored by measurement of the intracellular cAMP concentration by ELISA, anti-phospho-PKA substrate motif phosphorylation by immunoblotting, and an Epac-FRET assay in the presence and absence of adenosine receptor antagonists or ecto-nucleotide phosphodiesterase/pyrophosphatase2 (eNPP2) inhibitors...
March 27, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29568380/adenosine-a-2a-receptor-ligand-recognition-and-signaling-is-blocked-by-a-2b-receptors
#17
Sonja Hinz, Gemma Navarro, Dasiel Borroto-Escuela, Benjamin F Seibt, York-Christoph Ammon, Elisabetta de Filippo, Azeem Danish, Svenja K Lacher, Barbora Červinková, Muhammad Rafehi, Kjell Fuxe, Anke C Schiedel, Rafael Franco, Christa E Müller
The adenosine receptor (AR) subtypes A2A and A2B are rhodopsin-like Gs protein-coupled receptors whose expression is highly regulated under pathological, e.g. hypoxic, ischemic and inflammatory conditions. Both receptors play important roles in inflammatory and neurodegenerative diseases, are blocked by caffeine, and have now become major drug targets in immuno-oncology. By Förster resonance energy transfer (FRET), bioluminescence resonance energy transfer (BRET), bimolecular fluorescence complementation (BiFC) and proximity ligation assays (PLA) we demonstrated A2A -A2B AR heteromeric complex formation...
March 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29559698/dual-role-of-creb-in-the-regulation-of-vsmc-proliferation-mode-of-activation-determines-pro-or-anti-mitogenic-function
#18
Claire Hudson, Tomomi E Kimura, Aparna Duggirala, Graciela B Sala-Newby, Andrew C Newby, Mark Bond
Vascular smooth muscle cell (VSMC) proliferation has been implicated in the development of restenosis after angioplasty, vein graft intimal thickening and atherogenesis. We investigated the mechanisms underlying positive and negative regulation of VSMC proliferation by the transcription factor cyclic AMP response element binding protein (CREB). Incubation with the cAMP elevating stimuli, adenosine, prostacyclin mimetics or low levels of forksolin activated CREB without changing CREB phosphorylation on serine-133 but induced nuclear translocation of the CREB co-factors CRTC-2 and CRTC-3...
March 20, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29558203/enzymes-of-the-purinergic-signaling-system-exhibit-diverse-effects-on-the-degeneration-of-valvular-interstitial-cells-in-a-3-d-microenvironment
#19
Andreas Weber, Mareike Barth, Jessica Isabel Selig, Silja Raschke, Konstantinos Dakaras, Alexander Hof, Julia Hesse, Jürgen Schrader, Artur Lichtenberg, Payam Akhyari
Calcific aortic valve disease is an active disease process with lipoprotein deposition, chronic inflammation, and progressive leaflet degeneration. Expression of ectonucleotidases, a group of membrane-bound enzymes that regulate the metabolism of ATP and its metabolites, may coregulate the degeneration process of valvular interstitial cells (VICs). The aim of this study was to investigate the role of the enzymes of the purinergic system in the degeneration process of VICs. Ovine VICs were cultivated in vitro under different prodegenerative conditions and treated with inhibitors of ectonucleoside triphosphate diphosphohydrolase 1 (CD39)/ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), and 5'-nucleotidase (CD73), as well as with adenosine and adenosine receptor agonists...
March 20, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29548686/activation-of-adenosine-a-2a-or-a-2b-receptors-causes-hypothermia-in-mice
#20
Jesse Lea Carlin, Shalini Jain, Romain Duroux, R Rama Suresh, Cuiying Xiao, John A Auchampach, Kenneth A Jacobson, Oksana Gavrilova, Marc L Reitman
Extracellular adenosine is a danger/injury signal that initiates protective physiology, such as hypothermia. Adenosine has been shown to trigger hypothermia via agonism at A1 and A3 adenosine receptors (A1 AR, A3 AR). Here, we find that adenosine continues to elicit hypothermia in mice null for A1 AR and A3 AR and investigated the effect of agonism at A2A AR or A2B AR. The poorly brain penetrant A2A AR agonists CGS-21680 and PSB-0777 caused hypothermia, which was not seen in mice lacking A2A AR. MRS7352, a likely non-brain penetrant A2A AR antagonist, inhibited PSB-0777 hypothermia...
March 13, 2018: Neuropharmacology
keyword
keyword
86182
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"