Gene Symbol: ADORA3
Description: adenosine A3 receptor
Alias: A3AR, adenosine receptor A3
Species: human
Products:     ADORA3

Top Publications

  1. Gao Z, Chen A, Barak D, Kim S, Muller C, Jacobson K. Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human A3 adenosine receptor. J Biol Chem. 2002;277:19056-63 pubmed
    ..Thus, although not important for agonist binding, Trp(243) was critical for receptor activation. The results were interpreted using a rhodopsin-based model of ligand-A(3) receptor interactions. ..
  2. Ochaion A, Bar Yehuda S, Cohen S, Barer F, Patoka R, Amital H, et al. The anti-inflammatory target A(3) adenosine receptor is over-expressed in rheumatoid arthritis, psoriasis and Crohn's disease. Cell Immunol. 2009;258:115-22 pubmed publisher
    ..Taken together, NF-kappaB and CREB are involved with the over-expression of A(3)AR in patients with autoimmune inflammatory diseases. The receptor may be considered as a specific target to combat inflammation. ..
  3. Chen Y, Corriden R, Inoue Y, Yip L, Hashiguchi N, Zinkernagel A, et al. ATP release guides neutrophil chemotaxis via P2Y2 and A3 receptors. Science. 2006;314:1792-5 pubmed
    ..Thus, ATP release and autocrine feedback through P2Y2 and A3 receptors provide signal amplification, controlling gradient sensing and migration of neutrophils. ..
  4. Trincavelli M, Tuscano D, Marroni M, Falleni A, Gremigni V, Ceruti S, et al. A3 adenosine receptors in human astrocytoma cells: agonist-mediated desensitization, internalization, and down-regulation. Mol Pharmacol. 2002;62:1373-84 pubmed
    ..In conclusion, our results demonstrated that A(3) receptors, in astrocytoma cells, are regulated after short- and long-term agonist exposure. ..
  5. Madi L, Cohen S, Ochayin A, Bar Yehuda S, Barer F, Fishman P. Overexpression of A3 adenosine receptor in peripheral blood mononuclear cells in rheumatoid arthritis: involvement of nuclear factor-kappaB in mediating receptor level. J Rheumatol. 2007;34:20-6 pubmed
    A3 adenosine receptor (A3AR) upregulation has been found in cells of synovial tissue and in peripheral blood mononuclear cells (PBMC) of rats with adjuvant-induced arthritis...
  6. Gessi S, Merighi S, Varani K, Cattabriga E, Benini A, Mirandola P, et al. Adenosine receptors in colon carcinoma tissues and colon tumoral cell lines: focus on the A(3) adenosine subtype. J Cell Physiol. 2007;211:826-36 pubmed
    ..In conclusion this study indicates for the first time that in colon cancer cell lines endogenous adenosine, through the interaction with A(3) receptors, mediates a tonic proliferative effect. ..
  7. Varani K, Padovan M, Vincenzi F, Targa M, Trotta F, Govoni M, et al. A2A and A3 adenosine receptor expression in rheumatoid arthritis: upregulation, inverse correlation with disease activity score and suppression of inflammatory cytokine and metalloproteinase release. Arthritis Res Ther. 2011;13:R197 pubmed publisher
    ..The effect of A2A and A3AR agonists in nuclear factor kB (NF-kB) pathway was evaluated...
  8. Sridhar S, Liu H, Pham T, Damera G, Newbold P. Modulation of blood inflammatory markers by benralizumab in patients with eosinophilic airway diseases. Respir Res. 2019;20:14 pubmed publisher
    ..such as CLC, IL-5Rα, and PRSS33; immune-signaling complex genes (FCER1A); G-protein-coupled receptor genes (HRH4, ADORA3, P2RY14); and further immune-related genes (ALOX15 and OLIG2)...
  9. Maximino C, Gemaque J, Benzecry R, Lima M, Batista E, Picanço Diniz D, et al. Role of nitric oxide in the behavioral and neurochemical effects of IB-MECA in zebrafish. Psychopharmacology (Berl). 2015;232:1671-80 pubmed publisher
    ..The purpose of this study was to understand the role of the A3AR on anxiety and arousal models in zebrafish, and whether this role is mediated by the nitrergic modulation of ..

More Information

Publications122 found, 100 shown here

  1. Fang Z, Tosh D, Tanaka N, Wang H, Krausz K, O CONNOR R, et al. Metabolic mapping of A3 adenosine receptor agonist MRS5980. Biochem Pharmacol. 2015;97:215-23 pubmed publisher
    ..1.0]hexane-1-carboxamide (MRS5980) is an A3AR selective agonist containing multiple receptor affinity- and selectivity-enhancing modifications and a therapeutic ..
  2. Zhou Z, Sun C, Tilley S, Mustafa S. Mechanisms underlying uridine adenosine tetraphosphate-induced vascular contraction in mouse aorta: Role of thromboxane and purinergic receptors. Vascul Pharmacol. 2015;73:78-85 pubmed publisher
    ..that Up4A-induced aortic contraction is through COX-derived TXA2 production, which requires activation of A1 and/or A3AR. Concentration responses to Up4A were conducted in isolated aorta...
  3. Azuaje J, Carbajales C, González Gómez M, Coelho A, Caamaño O, Gutiérrez de Terán H, et al. Pyrazin-2(1H)-ones as a novel class of selective A3 adenosine receptor antagonists. Future Med Chem. 2015;7:1373-80 pubmed publisher
    b>A3AR antagonists are promising drug candidates as neuroprotective agents as well as for the treatment of inflammation or glaucoma...
  4. Corriden R, Kilpatrick L, Kellam B, Briddon S, Hill S. Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism. FASEB J. 2014;28:4211-22 pubmed publisher
    In our previous work, using a fluorescent adenosine-A3 receptor (A3AR) agonist and fluorescence correlation spectroscopy (FCS), we demonstrated high-affinity labeling of the active receptor (R*) conformation...
  5. Tosh D, Paoletta S, Chen Z, Moss S, Gao Z, Salvemini D, et al. Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor. Bioorg Med Chem Lett. 2014;24:3302-6 pubmed publisher
    ..Radioligand binding confirmed A3AR selectivity and N(6)-1S,2R stereoselectivity for one diastereomeric pair...
  6. Janes K, Wahlman C, Little J, Doyle T, Tosh D, Jacobson K, et al. Spinal neuroimmune activation is independent of T-cell infiltration and attenuated by A3 adenosine receptor agonists in a model of oxaliplatin-induced peripheral neuropathy. Brain Behav Immun. 2015;44:91-9 pubmed publisher
    ..We recently reported that activation of the Gi/Gq-coupled A3 adenosine receptor (A3AR) with selective A3AR agonists (i.e...
  7. Ranganathan A, Stoddart L, Hill S, Carlsson J. Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models. J Med Chem. 2015;58:9578-90 pubmed publisher
    ..fragments against homology models of the A3 and A1 adenosine receptors (ARs) with the goal to discover A3AR-selective ligands...
  8. Gao Z, Kim S, Gross A, Chen A, Blaustein J, Jacobson K. Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor. Mol Pharmacol. 2003;63:1021-31 pubmed
    ..1-i]purin-5-one (PSB-11) at the WT A(3)ARs, but not the D58N(2.50) mutant receptor. The results were interpreted using a rhodopsin-based molecular model of the A(3)AR to suggest multiple binding modes of the allosteric modulators. ..
  9. Kozma E, Gizewski E, Tosh D, Squarcialupi L, Auchampach J, Jacobson K. Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochem Pharmacol. 2013;85:1171-81 pubmed publisher
    ..They contained a fluorophore linked through the C2 or N(6) position and rigid A3AR-enhancing (N)-methanocarba modification. A hydrophobic C2-(1-pyrenyl) derivative MRS5704 bound nonselectively...
  10. Hofer M, Pospíšil M, Dušek L, Hoferová Z, Komůrková D. Enhanced survival of lethally irradiated adenosine A3 receptor knockout mice. A role for hematopoietic growth factors?. Purinergic Signal. 2015;11:79-85 pubmed publisher
    Adenosine A3 receptor knockout (A3AR KO) mice and their wild-type (WT) counterparts were compared from the point of view of their abilities to survive exposures to lethal doses of γ-radiation belonging to the range of radiation doses ..
  11. Alnouri M, Jepards S, Casari A, Schiedel A, Hinz S, Müller C. Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors. Purinergic Signal. 2015;11:389-407 pubmed publisher
    ..selective agonists include CCPA (for A1AR of rat and mouse), CGS-21680 (for A2A AR of rat), and Cl-IB-MECA (for A3AR of all three species)...
  12. Carlin J, Tosh D, Xiao C, Piñol R, Chen Z, Salvemini D, et al. Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors. J Pharmacol Exp Ther. 2016;356:474-82 pubmed publisher
    ..Here we use the potent, specific A3AR agonists MRS5698, MRS5841, and MRS5980 to show that adenosine also induces hypothermia via the A3AR...
  13. Carlin J, Jain S, Gizewski E, Wan T, Tosh D, Xiao C, et al. Hypothermia in mouse is caused by adenosine A1 and A3 receptor agonists and AMP via three distinct mechanisms. Neuropharmacology. 2017;114:101-113 pubmed publisher
    ..using telemetric monitoring of body temperature in wild type and receptor knock out (Adora1-/-, Adora3-/-) mice...
  14. Eisner C, Kim S, Grill A, Qin Y, Hoerl M, Briggs J, et al. Profound hypothermia after adenosine kinase inhibition in A1AR-deficient mice suggests a receptor-independent effect of intracellular adenosine. Pflugers Arch. 2017;469:339-347 pubmed publisher
    ..To assess the possible role of A2AR and A3AR activation in our experimental setting, we compared the effects of the agonists CPA (A1AR), CGS21680 (A2AR), and IB-..
  15. Ayoub B, Attia Y, Ahmed M. Structural re-positioning, in silico molecular modelling, oxidative degradation, and biological screening of linagliptin as adenosine 3 receptor (ADORA3) modulators targeting hepatocellular carcinoma. J Enzyme Inhib Med Chem. 2018;33:858-866 pubmed publisher
    ..with different clinical activities, containing 3,7-dihydro-1H-purine-2,6-dione, especially adenosine 3 receptors (ADORA3)...
  16. Venkatesan G, Paira P, Cheong S, Federico S, Klotz K, Spalluto G, et al. A facile and novel synthesis of N(2)-, C(6)-substituted pyrazolo[3,4-d]pyrimidine-4 carboxylate derivatives as adenosine receptor antagonists. Eur J Med Chem. 2015;92:784-98 pubmed publisher
    ..Most of the pyrazolo[3,4-d]pyrimidine-4-carboxylates displayed from moderate to good affinity at the human A3AR (hA3AR), as indicated by the low micromolar range of Ki values (Ki hA3AR = 0.7-34 μM)...
  17. Torres A, Vargas Y, Uribe D, Jaramillo C, Gleisner A, Salazar Onfray F, et al. Adenosine A3 receptor elicits chemoresistance mediated by multiple resistance-associated protein-1 in human glioblastoma stem-like cells. Oncotarget. 2016;7:67373-67386 pubmed publisher
    ..adenosine, thus controlling MRP1 transporter expression and activity via activation of the adenosine A3 receptor (A3AR). We showed PI3K/Akt and MEK/ERK1/2 signaling pathways downstream A3AR to control MRP1 in GSCs...
  18. Baram D, Dekel O, Mekori Y, Sagi Eisenberg R. Activation of mast cells by trimeric G protein Gi3; coupling to the A3 adenosine receptor directly and upon T cell contact. J Immunol. 2010;184:3677-88 pubmed publisher
    ..These results unveil the physiological G-protein coupled receptor that couples to Gi3 and establish the important role played by this G-protein in inflammatory conditions that involve adenosine-activated mast cells. ..
  19. Bar Yehuda S, Luger D, Ochaion A, Cohen S, Patokaa R, Zozulya G, et al. Inhibition of experimental auto-immune uveitis by the A3 adenosine receptor agonist CF101. Int J Mol Med. 2011;28:727-31 pubmed publisher
    ..The Gi protein associated A3 adenosine receptor (A3AR) is highly expressed in inflammatory cells whereas low expression is found in normal cells...
  20. Fishman P, Cohen S, Bar Yehuda S. Targeting the A3 adenosine receptor for glaucoma treatment (review). Mol Med Rep. 2013;7:1723-5 pubmed publisher
    ..A3 adenosine receptor (A3AR) agonists have been found to protect normal cells from undergoing apoptosis via the downregulation of death signals...
  21. Feoktistov I, Ryzhov S, Goldstein A, Biaggioni I. Mast cell-mediated stimulation of angiogenesis: cooperative interaction between A2B and A3 adenosine receptors. Circ Res. 2003;92:485-92 pubmed
    ..Thus, adenosine A2B and A3 receptors act in a functional cooperative fashion to promote angiogenesis by a paracrine mechanism involving the differential expression and secretion of angiogenic factors from human mast cells. ..
  22. Nayak A, Chandra G, Hwang I, Kim K, Hou X, Kim H, et al. Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists. J Med Chem. 2014;57:1344-54 pubmed publisher
    ..Hydrophobic N(6) and/or C2 substituents were tolerated in A3AR binding, but only an unsubstituted 6-amino group with a C2-hexynyl group promoted high hA2AAR affinity...
  23. Liñán Rico A, Wunderlich J, Enneking J, Tso D, Grants I, Williams K, et al. Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X₁, P2X₂, P2X₃ channels, P2Y and A₃ metabotropic receptors in neurotransmission. Neuropharmacology. 2015;95:83-99 pubmed publisher
    ..Adenosine inhibits fEPSPs and PSCaTs (IC50 = 25 µM), sensitive to MRS1220-antagonism (A3AR)...
  24. Ren T, Tian T, Feng X, Ye S, Wang H, Wu W, et al. An adenosine A3 receptor agonist inhibits DSS-induced colitis in mice through modulation of the NF-κB signaling pathway. Sci Rep. 2015;5:9047 pubmed publisher
    The role of the adenosine A3 receptor (A3AR) in experimental colitis is controversial...
  25. Fishman P, Cohen S. The A3 adenosine receptor (A3AR): therapeutic target and predictive biological marker in rheumatoid arthritis. Clin Rheumatol. 2016;35:2359-62 pubmed publisher
    The Gi protein-associated A3 adenosine receptor (A3AR) is over-expressed in inflammatory cells, and this high expression is also reflected in the peripheral blood mononuclear cells of patients with autoimmune inflammatory diseases such as ..
  26. Madi L, Ochaion A, Rath Wolfson L, Bar Yehuda S, Erlanger A, Ohana G, et al. The A3 adenosine receptor is highly expressed in tumor versus normal cells: potential target for tumor growth inhibition. Clin Cancer Res. 2004;10:4472-9 pubmed
    ..These findings and our previous data suggest A(3)AR as a potential target for tumor growth inhibition. ..
  27. Janes K, Esposito E, Doyle T, Cuzzocrea S, Tosh D, Jacobson K, et al. A3 adenosine receptor agonist prevents the development of paclitaxel-induced neuropathic pain by modulating spinal glial-restricted redox-dependent signaling pathways. Pain. 2014;155:2560-7 pubmed publisher
    ..We recently reported that activation of the Gi/Gq-coupled A3 adenosine receptor (A3AR) with selective A3AR agonists (ie, IB-MECA) blocked the development of chemotherapy induced-neuropathic pain evoked ..
  28. Cohen S, Barer F, Bar Yehuda S, Ijzerman A, Jacobson K, Fishman P. A₃ adenosine receptor allosteric modulator induces an anti-inflammatory effect: in vivo studies and molecular mechanism of action. Mediators Inflamm. 2014;2014:708746 pubmed publisher
    The A3 adenosine receptor (A3AR) is overexpressed in inflammatory cells and in the peripheral blood mononuclear cells of individuals with inflammatory conditions...
  29. Yoshino S, Cilluffo R, Prasad M, Best P, Atkinson E, Aoki T, et al. Sex-Specific Genetic Variants are Associated With Coronary Endothelial Dysfunction. J Am Heart Assoc. 2016;5:e002544 pubmed publisher
    ..with coronary epicardial endothelial dysfunction were ADORA1, KCNQ1, and DNAJC4 in the whole cohort, LPA, MYBPH, ADORA3, and PON1 in women and KIF6 and NFKB1 in men (P<0.01)...
  30. Beach K, Hung L, Arumugam B, Smith E, Ostrin L. Adenosine receptor distribution in Rhesus monkey ocular tissue. Exp Eye Res. 2018;174:40-50 pubmed publisher
    ..or fixed in 4% paraformaldehyde and processed for immunohistochemistry against ADORA1, ADORA2a, ADORA2b, and ADORA3. RNA was reverse-transcribed, and qPCR was performed using custom primers...
  31. Bouma M, Jeunhomme T, Boyle D, Dentener M, Voitenok N, Van Den Wildenberg F, et al. Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 receptors. J Immunol. 1997;158:5400-8 pubmed
    ..These data indicate that adenosine acts via A2 as well as A3 receptors to inhibit neutrophil degranulation and add to the anti-inflammatory potential of adenosine and adenosine-regulating agents in neutrophil-mediated tissue injury. ..
  32. Merighi S, Mirandola P, Milani D, Varani K, Gessi S, Klotz K, et al. Adenosine receptors as mediators of both cell proliferation and cell death of cultured human melanoma cells. J Invest Dermatol. 2002;119:923-33 pubmed
    ..We demonstrated that adenosine triggers a survival signal via A3 receptor activation and it kills the cell through A2A receptor inducing a signaling pathway that involves protein kinase C and mitogen-activated protein kinases. ..
  33. Paoletta S, Tosh D, Finley A, Gizewski E, Moss S, Gao Z, et al. Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain. J Med Chem. 2013;56:5949-63 pubmed publisher
    ..9 nM) as agonist, while corresponding p-sulfo isomer 6 (MRS5701) displayed mixed A1/A3AR agonism...
  34. Almansa R, Heredia Rodríguez M, Gomez Sanchez E, Andaluz Ojeda D, Iglesias V, Rico L, et al. Transcriptomic correlates of organ failure extent in sepsis. J Infect. 2015;70:445-56 pubmed publisher
    ..cell cycle (HIST1H1C, CKS2, CCNA2, CDK1, CCNB2, CIT, CCNB1, AURKA, RAD51), neutrophil protease activity (ELANE, ADORA3, MPO, MMP8, CTSG), IL-1R and IL-18R response correlated directly with SOFA and mortality...
  35. Jenko B, Lusa L, Tomsic M, Praprotnik S, Dolzan V. Clinical-pharmacogenetic predictive models for MTX discontinuation due to adverse events in rheumatoid arthritis. Pharmacogenomics J. 2017;17:412-418 pubmed publisher
    ..SLC19A1, ABCG2, ADORA3 and TYMS were associated with discontinuation because of AEs in clinical-pharmacogenetic model...
  36. Wu W, He Y, Feng X, Ye S, Wang H, Tan W, et al. MicroRNA-206 is involved in the pathogenesis of ulcerative colitis via regulation of adenosine A3 receptor. Oncotarget. 2017;8:705-721 pubmed publisher
    ..In patients with active-UC, miR-206 and adenosine A3 receptor (A3AR) levels were significantly upregulated and downregulated, respectively, and were inversely correlated...
  37. Aghaei M, Panjehpour M, Karami Tehrani F, Salami S. Molecular mechanisms of A3 adenosine receptor-induced G1 cell cycle arrest and apoptosis in androgen-dependent and independent prostate cancer cell lines: involvement of intrinsic pathway. J Cancer Res Clin Oncol. 2011;137:1511-23 pubmed publisher
    ..Loss of MMP, activation of caspase-3 and down-regulation of Bcl-2 expression indicated mitochondrial signaling pathway that involved in the apoptosis. ..
  38. Baraldi P, Baraldi S, Saponaro G, Aghazadeh Tabrizi M, Romagnoli R, Ruggiero E, et al. One-pot reaction to obtain N,N'-disubstituted guanidines of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold as human A3 adenosine receptor antagonists. J Med Chem. 2015;58:5355-60 pubmed publisher
    In this paper we describe an extension SAR study of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine nucleus as A3AR antagonist...
  39. Nishat S, Khan L, Ansari Z, Basir S. Adenosine A3 Receptor: A promising therapeutic target in cardiovascular disease. Curr Cardiol Rev. 2016;12:18-26 pubmed
    ..Recent studies have shown that A3AR is involved in the amelioration of cardiovascular complications by altering the expression of A3R...
  40. Koszałka P, Gołuńska M, Urban A, Stasiłojć G, Stanisławowski M, Majewski M, et al. Specific Activation of A3, A2A and A1 Adenosine Receptors in CD73-Knockout Mice Affects B16F10 Melanoma Growth, Neovascularization, Angiogenesis and Macrophage Infiltration. PLoS ONE. 2016;11:e0151420 pubmed publisher
    ..However, mainly A3AR activation increased both the microvessel density and expression of pro-angiogenic factors...
  41. Iyer S, Ranjan A, Elias H, Parrales A, Sasaki H, Roy B, et al. Genome-wide RNAi screening identifies TMIGD3 isoform1 as a suppressor of NF-?B and osteosarcoma progression. Nat Commun. 2016;7:13561 pubmed publisher
    ..Adenosine A3 receptor (A3AR) having an identical N-terminal region shows similar biological profiles to TMIGD3 i1...
  42. Nasser M, Masood M, Wei W, Li X, Zhou Y, Liu B, et al. Cordycepin induces apoptosis in SGC?7901 cells through mitochondrial extrinsic phosphorylation of PI3K/Akt by generating ROS. Int J Oncol. 2017;50:911-919 pubmed publisher
    ..apoptosis in SGC?7901 cells with the help of regulating mitochondrial extrinsic pathways by inhibition of A3AR and drive activation of DR3, which promote the activation of PI3K/Akt protein expression as well as collapse of ..
  43. Zhao R, Wang S, Huang Z, Zhang L, Yang X, Bai X, et al. Lipopolysaccharide-induced serotonin transporter up-regulation involves PKG-I and p38MAPK activation partially through A3 adenosine receptor. Biosci Trends. 2015;9:367-76 pubmed publisher
    ..protein kinase type I (PKG-I), p38 mitogen-activated protein kinases (p38MAPK) and A3 adenosine receptor (A3AR) inhibitors, SERT expression was evaluated by western blot and immunofluorescence analysis...
  44. Bulger E, Tower C, Warner K, Garland T, Cuschieri J, Rizoli S, et al. Increased neutrophil adenosine a3 receptor expression is associated with hemorrhagic shock and injury severity in trauma patients. Shock. 2011;36:435-9 pubmed publisher
    ..Hypertonic saline increases A3 expression of PMNs from healthy volunteers and less severely injured patients. ..
  45. Ohana G, Cohen S, Rath Wolfson L, Fishman P. A3 adenosine receptor agonist, CF102, protects against hepatic ischemia/reperfusion injury following partial hepatectomy. Mol Med Rep. 2016;14:4335-4341 pubmed publisher
    ..CF102 is a highly selective A3 adenosine receptor (A3AR) agonist, and has been identified to induce an anti?inflammatory and protective effect on the liver via the ..
  46. Tosh D, Padia J, Salvemini D, Jacobson K. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signal. 2015;11:371-87 pubmed publisher
    ..It is becoming an important pharmacological tool for defining A3AR effects and is orally active in a chronic neuropathic pain model...
  47. Akhtari M, Zargar S, Mahmoudi M, Vojdanian M, Rezaeimanesh A, Jamshidi A. Ankylosing spondylitis monocyte-derived macrophages express increased level of A2A adenosine receptor and decreased level of ectonucleoside triphosphate diphosphohydrolase-1 (CD39), A1 and A2B adenosine receptors. Clin Rheumatol. 2018;37:1589-1595 pubmed publisher
    ..Analysis of adenosine receptors (ADORA1، ADORA2A، ADORA2B، ADORA3), CD39 and CD73 gene expression was performed by SYBR green real-time PCR...
  48. Houlder E, Millier M, Highton J, Gwynne Jones D, Stamp L, Hessian P. Expression of the genes facilitating methotrexate action within subcutaneous rheumatoid nodules. Clin Exp Rheumatol. 2017;35:943-947 pubmed
    ..and mechanism of action (TYMS, MTR, MTRR) of MTX, including for the adenosine receptors ADORA1, ADORA2A, ADORA2B, ADORA3 and ADORA3variant were quantitated by real-time PCR in each nodule sample...
  49. Labazi H, Tilley S, Ledent C, Mustafa S. Role of Adenosine Receptor(s) in the Control of Vascular Tone in the Mouse Pudendal Artery. J Pharmacol Exp Ther. 2016;356:673-80 pubmed publisher
    ..AR activation-mediated vasodilation in the PA is mediated by both the A2AAR and A2BAR, whereas neither the A1AR nor A3AR play a role in vascular tone regulation of the PA...
  50. Tosh D, Ciancetta A, Warnick E, O CONNOR R, Chen Z, Gizewski E, et al. Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists. J Med Chem. 2016;59:3249-63 pubmed publisher
    Purine (N)-methanocarba-5'-N-alkyluronamidoriboside A3 adenosine receptor (A3AR) agonists lacking an exocyclic amine resulted from an unexpected reaction during a Sonogashira coupling and subsequent aminolysis...
  51. Ford A, Castonguay A, Cottet M, Little J, Chen Z, Symons Liguori A, et al. Engagement of the GABA to KCC2 signaling pathway contributes to the analgesic effects of A3AR agonists in neuropathic pain. J Neurosci. 2015;35:6057-67 pubmed publisher
    ..We have since demonstrated that A3AR agonists have potent analgesic actions in preclinical rodent models of neuropathic pain and that A3AR analgesia is ..
  52. Min H, Cha J, Kim K, Kim J, Ghee J, Kim H, et al. Renoprotective Effects of a Highly Selective A3 Adenosine Receptor Antagonist in a Mouse Model of Adriamycin-induced Nephropathy. J Korean Med Sci. 2016;31:1403-12 pubmed publisher
    ..A recent study reported that an A3 adenosine receptor (A3AR) antagonist attenuated the progression of renal fibrosis...
  53. Ciruela F, Albergaria C, Soriano A, Cuffí L, Carbonell L, Sanchez S, et al. Adenosine receptors interacting proteins (ARIPs): Behind the biology of adenosine signaling. Biochim Biophys Acta. 2010;1798:9-20 pubmed publisher
  54. Gorzalczany Y, Akiva E, Klein O, Merimsky O, Sagi Eisenberg R. Mast cells are directly activated by contact with cancer cells by a mechanism involving autocrine formation of adenosine and autocrine/paracrine signaling of the adenosine A3 receptor. Cancer Lett. 2017;397:23-32 pubmed publisher
    ..These findings provide evidence for a novel mode of unidirectional crosstalk between MCs and cancer cells implicating direct activation by cancer cells in MC reprogramming into a pro tumorigenic profile. ..
  55. Yi X, Wang W, Xie Q. Adenosine receptors enhance the ATP-induced odontoblastic differentiation of human dental pulp cells. Biochem Biophys Res Commun. 2018;497:850-856 pubmed publisher
    ..that HDPCs treated with ATP showed higher activity of ADORA1 (A1R), ADORA2B (A2BR), and ADORA3 (A3R)...
  56. Montinaro A, Iannone R, Pinto A, Morello S. Adenosine receptors as potential targets in melanoma. Pharmacol Res. 2013;76:34-40 pubmed publisher
    ..Here, we review the role played by A2aR and A3R in regulating cancer pathogenesis, with a focus on melanoma, and the therapeutic potential of adenosine receptors pharmacological modulation. ..
  57. Hill S, May L, Kellam B, Woolard J. Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization. Br J Pharmacol. 2014;171:1102-13 pubmed publisher
  58. Ren T, Qiu Y, Wu W, Feng X, Ye S, Wang Z, et al. Activation of adenosine A3 receptor alleviates TNF-?-induced inflammation through inhibition of the NF-?B signaling pathway in human colonic epithelial cells. Mediators Inflamm. 2014;2014:818251 pubmed publisher
    To investigate the expression of adenosine A3 receptor (A3AR) in human colonic epithelial cells and the effects of A3AR activation on tumor necrosis factor alpha (TNF-?-) induced inflammation in order to determine its mechanism of action ..
  59. Rudich N, Dekel O, Sagi Eisenberg R. Down-regulation of the A3 adenosine receptor in human mast cells upregulates mediators of angiogenesis and remodeling. Mol Immunol. 2015;65:25-33 pubmed publisher
    ..This study therefore identifies the human mast cell A3R as regulator of tissue remodeling gene expression in human mast cells and demonstrates a heretofore-unrecognized mode of feedback regulation that is exerted by this receptor. ..
  60. Kim S, Kim Y, Park H, Kim S, Kim S, Ye Y, et al. Adenosine deaminase and adenosine receptor polymorphisms in aspirin-intolerant asthma. Respir Med. 2009;103:356-63 pubmed publisher
    ..The genes for adenosine deaminase (ADA) and the four adenosine receptors (ADORA1, ADORA2A, ADORA2B, and ADORA3) were screened by direct sequencing, and 13 single nucleotide polymorphisms (SNPs) were selected among 23 ..
  61. Sun C, Wall N, Angelov N, Ririe C, Chen J, Boskovic D, et al. Changes in mRNA expression of adenosine receptors in human chronic periodontitis. Chin J Dent Res. 2011;14:113-20 pubmed
    ..of periodontitis, this study focused on the adenosine receptor (AR) expression profiles (A1AR, A2AAR, A2BAR and A3AR) in periodontal diseased tissues...
  62. Hinze A, Mayer P, Harst A, von Kugelgen I. Adenosine A(3) receptor-induced proliferation of primary human coronary smooth muscle cells involving the induction of early growth response genes. J Mol Cell Cardiol. 2012;53:639-45 pubmed publisher
    ..The results facilitate the understanding of the role of adenosine A(3) receptors in the cardiovascular system. ..
  63. Butler M, Sanmugalingam D, Burton V, Wilson T, Pearson R, Watson R, et al. Impairment of adenosine A3 receptor activity disrupts neutrophil migratory capacity and impacts innate immune function in vivo. Eur J Immunol. 2012;42:3358-68 pubmed publisher
    ..Our data indicate that A3Rs play a role in neutrophil migration and disrupting this function has the potential to adversely affect innate immune responses. ..
  64. Stoddart L, Kellam B, Briddon S, Hill S. Effect of a toggle switch mutation in TM6 of the human adenosine A? receptor on Gi protein-dependent signalling and Gi-independent receptor internalization. Br J Pharmacol. 2014;171:3827-44 pubmed publisher
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    ..of IFN-γ-regulated genes and IFN-γ levels, as well as upregulated expression of adenosine receptor 3 (ADORA3) and genes related to adenosine metabolism...
  66. Wittliff J, Sereff S, Daniels M. Expression of Genes for Methylxanthine Pathway-Associated Enzymes Accompanied by Sex Steroid Receptor Status Impacts Breast Carcinoma Progression. Horm Cancer. 2017;8:298-313 pubmed publisher
    ..Of PR+ carcinomas, diminished ADORA2B and RYR1 and elevated expressions of ADORA3, PDE4A, CYP2C8, and CYP2E were noted...
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    ..These results suggest that genetic variants in the adenosine receptor genes may predict the heart's response to ischemia or injury and might also influence an individual's response to adenosine therapy. ..
  69. Burnett L, Blais E, Unadkat J, Hille B, Tilley S, Babcock D. Testicular expression of Adora3i2 in Adora3 knockout mice reveals a role of mouse A3Ri2 and human A3Ri3 adenosine receptors in sperm. J Biol Chem. 2010;285:33662-70 pubmed publisher
    ..Expression of the orthologous ADORA3i3 transcript also is most prominent in human testis; presumably producing an A3Ri3 receptor that is functional in sperm and that may be a target for development of male-directed contraceptives. ..
  70. Gessi S, Varani K, Merighi S, Cattabriga E, Avitabile A, Gavioli R, et al. Expression of A3 adenosine receptors in human lymphocytes: up-regulation in T cell activation. Mol Pharmacol. 2004;65:711-9 pubmed
  71. Bar Yehuda S, Stemmer S, Madi L, Castel D, Ochaion A, Cohen S, et al. The A3 adenosine receptor agonist CF102 induces apoptosis of hepatocellular carcinoma via de-regulation of the Wnt and NF-kappaB signal transduction pathways. Int J Oncol. 2008;33:287-95 pubmed
    ..Taken together, A(3)AR is highly expressed in tumors and PBMCs of HCC patients and tumor-bearing rats. CF102 induced apoptosis and tumor growth inhibition. These data suggest A(3)AR as a novel targeted therapy to treat HCC. ..
  72. Mlejnek P, Dolezel P, Kosztyu P. P-glycoprotein mediates resistance to A3 adenosine receptor agonist 2-chloro-N6-(3-iodobenzyl)-adenosine-5'-n-methyluronamide in human leukemia cells. J Cell Physiol. 2012;227:676-85 pubmed publisher
    ..Although both cell lines expressed the A3 adenosine receptor (A3AR), cytotoxic effects of Cl-IB-MECA were not prevented by its selective antagonist MRS1523 (3-propyl-6-ethyl-5-[(..
  73. Panjehpour M, Karami Tehrani F. An adenosine analog (IB-MECA) inhibits anchorage-dependent cell growth of various human breast cancer cell lines. Int J Biochem Cell Biol. 2004;36:1502-9 pubmed
    ..These results suggest that the inhibitory effect of IB-MECA on the growth of human breast cancer cell lines is mediated through activation of A3 adenosine receptor. ..
  74. Wan W, Cui D, Yang X, Hu J, Li C, Hu S, et al. Expression of adenosine receptors in human retinal pigment epithelium cells in vitro. Chin Med J (Engl). 2011;124:1139-44 pubmed
    ..ADORA2B was strongly expressed in the nucleus, perinucleus and the cytoplasm, and ADORA3 was expressed weakly in the cytoplasm of RPE. ADORs are expressed in human RPE...
  75. Kim T, Kim Y, Woo J. The adenosine A3 receptor agonist Cl-IB-MECA induces cell death through Ca²?/ROS-dependent down regulation of ERK and Akt in A172 human glioma cells. Neurochem Res. 2012;37:2667-77 pubmed publisher
    Adenosine A(3) receptor (A3AR) is coupled to G proteins that are involved in a variety of intracellular signaling pathways and physiological functions...
  76. Dal Ben D, Buccioni M, Lambertucci C, Kachler S, Falgner N, Marucci G, et al. Different efficacy of adenosine and NECA derivatives at the human A3 adenosine receptor: insight into the receptor activation switch. Biochem Pharmacol. 2014;87:321-31 pubmed publisher
    ..The results suggest an explanation for the different agonistic behavior of adenosine and NECA derivatives, respectively. A sub-pocket of the binding site was analyzed as a crucial interaction domain for receptor activation. ..
  77. Cao H, Liu Z, Chang Z. Cordycepin induces apoptosis in human bladder cancer cells via activation of A3 adenosine receptors. Tumour Biol. 2017;39:1010428317706915 pubmed publisher
    ..Together, these data suggest that Cordyceps militaris hot water extracts containing cordycepin may be a promising treatment for bladder cancer via A3 adenosine receptor activation. ..
  78. Liang B, Jacobson K. A physiological role of the adenosine A3 receptor: sustained cardioprotection. Proc Natl Acad Sci U S A. 1998;95:6995-9 pubmed
    ..The study indicates that cardiac adenosine A3 receptor mediates a sustained cardioprotective function and represents a new cardiac therapeutic target. ..
  79. Gessi S, Cattabriga E, Avitabile A, Gafa R, Lanza G, Cavazzini L, et al. Elevated expression of A3 adenosine receptors in human colorectal cancer is reflected in peripheral blood cells. Clin Cancer Res. 2004;10:5895-901 pubmed
    ..This study provides the first evidence that A(3) receptor plays a role in colon tumorigenesis and, more importantly, can potentially be used as a diagnostic marker or a therapeutic target for colon cancer. ..
  80. Merighi S, Simioni C, Gessi S, Varani K, Mirandola P, Tabrizi M, et al. A(2B) and A(3) adenosine receptors modulate vascular endothelial growth factor and interleukin-8 expression in human melanoma cells treated with etoposide and doxorubicin. Neoplasia. 2009;11:1064-73 pubmed
    ..Consequently, we conclude that adenosine receptor modulation may be useful for refining the use of chemotherapeutic drugs to treat human cancer more effectively. ..
  81. Jafari S, Panjehpour M, Aghaei M, Joshaghani H, Enderami S. A3 Adenosine Receptor Agonist Inhibited Survival of Breast Cancer Stem Cells via GLI-1 and ERK1/2 Pathway. J Cell Biochem. 2017;118:2909-2920 pubmed publisher
    Numerous studies have demonstrated the role of A3 adenosine receptor (A3AR) and signaling pathways in the multiple aspects of the tumor...
  82. Monitto C, Levitt R, DiSilvestre D, Holroyd K. Localization of the A3 adenosine receptor gene (ADORA3) to human chromosome 1p. Genomics. 1995;26:637-8 pubmed
  83. Salvatore C, Jacobson M, Taylor H, Linden J, Johnson R. Molecular cloning and characterization of the human A3 adenosine receptor. Proc Natl Acad Sci U S A. 1993;90:10365-9 pubmed
    ..This raises the possibility that numerous physiological effects of adenosine may be mediated by A3 adenosine receptors. ..
  84. Atkinson M, Townsend Nicholson A, Nicholl J, Sutherland G, Schofield P. Cloning, characterisation and chromosomal assignment of the human adenosine A3 receptor (ADORA3) gene. Neurosci Res. 1997;29:73-9 pubmed
    The gene for the inhibitory G-protein coupled human A3 adenosine receptor (ADORA3) was isolated and sequence analysis shows that the coding region is interrupted by a single intron of size 2.4 kb...
  85. Madi L, Rosenberg Haggen B, Nyska A, Korenstein R. Enhancing pigmentation via activation of A3 adenosine receptors in B16 melanoma cells and in human skin explants. Exp Dermatol. 2013;22:74-7 pubmed publisher
    A3 adenosine receptor, A3AR, belongs to the Gi proteins coupled receptors. Activation of A3AR by its agonist, IB-MECA, decreases cAMP and was expected to reduce melanin level...
  86. Sajjadi F, Firestein G. cDNA cloning and sequence analysis of the human A3 adenosine receptor. Biochim Biophys Acta. 1993;1179:105-7 pubmed
    We report the cloning of the cDNA encoding the homolog of the A3 adenosine receptor (A3AR) from a human heart library. The receptor shares a surprisingly low degree of sequence homology to the rat A3AR...
  87. Fernandez P, Jara C, Aguilera V, Caviedes L, Diaz F, Radojkovic C, et al. Adenosine A?A and A? receptors are involved in the human endothelial progenitor cells migration. J Cardiovasc Pharmacol. 2012;59:397-404 pubmed publisher
    ..2 ± 0.01 nM). In conclusion, adenosine stimulates hEPC migration by activating A?A and A? but not A?B receptors and provides evidence to support a role of adenosine in modulating angiogenic capacity of hEPC. ..
  88. Klotz K. Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch Pharmacol. 2000;362:382-91 pubmed
    ..As a result, compounds that exhibit high affinity to only one subtype are an exception. Although the selection of ligands is immense, it is less than satisfying for most subtypes of adenosine receptors...
  89. Broussas M, Cornillet Lefebvre P, Potron G, Nguyen P. Adenosine inhibits tissue factor expression by LPS-stimulated human monocytes: involvement of the A3 adenosine receptor. Thromb Haemost. 2002;88:123-30 pubmed
    ..This was supported by the fact that A2 and A3 antagonists reversed the action of 2-Cado. We conclude that TF inhibition by ADO on human purified monocytes involved A3 receptors. ..
  90. Merighi S, Benini A, Mirandola P, Gessi S, Varani K, Leung E, et al. A3 adenosine receptors modulate hypoxia-inducible factor-1alpha expression in human A375 melanoma cells. Neoplasia. 2005;7:894-903 pubmed
    ..Collectively, these results suggest a cooperation between hypoxic and adenosine signals that ultimately may lead to the increase in HIF-1-mediated effects in cancer cells. ..
  91. Peculis R, Latkovskis G, Tarasova L, Pirags V, Erglis A, Klovins J. A nonsynonymous variant I248L of the adenosine A3 receptor is associated with coronary heart disease in a Latvian population. DNA Cell Biol. 2011;30:907-11 pubmed publisher
    Adenosine plays an important part in the cardiac response to ischemia and reperfusion. The human adenosine receptor A3 (A3R), along with other adenosine receptors, is involved in mediation of those effects...
  92. May L, Bridge L, Stoddart L, Briddon S, Hill S. Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics. FASEB J. 2011;25:3465-76 pubmed publisher
    ..0 ± 0.1, 5.9 ± 0.1, and 5.2 ± 0.1, respectively. This study provides new insight into the spatial and temporal specificity of drug action that can be provided by allosteric modulation across a GPCR homodimeric interface. ..