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Adenosine A3 receptor

adenosine A3 receptor, A3AR, ADORA3, A3R
This gene encodes a protein that belongs to the family of adenosine receptors, which are G-protein-coupled receptors that are involved in a variety of intracellular signaling pathways and physiological functions. The receptor encoded by this gene mediates a sustained cardioprotective function during cardiac ischemia, it is involved in the inhibition of neutrophil degranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death. Multiple transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Jul 2008] (from NCBI)
Top mentioned proteins: A2A, V1a, CAN, A2B, HAD
Papers on adenosine A3 receptor
Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors.
New
Reitman et al., Saint Louis, United States. In J Pharmacol Exp Ther, Feb 2016
Here we use the potent, specific A3AR agonists MRS5698, MRS5841, and MRS5980 to show that adenosine also induces hypothermia via the A3AR.
Discovery of Novel Adenosine Receptor Agonists that Exhibit Subtype Selectivity.
New
Ladds et al., In J Med Chem, Feb 2016
Some selected compounds were also tested on A1R and A3R in mammalian cells revealing that four of them are entirely A1R-selective agonists.
Adenosine A3 Receptor: A promising therapeutic target in cardiovascular disease.
Review
New
Basir et al., New Delhi, India. In Curr Cardiol Rev, Feb 2016
Adenosine A3 receptor is one of the important receptor which is extensively studied as a therapeutic target in cardiovascular disorder.
Role of adenosine receptor(s) in the control of vascular tone in the mouse pudendal artery.
New
Mustafa et al., Brussels, Belgium. In J Pharmacol Exp Ther, Jan 2016
Using pharmacologic and genetic approaches, our data suggest that AR activation-mediated vasodilation in the PA is mediated by both the A2AAR and A2BAR, while neither the A1AR nor A3AR play a role in vascular tone regulation of the PA.
Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.
New
Carlsson et al., Stockholm, Sweden. In J Med Chem, Jan 2016
To investigate these questions, we used molecular docking to screen >500 000 fragments against homology models of the A3 and A1 adenosine receptors (ARs) with the goal to discover A3AR-selective ligands.
Medicinal chemistry of adenosine, P2Y and P2X receptors.
Review
New
Müller et al., Bethesda, United States. In Neuropharmacology, Jan 2016
Some of these compounds, including A1 and A3 AR agonists, P2Y1R and P2Y12R antagonists, and P2X3, P2X4 and P2X7 antagonists, are potentially of clinical use in treatment of disorders of the nervous system, such as chronic pain, neurodegeneration and brain injury.
Lipopolysaccharide-induced serotonin transporter up-regulation involves PKG-I and p38MAPK activation partially through A3 adenosine receptor.
New
Du et al., Beijing, China. In Biosci Trends, Dec 2015
Using specific cyclic GMP-dependent 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.
Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands.
Review
New
Jacobson et al., l'Hospitalet de Llobregat, Spain. In Neuropharmacology, Nov 2015
Fluorescent ligands for A1R, A2AR, and A3R (adenosine receptors) and P2Y2R, P2Y4R, P2Y6R, and P2Y14R (nucleotide receptors) have been reported.
In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib.
New
Braddock et al., Macclesfield, United Kingdom. In Pharmacol Res Perspect, Oct 2015
R406 was selective outside the kinase domain, with only antagonist activity at the adenosine A3 receptor in the range relevant to clinical effects.
Anticancer and antimetastatic effects of cordycepin, an active component of Cordyceps sinensis.
Review
Yoshikawa et al., Nishinomiya, Japan. In J Pharmacol Sci, 2015
Based on in vitro studies, we report that WECS showed an anticancer action, and this action was antagonized by an adenosine A3 receptor antagonist.
Effects of a Particular Heptapeptide on the IFN-α-Sensitive CML Cells.
Zhang et al., Changsha, China. In Biomed Res Int, 2014
IFN-α-sensitive KT-1/A3 and IFN-α-resistant KT-1/A3R CML cells were transfected by pEGFP-KLWVIPQ expression vector and/or induced by IFN-α.
John Daly Lecture: Structure-guided Drug Design for Adenosine and P2Y Receptors.
Review
Tosh et al., Bethesda, United States. In Comput Struct Biotechnol J, 2014
A3AR agonists for neuropathic pain).
Stop and Go - Waves of Tarsier Dispersal Mirror the Genesis of Sulawesi Island.
Zischler et al., Mainz, Germany. In Plos One, 2014
To resolve the phylogeographic history of Sulawesi tarsiers we analyzed an island-wide sample for a set of five approved autosomal phylogenetic markers (ABCA1, ADORA3, AXIN1, RAG1, and TTR) and the paternally inherited SRY gene.
Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R.
Ragozzino et al., Roma, Italy. In Front Cell Neurosci, 2014
Specifically, the stimulation of both A1R and A3R reduces AMPA currents, while A2AR has an opposite potentiating effect.
Adenosine A₂A and A₃ receptors are involved in the human endothelial progenitor cells migration.
GeneRIF
Aguayo et al., Concepción, Chile. In J Cardiovasc Pharmacol, 2012
adenosine stimulates human endothelial progenitor cells migration by activating AA and A receptors and provides evidence to support a role of adenosine in modulating angiogenic capacity of hEPC
CXCL16 orchestrates adenosine A3 receptor and MCP-1/CCL2 activity to protect neurons from excitotoxic cell death in the CNS.
GeneRIF
Trettel et al., Roma, Italy. In J Neurosci, 2012
Inactivation of the ADORA3 receptor prevents the CXCL16 effect of neuroprotection against excitotoxic damage.
Increased neutrophil adenosine a3 receptor expression is associated with hemorrhagic shock and injury severity in trauma patients.
GeneRIF
Junger et al., Seattle, United States. In Shock, 2011
A3 receptor expression on the surface of PMNs is upregulated by injury, and increased expression levels are associated with greater injury severity and hypovolemic shock.
Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics.
GeneRIF
Hill et al., Nottingham, United Kingdom. In Faseb J, 2011
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.
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.
GeneRIF
Salami et al., Tehrān, Iran. In J Cancer Res Clin Oncol, 2011
control of prostate cancer cell growth through A3 adenosine receptor activation.
Adenosine receptor subtypes: characterization and therapeutic regulation.
Review
Impact
Stiles et al., Durham, United States. In Annu Rev Pharmacol Toxicol, 1994
Currently, four AR subtypes have been cloned: A1AR, A2aAR, A2bAR, and A3AR.
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