Property Summary

NCBI Gene PubMed Count 85
Grant Count 68
R01 Count 42
Funding $7,832,088.92
PubMed Score 248.22
PubTator Score 270.99

Knowledge Summary

Patent

No data available

TINX Plot

Synonym

Accession P0DMS8 A2A3P4 P33765 Q6UWU0 Q9BYZ1
Symbols A3AR

Gene

PDB

1OEA   1R7N  

  TechDev Info (1)

MLP Assay (12)

AID Type Active / Inconclusive / Inactive Description
624355 other 0 / 0 / 0 Late stage results from the probe development efforts to identify dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and nuclear factor NF-kappa-B (NF-kB): Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
624406 other 0 / 0 / 0 Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs
686924 other 0 / 0 / 1 ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound)
686925 other 0 / 0 / 1 ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound)
686926 other 0 / 0 / 1 ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound)
686927 other 0 / 0 / 1 ML353 Eurofin Panel Assay for mGlu5 SAM Inhibitor (Probe Compound)
743249 screening 1 / 0 / 0 Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM)
743250 screening 1 / 0 / 0 Discovery and characterization of a small molecule allosteric agonists of mas-related G-Protein coupled receptor X1 ( MrgX1)
743251 screening 1 / 0 / 0 Development of a novel orthosteric Muscarinic 5 (M5) antagonist possessing a hig degree of muscarinic subtype selectivity
743252 screening 1 / 0 / 0 Development of the first CNS penetrant Muscarinic 5 (M5) Positive Allosteric Modulator based on a novel non-isatin core
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Gene RIF (58)

PMID Text
26194548 Differential regulation in patients with LTP-induced anaphylaxis and those with NSAID-LTP-induced anaphylaxis of the IFN-gamma pathway, IgG receptors, and ADORA3 might provide the pathogenic basis of their distinct responses
25597247 This study identifies 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.
24750014 Effect of a toggle switch mutation in TM6 of the human adenosine A receptor on Gi protein-dependent signalling and Gi-independent receptor internalization
24161786 Different agonistic behavior at adenosine A3 receptor is linked to a sub-pocket of the binding site.
23856527 This is a review of the role played by A2aR and A3AR in regulating cancer pathogenesis, with a focus on melanoma, and the therapeutic potential of adenosine receptors pharmacological modulation. [review]
23817552 Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes.
23383108 A synthetic peptide corresponding to the immunosuppressive domain (amino acids 574-592) of HIV-1 gp41 downregulates the expression of adenosine A3 receptor (ADORA3) in peptide-treated PBMCs
23027555 A3Rs play a role in neutrophil migration and disrupting this function has the potential to adversely affect innate immune responses.
22906537 Activation of smooth muscle adenosine A(3) receptors increase proliferation of human coronary smooth cells.
22682496 There is differential expression of receptors in rheumatoid synovial tissue such that ADORA3 is expressed at significantly higher levels
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AA Sequence

MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYFIVSLALADIAVGVLVMPLAI      1 - 70
VVSLGITIHFYSCLFMTCLLLIFTHASIMSLLAIAVDRYLRVKLTVRYKRVTTHRRIWLALGLCWLVSFL     71 - 140
VGLTPMFGWNMKLTSEYHRNVTFLSCQFVSVMRMDYMVYFSFLTWIFIPLVVMCAIYLDIFYIIRNKLSL    141 - 210
NLSNSKETGAFYGREFKTAKSLFLVLFLFALSWLPLSIINCIIYFNGEVPQLVLYMGILLSHANSMMNPI    211 - 280
VYAYKIKKFKETYLLILKACVVCHPSDSLDTSIEKNSE                                    281 - 318
//

Text Mined References (86)

PMID Year Title
26194548 2016 Distinct transcriptome profiles differentiate nonsteroidal anti-inflammatory drug-dependent from nonsteroidal anti-inflammatory drug-independent food-induced anaphylaxis.
25597247 2015 Down-regulation of the A3 adenosine receptor in human mast cells upregulates mediators of angiogenesis and remodeling.
24864134 2014 Activation of adenosine A3 receptor alleviates TNF-?-induced inflammation through inhibition of the NF-?B signaling pathway in human colonic epithelial cells.
24750014 2014 Effect of a toggle switch mutation in TM6 of the human adenosine A? receptor on Gi protein-dependent signalling and Gi-independent receptor internalization.
24161786 2014 Different efficacy of adenosine and NECA derivatives at the human A3 adenosine receptor: insight into the receptor activation switch.
24114647 2014 G protein-coupled receptors and adipogenesis: a focus on adenosine receptors.
24024783 2014 Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization.
23953133 2013 Rare coding variants of the adenosine A3 receptor are increased in autism: on the trail of the serotonin transporter regulome.
23856527 2013 Adenosine receptors as potential targets in melanoma.
23817552 2013 Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes.
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