Property Summary

NCBI Gene PubMed Count 286
Grant Count 390
R01 Count 230
Funding $77,126,245.12
PubMed Score 923.31
PubTator Score 555.51

Knowledge Summary

Patent (11,545)

Expression

Synonym

Accession P29274 B2R7E0
Symbols A2aR
RDC8
ADORA2

Gene

PANTHER Protein Class (2)

PDB

5G53   1MMH   1UPE   2YDO   2YDV   3EML   3PWH   3QAK   3REY   3RFM   3UZA   3UZC   3VG9   3VGA   4EIY   4UG2   4UHR   5IU4   5IU7   5IU8   5IUA   5IUB   5K2A   5K2B  

  TechDev Info (1)

MLP Assay (12)

AID Type Active / Inconclusive / Inactive Description
1788 other 0 / 0 / 0 Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity
1921 other 2 / 0 / 0 Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity
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 (243)

PMID Text
27462812 crystal structure of the adenosine A(2A) receptor bound to an engineered G protein at 3.4 A resolution
27239843 This review examines the molecular mechanisms of inflammatory response in sepsis and the structure and functions of A(2A)AR and its role in the pathogenesis of sepsis
27167478 Functional polymorphisms of the genes encoding adenosine A2A receptors and dopamine transporters contribute to individual differences in impaired sleep quality by caffeine.
27144352 (19)F nuclear magnetic resonance is used to quantify the conformational landscape occupied by the adenosine A2A receptor (A2AR), a prototypical class A G-protein-coupled receptor
26873858 Data suggest that A2aR binding of antagonist (here, ZM241385) exhibits multistep drug-dissociation process, with antagonist consecutively interacting with topographically distinct regions/binding sites of A2aR.
26810542 gene expression of A2AR in PBMCs was significantly lower in idiopathic normal-pressure hydrocephalus patients than controls
26539478 This review will provide insight into the phenotypic changes that underline the resistance to death of liver cells preconditioned by pharmacological activation of A2aR and their implications to develop innovative strategies against liver IR damage
26355151 findings provide new insights into the anti-inflammatory mechanisms of A2AAR signaling and the potential utility of A2AAR agonists in inflammatory diseases.
26317759 Results show that ADORA1 rs2228079 and ADORA2A rs5751876 polymorphisms are associated with the risk of Gilles de la Tourette Syndrome, co-morbid disorders, and may affect the age of tics onset in Polish population.
26264576 activation of the A2AR reduced oxidative stress-induced DNA damage and caspase 3 activation in GABAergic neurons
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AA Sequence

MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAIPFAITISTGF      1 - 70
CAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTRAKGIIAICWVLSFAIGLTPM     71 - 140
LGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYFNFFACVLVPLLLMLGVYLRIFLAARRQLKQ    141 - 210
MESQPLPGERARSTLQKEVHAAKSLAIIVGLFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTN    211 - 280
SVVNPFIYAYRIREFRQTFRKIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGS    281 - 350
APHPERRPNGYALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS            351 - 412
//

Text Mined References (287)

PMID Year Title
27462812 2016 Structure of the adenosine A(2A) receptor bound to an engineered G protein.
27239843 [Adenosine A2A receptor as a drug target for treatment of sepsis].
27167478 2016 [Self-rated Caffeine Sensitivity: Implications for Personalized Sleep Medicine?].
27144352 2016 Activation of the A2A adenosine G-protein-coupled receptor by conformational selection.
26873858 2016 Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor.
26810542 2016 Down-regulation of adenosine A1 and A2A receptors in peripheral cells from idiopathic normal-pressure hydrocephalus patients.
26539478 2015 Pharmacological Preconditioning by Adenosine A2a Receptor Stimulation: Features of the Protected Liver Cell Phenotype.
26355151 2015 Multi-Inhibitory Effects of A2A Adenosine Receptor Signaling on Neutrophil Adhesion Under Flow.
26317759 2015 Association of ADORA1 rs2228079 and ADORA2A rs5751876 Polymorphisms with Gilles de la Tourette Syndrome in the Polish Population.
26264576 2015 Elucidating the role of the A2A adenosine receptor in neurodegeneration using neurons derived from Huntington's disease iPSCs.
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