| Tclin | Adenosine receptor A2a |
This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily, which is subdivided into classes and subtypes. The receptors are seven-pass transmembrane proteins that respond to extracellular cues and activate intracellular signal transduction pathways. This protein, an adenosine receptor of A2A subtype, uses adenosine as the preferred endogenous agonist and preferentially interacts with the G(s) and G(olf) family of G proteins to increase intracellular cAMP levels. It plays an important role in many biological functions, such as cardiac rhythm and circulation, cerebral and renal blood flow, immune function, pain regulation, and sleep. It has been implicated in pathophysiological conditions such as inflammatory diseases and neurodegenerative disorders. Alternative splicing results in multiple transcript variants. A read-through transcript composed of the upstream SPECC1L (sperm antigen with calponin homology and coiled-coil domains 1-like) and ADORA2A (adenosine A2a receptor) gene sequence has been identified, but it is thought to be non-coding. [provided by RefSeq, Jun 2013]
Comments
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 |
theophylline
pKi 9.22
caffeine
pKi 5.61
regadenoson
pEC50 5.89
adenosine
pEC50 6.15
choline theophyllinate
pKi 9.22
bufylline
pKi 9.22
istradefylline
pKi 8.66
CHEMBL3125711
pKi 7.00
CHEMBL349716
pKi 7.00
CHEMBL456125
pKi 7.00
CHEMBL199898
pKi 7.00
CHEMBL165560
pKi 7.00
CHEMBL1170135
pKi 7.00
CHEMBL488152
pKi 7.00
CHEMBL1950659
pKi 7.00
CHEMBL331372
pKd 7.00
CHEMBL3133067
pKi 7.00
CHEMBL589251
pKi 7.00
CHEMBL3754353
pKi 7.00
CHEMBL139182
pKi 7.00
CHEMBL166424
pKi 7.00
CHEMBL520031
pKi 7.00
CHEMBL167343
pKi 7.00
CHEMBL194696
pKi 7.00
CHEMBL3797433
pKi 7.00
CHEMBL118923
pKi 7.00
CHEMBL355761
pKi 7.00
| 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 |
| More... |
| 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 |
| More... |
MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAIPFAITISTGF 1 - 70 CAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTRAKGIIAICWVLSFAIGLTPM 71 - 140 LGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYFNFFACVLVPLLLMLGVYLRIFLAARRQLKQ 141 - 210 MESQPLPGERARSTLQKEVHAAKSLAIIVGLFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTN 211 - 280 SVVNPFIYAYRIREFRQTFRKIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGS 281 - 350 APHPERRPNGYALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS 351 - 412 //
| 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. |
| More... |
