Recombinant Human Adenosine receptor A2a (ADORA2A), partial

1. the A2AR-D2R heterotetramer-AC5 complex sustains the canonical antagonistic Gs-Gi interaction at the adenylyl cyclase level PMID: 29593213
2. Here, ligand-binding kinetics of the full-length human adenosine A2A receptor (A2AR) reconstituted in detergent micelles were measured using a fluorescently labeled ligand via fluorescence anisotropy. PMID: 27577981
3. alpha2A- and alpha2C-adrenoceptors are functional receptors for norepinephrine, dopamine, and other previously assumed selective D2-like receptor ligands. PMID: 29552726
4. Mechanistic insights into allosteric regulation of the A2A adenosine G protein-coupled receptor by physiological cations have been described. PMID: 29636462
5. expression A2AR mRNA in PBMCs was associated with asthma severity. Foxp3 mRNA, TGF-beta, and FEV1%pred positively correlated with A2AR mRNA in asthma. PMID: 27216911
6. This study reported associations between the c.1083T>C polymorphism in the adenosine A2A receptor gene (ADORA2A) and sleep variables PMID: 28215251
7. Enhancement of inosine-mediated A2AR signaling through positive allosteric modulation has been reported. PMID: 29126977
8. These data indicate that low [Na(+)] is required to allow large agonist-induced structural changes in A2AR, and that patterns of sidechain dynamics substantially differ between agonist (NECA) and inverse agonist (ZM241385) bound receptors, with the inverse agonist suppressing fast picosecond-nanosecond timescale motions at the G protein binding site. PMID: 28984574
9. Low adenosine A2a receptor expression is associated with ulcerative colitis. PMID: 27476546
10. Results demonstrate that A2AR act on GR nuclear translocation and GR-dependent transcriptional regulation which suggest that A2AR is a major regulator of GR function and that this functional interconnection may be a trigger to age-related memory deficits. PMID: 27510168
11. the present study indicates that A2bR may play a potential oncogenic role in BUC progression and act as a potential biomarker to identify BUC patients with poor clinical outcomes. PMID: 28548944
12. Report prognostic impact of ADORA2A expression in non-small lung cancers. PMID: 28060732
13. genetic association studies in population in Germany: Data suggest that an SNP in ADORA2A (1976T/C, rs5751876) is associated with interoceptive (resting) and exteroceptive (executive function/task-based) processing in frontal lobe and insular cortex neural networks. Facilitated processing of interoceptive/exteroceptive information in salience network is suggested to promote development of anxiety and anxiety disorders. PMID: 27262510
14. A2A receptor stimulation promotes collagen type III synthesis via the activation of canonical and non-canonical beta-catenin, consistent with a role for A2A receptors in dermal fibrosis and scarring. PMID: 27595240
15. It is significantly associated with hippocampal volume and the minor allele of rs9608282 in ADORA2A is associated with larger hippocampal volumes and better memory. PMID: 28941407
16. Study corroborated results from a previous report that described interactions between ADORA2A and CYP1A2 polymorphisms and coffee consumption in Parkinson's disease. PMID: 28135712
17. However, the contribution of the A2AR to the control of impulsive reward seeking remains unknown. Using mice that were exposed to differential reward of low rate (DRL) schedules during Pavlovian-conditioning, second-order schedule discrimination, and the 5-choice serial reaction time task (5-CSRTT), we demonstrate that deficits of A2AR function promote impulsive responses. PMID: 28418405
18. Western blot analysis indicates that the A2A receptor is more abundant in the hippocampus of medial temporal lobe epilepsy patients compared to control individuals. Immunoreactivity against the A2A receptor predominates in astrocytes staining positively for the glial fibrillary acidic protein. PMID: 27650530
19. Results suggest that the combination of the ADORA2A rs2298383TT and MTHFR 1298AC-677CT genotypes might lead to a low risk of nodule formation in patients treated with methotrexate. PMID: 27846189
20. Hypoxic postconditioning protects against apoptosis induced by reoxygenation via activation of adenosine A2a receptors on dermal microvascular endothelial cells. PMID: 28606618
21. results unveil intracellular signaling pathways targeted by the A2AR, some of which might be key in modulating neutrophil functions. PMID: 28179537
22. A2A AR activation on BBB endothelial cells offers a therapeutic window that can be fine-tuned for drug delivery to the brain and has potential as a CNS drug-delivery technology. PMID: 27043281
23. Hypoxic postconditioning attenuates apoptosis via inactivation of adenosine A2a receptor through NDRG3-Raf-ERK pathway. PMID: 28743501
24. ADORA2A rs2298383 and high cumulative dose of systemic methotrexate (MTX) administration were significantly associated with MTX-related leukoencephalopathy PMID: 27399166
25. lipid 1,2-dihexanoyl-sn-glycero-3-phosphocholine (DHPC, di-6:0PC). After solubilization in DDM, DDM/CHAPS, or DHPC micelles, although A2AR was found to retain its native-like fold, its binding ability was significantly compromised compared to DDM or DDM/CHAPS with CHS. It therefore appears that although cholesterol is not needed for A2AR to retain a native-like, alpha-helical conformation PMID: 27241126
26. We report an investigation designed to explore alternative approaches for ranking of docking poses in the search for antagonists of the adenosine A2A receptor, an attractive target for structure-based virtual screening PMID: 27334985
27. A higher regeneration rate in the CF102 treatment group was observed compared with the control group, suggesting that CF102 had a positive effect on the proliferation of hepatocytes following hepatectomy. CF102 had a protective effect on the liver of Wistar rats subsequent to IR injury during hepatectomy. This may be due to an antiinflammatory and antiapoptotic effect mediated by the A3AR. PMID: 27666664
28. Adenosine A(2A) receptor 1083 T > C polymorphism is not associated with the positivity of head-up tilt test and its proposed role in predisposition to Vasovagal Syncope was not confirmed PMID: 26710963
29. Low level of ADORA1/ADORA2A expression increased susceptibility of brain tumor-associated epilepsy. PMID: 27038930
30. No association was found between the ADORA2A rs2298383 polymorphism and panic disorder. The ADORA2A TT homozygous wild-type genotype and the ACCN2 TT/ADORA2A CT diplotype were more represented in controls. PMID: 26589317
31. gene expression of A2AR in PBMCs was significantly lower in idiopathic normal-pressure hydrocephalus patients than controls PMID: 26810542
32. crystal structure of the adenosine A(2A) receptor bound to an engineered G protein at 3.4 A resolution PMID: 27462812
33. 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 PMID: 26539478
34. 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. PMID: 26873858
35. activation of the A2AR reduced oxidative stress-induced DNA damage and caspase 3 activation in GABAergic neurons PMID: 26264576
36. Functional polymorphisms of the genes encoding adenosine A2A receptors and dopamine transporters contribute to individual differences in impaired sleep quality by caffeine. PMID: 27167478
37. 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 PMID: 27239843
38. (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 PMID: 27144352
39. ST1535 metabolites ST3932 and ST4206 are effective adenosine A2A receptor antagonists which maybe useful in treating Parkinson disease. PMID: 25936513
40. activation of A2A adenosine receptor (AR) with an FDA-approved agonist potently permeabilizes an in vitro primary human blood-brain barrier (hBBB) to the passage of chemotherapeutic drugs and T cells. PMID: 25262373
41. ADORA2A and GRK5 gene variants may influence the etiology of malaria infection. PMID: 26066465
42. placental expression highest at no more than 10 weeks gestational age PMID: 25745823
43. a comparative molecular dynamics (MD) study of the human adenosine receptor type 2A (hA(2A)R) in complex with caffeine, is reported. PMID: 25992797
44. these data suggest a possible role for CD73 and A2A in inflammation observed in patients with T2D and obesity mediated via apoptosis. PMID: 25770019
45. Genetic study showed association of single nucleotide polymorphisms in alpha2A-AR gene locus with bone remodelling markers, identifying the individuals with higher risk of development of osteoporosis. PMID: 25818344
46. This study found a relation between polymorphisms of adenosine A2A and the caffeine effects on the attentional domains of Orienting and Executive control. PMID: 25819143
47. Expression of NPP1 and 5'-nucleotidase by valve interstitial cells promotes the mineralization of the aortic valve through A2aR and a cAMP/PKA/CREB pathway. PMID: 25644539
48. An association was observed for SNPs in ADORA2A and levodopa-induced dyskinesia in Parkinson's disease patients. PMID: 25872644
49. the A2AR-SMALP, generated from yeast (Pichia pastoris) or mammalian cells, exhibited increased thermostability (~5 degrees C) compared with detergent [DDM (n-dodecyl-beta-D-maltopyranoside)]-solubilized A2AR controls. PMID: 25720391
50. findings provide new insights into the anti-inflammatory mechanisms of A2AAR signaling and the potential utility of A2AAR agonists in inflammatory diseases. PMID: 26355151

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HGNC: 263

OMIM: 102776

KEGG: hsa:135

STRING: 9606.ENSP00000336630

UniGene: Hs.197029