Introduction of ADORA2A

ADORA2A is encoded by ADORA2A gene. It belongs to the G-protein-coupled receptor (GPCR) family which has been extensively studied during the past few decades because it offers numerous possibilities for therapeutic applications. It is one of the four subtypes of adenosine receptors (A1R, A2AR, A2BR, A3R). ADORA2A possess seven transmembrane alpha helices and uses adenosine as the preferred endogenous agonist. Meanwhile, its structure reveals a ligand binding pocket distinct from that of other structurally determined GPCRs.

Function of ADORA2A Membrane Protein

The activity of ADORA2A is mediated by G proteins, resulting in the activation of adenylyl cyclase and elevating intracellular cAMP. ADORA2A plays a vital role in many biological functions, such as cardiac rhythm and circulation, cerebral and renal blood flow, immune function, pain regulation, and sleep. Since ADORA2A is enriched in brains and involves in the regulation of glutamate and dopamine release, it is a potential therapeutic target of certain neurological diseases such as insomnia, pain regulation, depression, drug addiction, and Parkinson's disease. It is also a major target of caffeine, which is a competitive antagonist of this protein. Besides, ADORA2A is also abundant in vasculature and platelets and participates in the regulation of myocardial oxygen consumption and blood pressure. It is supposed to regulate myocardial oxygen demand and to increase the coronary circulation by vasodilation. In addition, it can negatively regulate over-reactive immune cells and protect tissues from collateral inflammatory damages by suppressing immune cells.

Fig.1 Structure of ADORA2A membrane protein.

Application of ADORA2A Membrane Protein in Literature

1. Domenici M.R., et al. Neuronal adenosine A_2A receptor overexpression is neuroprotective towards 3-nitropropionic acid-induced striatal toxicity: a rat model of Huntington's disease. Purinergic Signal. 2018, 14(3): 235-243. PubMed ID: 29770921

This article reports that the selective overexpression of ADORA2A at the neuronal level reduced 3-NP-induced neurodegeneration, which suggests an important function of the neuronal ADORA2A in the modulation of neurodegeneration.

2. Zheng Z., et al. Lumbar sympathectomy reduces vascular permeability, possibly through decreased adenosine receptor A2a expression in the hind plantar skin of rats. Clin Hemorheol Microcirc. 2018, 68(1): 5-15. PubMed ID: 29439317

This article reveals that reduced expression of ADORA2A is possibly related to that vascular permeability in the hind plantar skin of rats decreases following lumbar sympathectomy.

3. Caliman A.D., et al. Mapping the allosteric sites of the A_2A adenosine receptor. Chem Biol Drug Des. 2018, 91(1): 5-16. PubMed ID: 28639411

Authors in this group apply the fragment-based mapping algorithm, FTMap, on the conformations of ADORA2A and uncover five non-orthosteric sites on the ADORA2A. These sites are potential for the treatment of inflammatory and neurological diseases.

4. Schulz N., et al. Critical role for adenosine receptor A2a in β-cell proliferation. Mol Metab. 2016, 5(11): 1138-1146. PubMed ID: 27818940

This article focuses on the pharmacological activation of adenosine signaling in β-cell proliferation in zebrafish. It shows that A2a receptor plays an important role in adenosine signaling and compensatory β-cell proliferation. Meanwhile, this feature can be used in future therapeutic development for diabetes.

5. Li H., et al. Pentoxifylline inhibits pulmonary inflammation induced by infrarenal aortic cross-clamping dependent of adenosine receptor A2A. Am J Transl Res. 2016, 8(5): 2210-21. PubMed ID: 27347328

This article evaluates the protective effects of pentoxifylline in a rat model of infrarenal aortic cross-clamping (IAC), which is commonly used during infrarenal vascular operations. It indicates that pentoxifylline plays a protective role in IAC-induced acute lung injury in rats by inhibiting pulmonary inflammation and ADORA2A participates in this regulation through A2A signaling pathways.

ADORA2A Preparation Options

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