Adenosine A_2A Receptor (human, recombinant)

Adenosine A_2A receptor (human, recombinant) contains amino acids corresponding to the full length, wild-type, human A_2A receptor, as well as N-terminal histidine and streptavidin tags with a TEV protease cleavage site. The A_2A receptor is a G protein-coupled receptor (GPCR) that is activated by adenosine on presynaptic terminals to induce neurotransmitter release and on postsynaptic terminals to increase excitability.¹ Signaling through the A_2A receptor occurs through G_s, G_olf, and G_15/16 proteins to increase cyclic AMP or inositol-(1,4,5)-trisphosphate (IP₃) activity.² It is expressed in the brain on striatal-pallidal GABAergic neurons and in the olfactory bulb as well as other brain regions. It is also expressed in the periphery in organs and cells involved with immune function, including the spleen, thymus, leukocytes, and blood platelets as well as in the heart, lung, and blood vessels. A_2A receptor activity induced by agonists has neurodegenerative effects, which has led to the development of A_2A receptor antagonists, but has shown mixed effects on seizure activity in rodent models.¹ The A_2A receptor also plays a role in the regulation of enteric nervous system function, vasodilation of coronary arteries, and the immune response.³ In addition to signaling through the A_2A receptor alone, it can form heteromers with other GPCRs, including adenosine A₁, dopamine D₂ and D₃, cannabinoid CB₁, and metabotropic glutamate receptor 5 (mGluR5).^4,5 The function of these receptors is influenced by the interaction, with the A_2A receptor decreasing dopamine binding to the D₂ receptor and mGluR5 potentiating the effects of the A_2A receptor on adenylyl cyclase and MAPK signaling.⁴ Cayman's Adenosine A_2A Receptor (human, recombinant) protein is provided in a virus-like particle (VLP) format, which helps maintain this membrane protein in a native-like conformation and lipid environment for use in binding assays. This protein consists of 420 amino acids and has a calculated molecular weight of 45.71 kDa.

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1. Stockwell, J., Jakova, E., and Cayabyab, F.S. Adenosine A₁ and A_2A receptors in the brain: Current research and their role in neurodegeneration. Molecules 22(4), pii: E676 (2017).

2. Fredholm, B.B., Arslan, G., Halldner, L., et al. Structure and function of adenosine receptors and their genes. Naunyn Schmiedebergs Arch. Pharmacol. 362(4-5), 364-374 (2000).

3. Sousa, J.B., and Diniz, C. The adenosinergic system as a therapeutic target in the vasculature: New ligands and challenges. Molecules 22(5), pii: E752 (2017).

4. Ferré, S., Ciruela, F., Quiroz, C., et al. Adenosine receptor heteromers and their integrative role in striatal function. ScientificWorldJournal 7, 74-85 (2007).

5. Torvinen, M., Marcellino, D., Canals, M., et al. Adenosine A_2A receptor and dopamine D₃ receptor interactions: Evidence of functional A_2A/D₃ heteromeric complexes. Mol. Pharmacol. 67(2), 400-407 (2005).