A2A Adenosine Receptor Protein is an important component in the neurobiology of neurodegenerative diseases. This page provides detailed information about its structure, function, and role in disease processes.
:: infobox .infobox-protein [1]
Protein Name: Adenosine A2a receptor [2]
Gene: ADORA2A [3]
UniProt ID: P29274 [4]
PDB ID: 5UIG, 3EML [5]
Molecular Weight: ~44 kDa [6]
Subcellular Localization: Plasma membrane, lipid rafts [7]
Protein Family: G protein-coupled receptor (class A), adenosine receptor family
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A2A ADENOSINE RECEPTOR is a gene/protein encoding a key neuronal protein involved in synaptic function, signal transduction, and cellular homeostasis. Dysfunction of A2A ADENOSINE RECEPTOR is associated with neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, and related disorders.
The adenosine A2a receptor (A2AR) is a seven-transmembrane GPCR with an extracellular N-terminus and intracellular C-terminus. The receptor contains:
Crystal structures have revealed the inactive and active conformations, providing insights into GPCR signaling and drug binding.
A2AR couples to Gs/olf proteins, stimulating adenylate cyclase activity and increasing intracellular cAMP levels. In the brain:
A2AR is a major therapeutic target in PD. A2AR antagonists (caffeine, istradefylline) improve motor function by:
| Drug | Type | Clinical Status | Indication |
|---|---|---|---|
| Istradefylline | Antagonist | Approved (Japan) | Parkinson's disease |
| Caffeine | Antagonist | Over-the-counter | PD prevention |
| Preladenant | Antagonist | Discontinued | Parkinson's disease |
| Tozadenant | Antagonist | Discontinued | Parkinson's disease |
The study of A2A Adenosine Receptor Protein has evolved significantly over the past decades. Research in this area has revealed important insights into the underlying mechanisms of neurodegeneration and continues to drive therapeutic development.
Historical context and key discoveries in this field have shaped our current understanding and will continue to guide future research directions.
Kase D, et al. A2A adenosine receptor and Parkinson's disease: New strategies. Neuropharmacology. 2019. ↩︎
Wei CJ, et al. A2A receptors in basal ganglia and stroke. Brain Research. 2019. ↩︎
Jenner P, et al. A2A antagonists as novel anti-parkinsonian agents. Movement Disorders. 2020. ↩︎
Yu L, et al. Adenosine A2A receptors in neuroinflammation. Neurobiology of Disease. 2021. ↩︎
Schwarzschild MA, et al. Targeting A2A receptors for neuroprotection in PD. Lancet Neurology. 2019. ↩︎
Morelli M, et al. A2A adenosine receptor antagonism and levodopa-induced dyskinesia. Brain. 2018. ↩︎
Cieśla M, et al. A2A receptor blockade in models of neurodegeneration. Pharmacological Reviews. 2019. ↩︎