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26 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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ADORA2A
adenosine A2a receptor
Chromosome 22 · 22q11.23
NCBI Gene: 135Ensembl: ENSG00000128271.23HGNC: HGNC:263UniProt: A8K1F6
412PubMed Papers
20Diseases
28Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
RESEARCH IMPACT
Highly StudiedTrending
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
lipid bindingprotein bindingG protein-coupled adenosine receptor activityenzyme bindingmigraine disorderasthmaParkinson diseaseparoxysmal tachycardia
✦AI Summary

ADORA2A encodes the adenosine A2a receptor, a G protein-coupled receptor that mediates adenosine signaling through activation of adenylyl cyclase. The receptor plays crucial roles in multiple physiological and pathological processes. In endothelial cells, ADORA2A promotes pathological angiogenesis by enhancing HIF-1α-dependent glycolysis through ERK/Akt signaling pathways 1. The receptor also drives endothelial-to-mesenchymal transition, contributing to subretinal fibrosis in age-related macular degeneration 2. In cancer, ADORA2A upregulation during neuroendocrine differentiation rewires proline metabolism via ERK/MYC/PYCR signaling, promoting epigenetic reprogramming and lineage plasticity 3. The receptor mediates immunosuppressive effects during sepsis, where adenosine produced by CD39hi B cells signals through ADORA2A to impair macrophage function 4. Genetic polymorphisms in ADORA2A influence caffeine metabolism and consumption patterns, with variants affecting habitual caffeine intake by 3-32% 5. Sleep homeostasis involves adenosine signaling, with basal forebrain glutamatergic neurons controlling extracellular adenosine levels 6. These findings highlight ADORA2A as a promising therapeutic target for treating angiogenic diseases, cancer lineage plasticity, and sepsis-induced immunosuppression.

Sources cited
1
ADORA2A promotes pathological angiogenesis by enhancing HIF-1α-dependent glycolysis through ERK/Akt signaling
PMID: 28928465
2
ADORA2A drives endothelial-to-mesenchymal transition contributing to subretinal fibrosis
PMID: 38446902
3
ADORA2A upregulation rewires proline metabolism and promotes epigenetic reprogramming in neuroendocrine cancers
PMID: 38099497
4
ADORA2A mediates immunosuppressive effects during sepsis through adenosine signaling
PMID: 34473957
5
ADORA2A genetic variants influence caffeine metabolism and consumption patterns
PMID: 39438936
6
Adenosine signaling is involved in sleep homeostasis regulation
PMID: 32883833
Disease Associationsⓘ20
migraine disorderOpen Targets
0.61Moderate
asthmaOpen Targets
0.61Moderate
Parkinson diseaseOpen Targets
0.61Moderate
paroxysmal tachycardiaOpen Targets
0.59Moderate
ApneaOpen Targets
0.57Moderate
PainOpen Targets
0.57Moderate
Wolff-Parkinson-White SyndromeOpen Targets
0.56Moderate
Airway obstructionOpen Targets
0.55Moderate
hepatic veno-occlusive diseaseOpen Targets
0.54Moderate
neurodegenerative diseaseOpen Targets
0.53Moderate
HeadacheOpen Targets
0.53Moderate
chronic obstructive pulmonary diseaseOpen Targets
0.53Moderate
cardiovascular diseaseOpen Targets
0.51Moderate
chronic bronchitisOpen Targets
0.46Moderate
intermittent vascular claudicationOpen Targets
0.43Moderate
coronary artery diseaseOpen Targets
0.40Moderate
attention deficit hyperactivity disorderOpen Targets
0.39Weak
drug dependenceOpen Targets
0.37Weak
CoughOpen Targets
0.37Weak
orthostatic hypotensionOpen Targets
0.37Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets28
ADENOSINEApproved
Adenosine receptor agonist
Wolff-Parkinson-White Syndrome
AMINOPHYLLINEApproved
Adenosine receptor antagonist
asthma
AMP579Phase II
Adenosine A1 receptor agonist
familial hyperlipidemia
APADENOSONPhase III
Adenosine A2a receptor agonist
coronary artery disease
BINODENOSONPhase III
Adenosine A2a receptor agonist
hypertension
BVT.115959Phase II
Adenosine A2a receptor agonist
Pain
CAFFEINEApproved
Adenosine receptor antagonist
migraine disorder
CAFFEINE CITRATEApproved
Adenosine receptor antagonist
Apnea
CIFORADENANTPhase I/II
Adenosine A2a receptor antagonist
Parkinson disease
DEFIBROTIDEApproved
Adenosine A2 receptor agonist
Recurrent thrombophlebitis
ETRUMADENANTPhase II
Adenosine A2b receptor antagonist
metastatic prostate cancer
EVODENOSONPhase I/II
Adenosine A2a receptor agonist
arteriosclerosis
IMARADENANTPhase II
Adenosine A2a receptor antagonist
prostate cancer
ISTRADEFYLLINEApproved
Adenosine A2a receptor antagonist
Parkinson disease
OXTRIPHYLLINEApproved
Adenosine receptor antagonist
Cough
PBF-509Phase I/II
Adenosine A2a receptor antagonist
non-small cell lung carcinoma
PBF-999Phase I
Phosphodiesterase 10A inhibitor
Huntington disease
PENTOXIFYLLINEApproved
Adenosine A2 receptor antagonist
cardiovascular disease
PRELADENANTPhase III
Adenosine A2a receptor antagonist
Parkinson disease
REGADENOSONApproved
Adenosine A2a receptor agonist
cardiovascular disease
REGADENOSON ANHYDROUSPhase III
Adenosine A2a receptor agonist
coronary artery disease
SIPAGLADENANTPhase II
Adenosine A2a receptor inverse agonist
Parkinson disease
SONEDENOSONPhase II
Adenosine A2a receptor agonist
diabetic foot
ST1535Phase I
Adenosine A2a receptor antagonist
THEOPHYLLINEApproved
Phosphodiesterase 4 inhibitor
asthma
TOZADENANTPhase III
Adenosine A2a receptor antagonist
Parkinson disease
UK432097Phase II
Adenosine A2a receptor agonist
chronic obstructive pulmonary disease
VIPADENANTPhase II
Adenosine A2a receptor antagonist
Parkinson disease
Related Genes
GRM5Protein interaction100%NTRK1Protein interaction99%PRKACBProtein interaction99%GNASProtein interaction95%NTRK2Protein interaction94%VIPProtein interaction91%
Tissue Expression6 tissues
Bone Marrow
100%
Liver
82%
Lung
15%
Ovary
12%
Brain
4%
Heart
0%
Gene Interaction Network
Click a node to explore
ADORA2AGRM5NTRK1PRKACBGNASNTRK2VIP
PROTEIN STRUCTURE
Preparing viewer…
PDB5NM4 · 1.70 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.85LoF Tolerant
pLIⓘ
0.03Tolerant
Observed/Expected LoF0.51 [0.32–0.85]
RankingsWhere ADORA2A stands among ~20K protein-coding genes
  • #697of 20,598
    Most Researched412 · top 5%
  • #149of 1,025
    FDA-Approved Drug Targets10 · top quartile
  • #7,304of 17,882
    Most Constrained (LOEUF)0.85
Genes detectedADORA2A
Sources retrieved26 papers
Response time—
📄 Sources
26▼
1
International society of sports nutrition position stand: caffeine and exercise performance.
PMID: 33388079
J Int Soc Sports Nutr · 2021
1.00
2
ADORA2A-driven proline synthesis triggers epigenetic reprogramming in neuroendocrine prostate and lung cancers.
PMID: 38099497
J Clin Invest · 2023
0.90
3
Effects of Caffeine on Resistance Exercise: A Review of Recent Research.
PMID: 34291426
Sports Med · 2021
0.80
4
Genetic susceptibility to caffeine intake and metabolism: a systematic review.
PMID: 39438936
J Transl Med · 2024
0.70
5
PARylation of POLG Mediated by PARP1 Accelerates Ferroptosis-Induced Vascular Calcification via Activating Adora2a/Rap1 Signaling.
PMID: 40401372
Arterioscler Thromb Vasc Biol · 2025
0.64