Protein / target
Adenosine receptor A2a
Protein at a glance
Biological role
Type 5 metabotropic glutamate receptor binding
Primary system
Nervous system
Strongest disease association
Parkinson disease
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
10 approved · 17 in clinical development
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Receptor for adenosine (By similarity). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase (By similarity)
Subcellular location
Domains and Gene Ontology detail (62)Hide
Gene Ontology
- Casymmetric synapse
- Caxolemma
- Cdendrite
- Cglutamatergic synapse
- Cintermediate filament
- Cmembrane
- Cneuronal cell body
- Cplasma membrane
- Cpostsynaptic membrane
- Cpresynaptic active zone
- Cpresynaptic membrane
- Falpha-actinin binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Excitatory neurotransmission
- ·glutamatergic synapse
- ·excitatory postsynaptic potential
- ·positive regulation of synaptic transmission, glutamatergic
- ·synaptic transmission, glutamatergic
Synaptic signalling
- ·asymmetric synapse
- ·glutamatergic synapse
- ·postsynaptic membrane
- ·presynaptic active zone
G protein-coupled signalling
- ·G protein-coupled adenosine receptor activity
- ·adenylate cyclase-activating G protein-coupled receptor signaling pathway
- ·adenylate cyclase-modulating G protein-coupled receptor signaling pathway
- ·G protein-coupled adenosine receptor signaling pathway
Apoptosis & cell death
- ·apoptotic process
- ·negative regulation of neuron apoptotic process
Immune signalling
- ·inflammatory response
Transcriptional regulation
- ·regulation of DNA-templated transcription
View underlying pathways (4)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Adenosine receptor agonist
Appears in clinical studies involving paroxysmal tachycardia, Wolff-Parkinson-White syndrome, cardiovascular disorder, Paroxysmal supraventricular tachycardia
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Highest overall evidence
Remaining associations by Open Targets' aggregated evidence score.
Show all associationsHide all associations
Open Targets ranks 957 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 27 total
cardiovascular disorder · COVID-19 · sickle cell disease
chronic obstructive pulmonary disease
diabetic foot
asthma · chronic bronchitis · chronic obstructive pulmonary disease
acute chest syndrome · sickle cell disease
cardiovascular disorder · intermittent vascular claudication · liver failure
non-small cell lung carcinoma
Parkinson disease · Parkinson disease
Parkinson disease · Parkinson disease · Parkinson disease
coronary artery disorder
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.
- New publicationAdenosine Receptors in Neuroinflammation and Neurodegeneration.
- New publicationREDIportal: toward an integrated view of the A-to-I editing.
- New publicationAdvances in A-to-I RNA editing in cancer.
- New publicationMicroglia regulate motor neuron plasticity via reciprocal fractalkine and adenosine signaling.
- New publicationAstrocytic neuroligin 3 regulates social memory and synaptic plasticity through adenosine signaling in male mice.
- New publicationWTAP participates in neuronal damage by protein translation of NLRP3 in an m6A-YTHDF1-dependent manner after traumatic brain injury.
- New publicationAdenosine and adenosine receptors in metabolic imbalance-related neurological issues.
- New publicationAstrocytic ALKBH5 in stress response contributes to depressive-like behaviors in mice.
- New publicationAdenosine and Cortical Plasticity.
- New publicationProgrammable RNA N<sup>6</sup>-methyladenosine editing with CRISPR/dCas13a in plants.
- New publicationm<sup>1</sup>A in CAG repeat RNA binds to TDP-43 and induces neurodegeneration.
- New publicationUtilizing AAV-mediated LEAPER 2.0 for programmable RNA editing in non-human primates and nonsense mutation correction in humanized Hurler syndrome mice.
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.