Protein / target
Adenosine receptor A2a
Protein at a glance
Biological role
Type 5 metabotropic glutamate receptor binding
Strongest disease association
Parkinson's Disease
Therapeutic position
Established drug target
Research activity
Emerging research
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Receptor for adenosine.
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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.
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Excitatory neurotransmission
- ·glutamatergic synapse
- ·excitatory postsynaptic potential
- ·positive regulation of synaptic transmission, glutamatergic
- ·synaptic transmission, glutamatergic
Cell proliferation & survival
- ·negative regulation of cell population proliferation
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
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.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
10 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Adenosine A2 receptor agonist
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene ADORA2A
Gene-level evidence surfaced through the gene ADORA2A that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
View evidence synthesis (4)Hide
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 per-type scores above show the calculation.
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Drug development
27 compounds recorded · 10 approved · 17 in clinical development
View all recorded compounds (10)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
View underlying tractability evidence (10)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 2 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- 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 publicationm<sup>1</sup>A in CAG repeat RNA binds to TDP-43 and induces neurodegeneration.
- New publicationThe Immune Regulatory Role of Adenosine in the Tumor Microenvironment.
- Regulatory approval
Approval: Defitelio (EMA)
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.
Research activity
Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.
Most cited
Recent
Europe PMC papers linked directly to this protein.