Adenosine A2A receptor (ADORA2A)
The A2A receptor is where adenosine lands on a T cell and tells it to rest. Oral antagonists, cousins of caffeine, are in phase 2 combinations with PD-1 blockade and chemotherapy.
Overview
ADORA2A (chromosome 22q11.23) encodes a G-protein-coupled adenosine receptor whose activity is mediated by G proteins that activate adenylyl cyclase (UniProt P29274). Ectonucleotidases and adenosine receptors are broadly expressed and have emerged as immuno-oncology targets, with early-phase trials showing promising results (Allard et al. 2019, Immunol Rev). Ciforadenant is in phase 1b/2 with ipilimumab and nivolumab (NCT05501054), etrumadenant (A2A/A2B) in phase 2 combinations in pancreatic cancer (NCT06048484), and inupadenant in phase 2 with chemotherapy in non-squamous non-small-cell lung cancer (NCT05403385).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · The A2A receptor is where adenosine lands on a T cell and tells it to rest. Oral antagonists, cousins of caffeine, are in phase 2 combinations with PD-1 blockade and chemotherapy.
- 1 · What it is
The A2A receptor is where adenosine lands on a T cell and tells it to rest. Oral antagonists, cousins of caffeine, are in phase 2 combinations with PD-1 blockade and chemotherapy.
- 2 · What goes wrong in cancer
The receptor end of the CD39-CD73-adenosine axis; antagonists are small molecules.
- 3 · How drugs use it
No product in this corpus aims at Adenosine A2A receptor (ADORA2A) yet. Because it sits on the outside of the cell, it can be reached from the bloodstream: antibodies flag the cell, ADCs deliver a toxin, radioligands deliver radiation, and CAR-T or bispecifics bring a T cell.
External identifiers
Sources: HGNC HGNC:263 (approved symbol, name, aliases and cross-references); UniProt P29274 (protein name, function and tissue specificity)
Biology
The receptor end of the CD39-CD73-adenosine axis; antagonists are small molecules.
- Broadly expressed, per Allard et al. 2019; UniProt records no human tissue distribution
- Pancreatic and non-small-cell lung cancer trials of antagonists
Notes
top- Prevalence not recorded: HGNC and UniProt carry no positivity rates.
Latest papers
topQuery for this target: (TITLE:"Adenosine A2A receptor" OR ABSTRACT:"Adenosine A2A receptor" OR TITLE:"ADORA2A" OR ABSTRACT:"ADORA2A" OR TITLE:"A2AR" OR ABSTRACT:"A2AR" OR TITLE:"A2A receptor" OR ABSTRACT:"A2A receptor" OR TITLE:"adenosine A2a receptor" OR ABSTRACT:"adenosine A2a receptor" OR TITLE:"RDC8" OR ABSTRACT:"RDC8") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Adenosine A2A receptor (ADORA2A), not a curated reading list.
Similar pages
not linked directly; found by shared links- TargetTDO2
Shares The cancer-immunity cycle, Checkpoint (two meanings) and the tag checkpoint-map.
- TargetCD96
Shares The cancer-immunity cycle, Checkpoint (two meanings), Non-small-cell lung cancer and the tag checkpoint-map.
- TargetLILRB1 (ILT2)
Shares The cancer-immunity cycle, Checkpoint (two meanings) and the tag checkpoint-map.
- TargetHHLA2 (B7-H7)
Shares The cancer-immunity cycle, Checkpoint (two meanings) and the tag checkpoint-map.
- TargetGITR (TNFRSF18)
Shares The cancer-immunity cycle, Checkpoint (two meanings) and the tag checkpoint-map.
- TargetCD27
Shares The cancer-immunity cycle, Checkpoint (two meanings) and the tag checkpoint-map.
- TargetHLA-E
Shares The cancer-immunity cycle, Checkpoint (two meanings) and the tag checkpoint-map.
- TargetLILRB2 (ILT4)
Shares The cancer-immunity cycle, Checkpoint (two meanings) and the tag checkpoint-map.