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Target intelligence / Profile preview
Adenosine Receptor A₂ᴮ (ADORA₂ᴮ)
- Target
- ADORA₂ᴮ
- Molecular classification
- GPCR, G protein-coupled receptor, Class-A GPCR, Receptor
01
Overview
The adenosine A2B receptor (ADORA2B) is a G protein-coupled receptor that binds adenosine. It is broadly expressed and has low affinity for adenosine, requiring micromolar concentrations for activation, which typically occurs during tissue stress. It primarily couples to Gs proteins, increasing cAMP. It plays roles in vascular tone, immune cell function, and is implicated in cancer, renal disease, diabetes, vascular diseases, lung diseases, and inflammatory disorders, making it a therapeutic target for these conditions.
- Other names
- A2B adenosine receptor
02
Mechanism of action
Agonism of adenylyl cyclase via Gs protein coupling; antagonism to block adenosine binding and downstream signaling.
03
Biological functions
Signal transductionImmune modulationVascular regulationSmooth muscle relaxation
04
Disease associations
Cancer progressionCancer metastasisDiabetes mellitus complicationsRenal diseaseAsthmaInflammatory disordersVascular diseasesHypertension
05
Safety considerations
Potential for off-target effects due to structural similarities with other adenosine receptors.Complex role in different tissues and disease stages may lead to unintended consequences upon modulation.
06
Interacting drugs
BAY 60–6583
15 more in the full profile.
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