Target intelligence / Profile preview

Adenosine receptor A2B and Adenosine receptor A3 (A2BAR and A3AR)

Target
A2BAR and A3AR
Molecular classification
G protein-coupled receptor, Class A GPCR, Receptor
01

Overview

Adenosine receptors A2B and A3 are distinct subtypes of the G protein-coupled receptor (GPCR) family that mediate the physiological and pathological effects of extracellular adenosine. The A2B receptor is characterized by its low affinity for adenosine, typically becoming active under conditions of high adenosine concentration such as hypoxia, inflammation, and tissue injury. In contrast, the A3 receptor is a high-affinity subtype involved in complex signaling pathways that regulate cell survival, immune responses, and cardioprotection. Both receptors are frequently overexpressed in various cancers and inflammatory diseases, serving as critical nodes in the tumor microenvironment and autoimmune progression. Therapeutic strategies involve the use of A2B antagonists to inhibit tumor growth and asthma-related inflammation, while A3 agonists are being developed for their anti-inflammatory and pro-apoptotic effects in rheumatoid arthritis and liver cancer. Dual targeting of these receptors is an area of active research, aiming to leverage their combined roles in modulating immune surveillance and tissue repair.

Other names
ADORA2BADORA3A2B adenosine receptorA3 adenosine receptorAdenosine A2B receptorAdenosine A3 receptorPurinergic receptor A2BPurinergic receptor A3
02

Mechanism of action

Agonism and Antagonism

03

Biological functions

Signal transductionImmune responseCell proliferationCell deathInflammationVasodilationCardioprotectionMast cell degranulationAngiogenesis
04

Disease associations

CancerInflammationAsthmaCardiovascular diseaseDiabetesRenal diseaseRheumatoid arthritisPsoriasisIschemia-reperfusion injury
05

Safety considerations

Paradoxical pro- and anti-inflammatory effectsSpecies-dependent pharmacological profiles (human vs rodent)Potential cardiovascular side effectsMetabolic effects on glucose and lipid homeostasis
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Interacting drugs

PBF-1129

11 more in the full profile.

07

Biomarkers

A3AR expression in peripheral blood mononuclear cells (PBMCs)A2BAR expression in tumor tissueExtracellular adenosine levels

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