Adenosine receptor A2b (ADORA2B) (ADORA2B)

The Adenosine receptor A2b (ADORA2B) is a G protein-coupled receptor (GPCR) belonging to the P1 purinergic receptor family [2, 13]. It is characterized by its low affinity for adenosine, requiring micromolar concentrations typically found in stressed or hypoxic environments for activation [6, 8]. Upon ligand binding, A2b primarily signals through Gs proteins to increase intracellular cAMP, although it can also couple with Gq and Gi proteins in a cell-specific manner [2, 14]. This receptor plays a dual role in inflammation, promoting pro-inflammatory cytokine release (e.g., IL-6, IL-8) from mast cells and fibroblasts while also inducing anti-inflammatory mediators like IL-10 in other contexts [1, 2, 10]. In oncology, A2b is frequently overexpressed and contributes to tumor progression by promoting angiogenesis, metastasis, and an immunosuppressive microenvironment [5, 10]. Consequently, A2b antagonists are being explored for cancer and asthma, while agonists are investigated for their cardioprotective and metabolic benefits [2, 6, 7]. Additionally, A2b interacts with netrin-1 to regulate axon elongation and has been implicated in the regulation of vascular tone and adipogenesis [6, 12]. Its complex, often paradoxical, roles in disease make it a challenging but promising therapeutic target [5, 10].

Other names

ADORA2BAdenosine A2b receptorADORA2AA2BR

Adenosine receptor antagonism and agonism [2, 7, 10]