Therapeutic Potentials of A2B Adenosine Receptor Ligands: Current Status and Perspectives

Background: Adenosine receptors (ARs) are classified as A(1), A(2A), A(2B), and A(3) subtypes belong to the superfamily of G-protein coupled receptors (GPCRs). More than 40% of modern medicines act through either activation or inhibition of signaling processes associated with GPCRs. In particular, A(2B) AR signaling pathways are implicated in asthma, inflammation, cancer, ischemic hyperfusion, diabetes mellitus, cardiovascular diseases, gastrointestinal disorders, and kidney disease. Methods: This article reviews different disease segments wherein A(2B) AR is implicated and discusses the potential role of subtype-selective A(2B) AR ligands in the management of such diseases or disorders. All the relevant publications on this topic are reviewed and presented scientifically. Results: This review provides an up-to-date highlight of the recent advances in the development of novel and selective A(2B) AR ligands and their therapeutic role in treating various disease conditions. A special focus has been given to the therapeutic potentials of selective A(2B) AR ligands in the management of airway inflammatory conditions and cancer. Conclusions: This systematic review demonstrates the current status and perspectives of A(2B) AR ligands as therapeutically useful agents that would assist medicinal chemists and pharmacologists in discovering novel and subtype-selective A(2B) AR ligands as potential drug candidates.