Abstract
Background: Adenosine receptors (ARs) are classified as A1, A2A, A2B, and A3 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, A2B 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 A2B AR is implicated and discusses the potential
role of subtype-selective A2B 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 A2B AR ligands and their therapeutic role in treating various disease conditions. A special focus has been
given to the therapeutic potentials of selective A2B AR ligands in the management of airway inflammatory conditions
and cancer.
Conclusions: This systematic review demonstrates the current status and perspectives of A2B AR ligands as
therapeutically useful agents that would assist medicinal chemists and pharmacologists in discovering novel and
subtype-selective A2B AR ligands as potential drug candidates.
Keywords:
A2B adenosine receptor, asthma, cancer, diabetes, GIT disorders, G-protein coupled receptors (GPCRs).
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