The field of therapeutic application of the A₃ adenosine receptor (A₃AR) antagonists represents a rapidly growing and intense area of research in the adenosine field. Even if there are currently no A₃AR antagonists in clinical phases, in light of the plethora of biological effects attributed to A₃ARs, substantial efforts in medicinal chemistry have been directed toward developing antagonists for the A₃AR subtype. In this review, we summarize the more recent and promising evidences of the possible A₃AR application as drug candidates, and the role of the receptor-driven design in their in silico characterization.
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