The A3 adenosine receptor: history and perspectives

Area of Science:

• Biochemistry
• Pharmacology
• Immunology

Background:

• Adenosine is a purine nucleoside regulating tissue function, especially during energy deficit.
• Adenosine receptors (ARs), a family of G protein-coupled receptors, mediate adenosine's effects.
• The A(3) adenosine receptor (A(3)AR) is overexpressed in inflammatory and cancer cells, presenting a therapeutic target.

Observation:

• A(3)AR exhibits dual roles, acting protectively or harmfully in various pathophysiological conditions.
• The therapeutic potential of selective A(3)AR agonists versus antagonists was a significant challenge.
• Clinical data indicate A(3)AR agonists are effective and safe.

Findings:

• A(3)AR agonists are currently in clinical development for rheumatoid arthritis, psoriasis, glaucoma, and hepatocellular carcinoma.
• The overexpression of A(3)AR in disease states supports its role as a therapeutic target.
• Adenosine ligands are progressing towards clinical application for significant health benefits.

Implications:

• Targeting A(3)AR with agonists offers a promising therapeutic strategy for various diseases.
• The development of adenosine-based drugs could lead to life-saving treatments.
• Further research into adenosine receptor modulation may unlock new avenues for disease management.