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Review ArticleReview Article

The A3 Adenosine Receptor: History and Perspectives

Pier Andrea Borea, Katia Varani, Fabrizio Vincenzi, Pier Giovanni Baraldi, Mojgan Aghazadeh Tabrizi, Stefania Merighi and Stefania Gessi
David R. Sibley, ASSOCIATE EDITOR
Pharmacological Reviews January 2015, 67 (1) 74-102; DOI: https://doi.org/10.1124/pr.113.008540
Pier Andrea Borea
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
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Katia Varani
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
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Fabrizio Vincenzi
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
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Pier Giovanni Baraldi
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
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Mojgan Aghazadeh Tabrizi
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
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Stefania Merighi
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
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Stefania Gessi
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
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David R. Sibley
Department of Medical Sciences, Pharmacology Section (P.A.B., K.V., F.V., S.M., S.G.), and Department of Pharmaceutical Sciences, University of Ferrara, Italy (P.G.B., M.A.T.)
Roles: ASSOCIATE EDITOR
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Abstract

By general consensus, the omnipresent purine nucleoside adenosine is considered a major regulator of local tissue function, especially when energy supply fails to meet cellular energy demand. Adenosine mediation involves activation of a family of four G protein–coupled adenosine receptors (ARs): A1, A2A, A2B, and A3. The A3 adenosine receptor (A3AR) is the only adenosine subtype to be overexpressed in inflammatory and cancer cells, thus making it a potential target for therapy. Originally isolated as an orphan receptor, A3AR presented a twofold nature under different pathophysiologic conditions: it appeared to be protective/harmful under ischemic conditions, pro/anti-inflammatory, and pro/antitumoral depending on the systems investigated. Until recently, the greatest and most intriguing challenge has been to understand whether, and in which cases, selective A3 agonists or antagonists would be the best choice. Today, the choice has been made and A3AR agonists are now under clinical development for some disorders including rheumatoid arthritis, psoriasis, glaucoma, and hepatocellular carcinoma. More specifically, the interest and relevance of these new agents derives from clinical data demonstrating that A3AR agonists are both effective and safe. Thus, it will become apparent in the present review that purine scientists do seem to be getting closer to their goal: the incorporation of adenosine ligands into drugs with the ability to save lives and improve human health.

Footnotes

  • dx.doi.org/10.1124/pr.113.008540.

  • Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 67 (1)
Pharmacological Reviews
Vol. 67, Issue 1
1 Jan 2015
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Review ArticleReview Article

The A3 Receptor: History and Perspectives

Pier Andrea Borea, Katia Varani, Fabrizio Vincenzi, Pier Giovanni Baraldi, Mojgan Aghazadeh Tabrizi, Stefania Merighi and Stefania Gessi
Pharmacological Reviews January 1, 2015, 67 (1) 74-102; DOI: https://doi.org/10.1124/pr.113.008540

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Review ArticleReview Article

The A3 Receptor: History and Perspectives

Pier Andrea Borea, Katia Varani, Fabrizio Vincenzi, Pier Giovanni Baraldi, Mojgan Aghazadeh Tabrizi, Stefania Merighi and Stefania Gessi
Pharmacological Reviews January 1, 2015, 67 (1) 74-102; DOI: https://doi.org/10.1124/pr.113.008540
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  • Article
    • Abstract
    • I. Introduction
    • II. The Discovery of the A3 Adenosine Receptor
    • III. Molecular Characterization of the A3 Adenosine Receptor
    • IV. Medicinal Chemistry and Pharmacology of A3 Adenosine Receptor Ligands
    • V. Distribution of the A3 Adenosine Receptor
    • VI. Intracellular Pathways Regulated by the A3 Adenosine Receptor
    • VII. Biologic Functions and Therapeutic Applications of the A3 Adenosine Receptor
    • VIII. Recent Drug Development Efforts
    • IX. Concluding Remarks
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