Pharmacology of Adenosine Receptors: The State of the Art

Physiological Reviews
Pier Andrea BoreaKatia Varani

Abstract

Adenosine is a ubiquitous endogenous autacoid whose effects are triggered through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Due to the rapid generation of adenosine from cellular metabolism, and the widespread distribution of its receptor subtypes in almost all organs and tissues, this nucleoside induces a multitude of physiopathological effects, regulating central nervous, cardiovascular, peripheral, and immune systems. It is becoming clear that the expression patterns of adenosine receptors vary among cell types, lending weight to the idea that they may be both markers of pathologies and useful targets for novel drugs. This review offers an overview of current knowledge on adenosine receptors, including their characteristic structural features, molecular interactions and cellular functions, as well as their essential roles in pain, cancer, and neurodegenerative, inflammatory, and autoimmune diseases. Finally, we highlight the latest findings on molecules capable of targeting adenosine receptors and report which stage of drug development they have reached.

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Methods Mentioned

BETA
deamination
glycosylation
surgical resection
coronary artery bypass
antisense oligonucleotide
xenograft

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NCT02509546
NCT03098979
NCT02992288
NCT01788631
NCT01446094
NCT02115308
NCT02130453
NCT03103061
NCT02589977
NCT03090087

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