Adenosine Receptors: Structure, Distribution, and Signal Transduction

  • Stefania Merighi
  • Stefania GessiEmail author
  • Pier Andrea Borea
Part of the The Receptors book series (REC, volume 34)


Adenosine receptors A1, A2A, A2B, and A3 are effector proteins triggered by the endogenous nucleoside adenosine to exert its numerous vital physiological effects, behaving like a guardian angel. This chapter offers an overview of the updated knowledge concerning the structure, distribution, and signal transduction of adenosine receptors. They are a family of G protein-coupled receptors widely distributed through the body, from central nervous system to peripheral organs, important and ubiquitous regulators of numerous cellular signaling. Their presence on every cell renders them an attractive opportunity for the pharmacological research and development of new drugs but also a challenge in the difficulty to produce tissue-selective ligands avoided of side effects. To aid this process, several efforts have been invested to reveal the molecular structure and the consequent mechanism of ligand binding of these receptors, and until now more than 30 structures have been published for the human A2A subtype. Finally, the principal adenosine receptor signaling pathways including adenylyl cyclase, phospholipase C, inositol triphosphate, diacylglycerol, phosphatidylinositol 3-kinase, and mitogen-activated protein kinases determining their effects on several transcription factors, such as hypoxia-inducible factor 1, cyclic AMP (cAMP)-responsive elements, nuclear factor-kB, and exchange protein directly activated by cAMP as the most relevant, are presented.


Adenosine receptors Signal transduction cAMP Distribution Kinases 


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Copyright information

© Springer Nature Switzerland AG 2018

Authors and Affiliations

  • Stefania Merighi
    • 1
  • Stefania Gessi
    • 1
    Email author
  • Pier Andrea Borea
    • 1
  1. 1.Department of Medical SciencesUniversity of FerraraFerraraItaly

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