Encyclopedia of Molecular Pharmacology

Living Edition
| Editors: Stefan Offermanns, Walter Rosenthal

Adenosine Receptors

  • Kenneth A. JacobsonEmail author
Living reference work entry
DOI: https://doi.org/10.1007/978-3-030-21573-6_175-1
  • 52 Downloads

Synonyms

Definition

Extracellular adenosine acts through a class of G protein-coupled receptors (GPCRs), defined across mammalian species as A1, A2A, A2B, and A3ARs (adenosine receptors). Adenosine has a cytoprotective and allostatic role in the body, both in the periphery and in the central nervous system. Following binding of adenosine, or another naturally occurring agonist, the receptor interacts with heterotrimeric G proteins and β-arrestin to stimulate or inhibit downstream signaling cascades, or to induce receptor desensitization.

Basic Characteristics

The purine nucleoside adenosine, as a natural local modulator of cell action, increases the ratio of oxygen supply to demand, suppresses excessive inflammation, and promotes tissue protection against apoptosis or ischemic damage. ARs also have effects on proliferation and differentiation. Nearly every cell type in the body expresses one or more of these receptors, indicating the fundamental...

This is a preview of subscription content, log in to check access.

References

  1. Canas PM, Cunha RA, Agostinho P (2018) Adenosine receptors in Alzheimer’s disease. In: Borea P, Varani K, Gessi S, Merighi S, Vincenzi F (eds) the adenosine receptors. The receptors, vol 34. Humana Press, Cham.  https://doi.org/10.1007/978-3-319-90808-3_11CrossRefGoogle Scholar
  2. Chen J, Eltzschig H, Fredholm B (2013) Adenosine receptors as drug targets — what are the challenges? Nat Rev Drug Discov 12:265–286CrossRefGoogle Scholar
  3. Jacobson KA, Tosh DK, Jain S, Gao ZG (2019) Historical and current adenosine receptor agonists in preclinical and clinical development. Frontiers Cell Neurosci 13:124CrossRefGoogle Scholar
  4. Jarvis MF (2019) Therapeutic potential of adenosine kinase inhibition-revisited. Pharmacol Res Perspect 7(4):e00506.  https://doi.org/10.1002/prp2.506CrossRefPubMedPubMedCentralGoogle Scholar
  5. Jespers W, Schiedel AC, Heitman LH, Cooke RM, Kleene L, van Westen GJP et al (2018) Structural mapping of adenosine receptor mutations: ligand binding and signaling mechanisms. Trend Pharmacol Sci 39:75–89CrossRefGoogle Scholar
  6. Müller CE, Jacobson KA (2011) Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta Biomembr 1808:1290–1308CrossRefGoogle Scholar
  7. Pastor-Anglada M, Pérez-Torras S (2018) Who is who in adenosine transport. Front Pharmacol 9:627.  https://doi.org/10.3389/fphar.2018.00627CrossRefPubMedPubMedCentralGoogle Scholar
  8. Xiao C, Liu N, Jacobson KA, Gavrilova O, Reitman ML (2019) Physiology and effects of nucleosides in mice lacking all four adenosine receptors. PLoS Biol 17(3):e3000161.  https://doi.org/10.1371/journal.pbio.3000161CrossRefPubMedPubMedCentralGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg New York 2020

Authors and Affiliations

  1. 1.Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes Digestive and Kidney DiseasesNational Institutes of HealthBethesdaUSA