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ACS Pharmacol Transl Sci. 2021 Jan 21;4(1):314-326. doi: 10.1021/acsptsci.0c00195. eCollection 2021 Feb 12.

Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor.

ACS pharmacology & translational science

Giuseppe Deganutti, Kerry Barkan, Barbara Preti, Michele Leuenberger, Mark Wall, Bruno G Frenguelli, Martin Lochner, Graham Ladds, Christopher A Reynolds

Affiliations

  1. Centre for Sport, Exercise and Life Sciences, Faculty of Health and Life Sciences, Coventry University, Alison Gingell Building, Coventry CV1 5FB, U.K.
  2. Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge, CB2 1PD, U.K.
  3. Institute of Biochemistry and Molecular Medicine, University of Bern, 3012 Bern, Switzerland.
  4. School of Life Sciences, University of Warwick, Gibbet Hill Road, Coventry CV4 7AL, U.K.

PMID: 33615181 PMCID: PMC7887845 DOI: 10.1021/acsptsci.0c00195

Abstract

Despite being among the most characterized G protein-coupled receptors (GPCRs), adenosine receptors (ARs) have always been a difficult target in drug design. To date, no agonist other than the natural effector and the diagnostic regadenoson has been approved for human use. Recently, the structure of the adenosine A1 receptor (A

© 2021 American Chemical Society.

Conflict of interest statement

The authors declare no competing financial interest.

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