AUTHOR=Pasquini Silvia , Contri Chiara , Cappello Martina , Borea Pier Andrea , Varani Katia , Vincenzi Fabrizio TITLE=Update on the recent development of allosteric modulators for adenosine receptors and their therapeutic applications JOURNAL=Frontiers in Pharmacology VOLUME=13 YEAR=2022 URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2022.1030895 DOI=10.3389/fphar.2022.1030895 ISSN=1663-9812 ABSTRACT=
Adenosine receptors (ARs) have been identified as promising therapeutic targets for countless pathological conditions, spanning from inflammatory diseases to central nervous system disorders, from cancer to metabolic diseases, from cardiovascular pathologies to respiratory diseases, and beyond. This extraordinary therapeutic potential is mainly due to the plurality of pathophysiological actions of adenosine and the ubiquitous expression of its receptors. This is, however, a double-edged sword that makes the clinical development of effective ligands with tolerable side effects difficult. Evidence of this is the low number of AR agonists or antagonists that have reached the market. An alternative approach is to target allosteric sites