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Mark Zylka, University of North Carolina at Chapel Hill
Adenosine A1 and A2 receptor agonists show promise as therapeutic agents for pain (reviewed in Zylka, TIMM, 2011, PMID: 21236731). A recent study by Liu et al., along with a previous study by this group (PMID: 21393508), report the high-resolution crystal structure of the adenosine A2 receptor bound to an agonist along with structural details of where sodium ions and lipids bind. Several potent and selective agonists of the A2A receptor exist. This new crystal structure could be used to refine the activity of agonists and develop allosteric modulators. Such compounds could be used to treat pain and other medical conditions.