This technology includes compounds that are selective agonists of the A3 receptor for the treatment of various disorders such as cancer and autoinflammatory diseases. Structurally, these compounds extend the class of (N)-methanocarba derivatives that are selective agonists of the A3 receptor.
The discovery could be used in either a therapeutic or diagnostic mode. Other A3 agonists are in advanced clinical trials for treatment of various disorders such as hepatocellular carcinoma, autoimmune inflammatory diseases, and other conditions.
This class of compounds produced full agonists of the human A3AR of nanomolar affinity that were consistently highly selective >1000-fold vs. A1AR and A2AAR.