Jacobson, Kenneth (NIDDK)
Novel A3 adenosine antagonists available for licensing. A3 receptors are particularly highly expressed in inflammatory cells, making it a potentially desirable target for inflammatory diseases. This technology relates to highly specific antagonists and partial agonists of A3 adenosine receptors, which are negatively coupled to adenylate cyclase and have been broadly implicated in inflammation, cardiovascular disease, endocrine conditions and cancer. Further, A3 adenosine receptors have been implicated in asthma and glaucoma.
- There are four known subtypes of adenosine receptors (A1, A2A, A2B, and A3). All are positively or negatively linked to cAMP, but have different distributions and different therapeutic potentials. In particular, the use of A1 and A2 selective ligands has been limited by the ubiquity of expression of the receptors throughout the body and the resultant side effects. On the other hand, high levels of A3 receptor expression are limited to the CNS, testes, and the immune system. Thus, A3 receptors represent a potentially highly specific target for treating related diseases.