Possible targeting of G protein coupled receptors to manipulate inflammation in vivo using synthetic and natural ligands.
Cyclic AMP elevating Gs protein coupled receptors were considered for a long time to be immunosuppressive. One of these receptors, adenosine A(2A) receptor, was implicated in a physiological mechanism that down regulates inflammation and protects tissues from excessive immune mediated damage. Targeting of these receptors by selective agonists may lead to better protocols of anti-inflammatory treatments. At the same time inhibiting the Gs protein coupled mediated signalling with antagonists could be explored in studies of approaches to enhance inflammation and tissue damage. Enhancement of targeted tissue damage is highly desirable when it is cancerous tissue, while enhancement of inflammatory events might be desirable in the development of new vaccine adjuvants.
Kinsel
J F
JF
Sitkovsky
M V
MV
D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use; D019205:GTP-Binding Protein alpha Subunits, Gs / Q000378:metabolism*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000503:physiopathology*; D008024:Ligands; D051379:Mice; D043705:Receptor, Adenosine A2A / Q000502:physiology*
D058917:Adenosine A2 Receptor Antagonists; D000893:Anti-Inflammatory Agents; D008024:Ligands; D043705:Receptor, Adenosine A2A; D019205:GTP-Binding Protein alpha Subunits, Gs