Structural basis of Resolvin mediated GPCR signalling


Figure from M.G. Duvall, B.D. Levy / European Journal of Pharmacology 785 (2016) 144–155

Resolvins are omega-3 lipid derived signalling molecules. Unlike anti-inflammatory drugs like Ibuprofen, that try to block pro-inflammatory signalling inside the cell, Resolvins have the ability to “switch-off” these signals at their source, thereby leading to a natural resolution of inflammation. They achieve this by binding to specific G-protein coupled receptors (GPCRs), the cellular “inbox” for external messages, that then relay these messages to the inside of the cell. GPCRs play a central role in mediating health and disease, and it is currently estimated that up to 50% of drugs currently approved drugs target these proteins. Understanding how Resolvin signalling is mediated by this mechanism has therapeutic implications for all diseases where a state of chronic inflammation is involved, from arthritis to depression.