It has been shown recently that in addition to their classical role in desensitizing G protein coupled receptors (GPCR’s), beta-arrestins can act as signaling molecules independently and certain ligands (biased ligands) can selectively activate one pathway but not the other . Different biological responses have been observed with such beta-arrestin biased agonists, compared with traditional GPCR therapeutics designed to activate G-proteins. However, the lack of well characterized ligands for the beta-arrestin pathway demonstrates there is a need for effective screening methods to obtain selective therapeutics that could avoid the side effects of mediating G-protein signaling.
UC San Diego researchers have developed screening methods for beta-arrestin2 biased agonists that bind GPR120 and methods for treating inflammation via activation of a beta-arrestin2 dependent signaling pathway . Data obtained using a model compound to activate the GPCR suggests a novel role for this GPCR in modulating inflammatory responses through the beta-arrestin pathways. Model compounds investigated include DHA and EPA which do not activate the beta-arrestin1 pathway
Treatment of disorders involving inflammation including diabetes, obesity, arthritis, IBD, and neurodegeneration
Demonstration of anti-inflammatory response in in-vitro cellular assays.
|United States Of America||Issued Patent||8,987,332||03/24/2015||2009-028|
biomedical/inflammation (diabetes obesity neurodegeneration), research tools (screening assays)