Beta-Arrestin Biased GPCR Agonists for Inflammation and Metabolic Disease

Tech ID: 20932 / UC Case 2009-028-0

Background

 

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.

Technology Description

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

Applications

Treatment of disorders involving inflammation including diabetes, obesity, arthritis, IBD, and neurodegeneration

State Of Development

Demonstration of anti-inflammatory response in in-vitro cellular assays.

Patent Status

Country Type Number Dated Case
United States Of America Issued Patent 8,987,332 03/24/2015 2009-028
 

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Inventors

  • Olefsky, Jerrold M.

Other Information

Keywords

biomedical/inflammation (diabetes obesity neurodegeneration), research tools (screening assays)

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