Beta-Arrestin Biased GPCR Agonists for Inflammation and Metabolic Disease

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


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 themselves. Thus, it is now widely held that GPCR’s are able to signal through parallel G-Protein and beta-arrestin pathways. Next generation GPCR therapeutics will be advanced by fine-tuning the actions along these pathways.

GPCR ligands that preferentially activate the latter pathway are called beta-arrestin “biased” agonists. Different biological responses have been observed with such beta-arrestin biased agonists, compared with traditional GPCR therapeutics designed to activate G-proteins.

Technology Description

UC San Diego researchers have developed screening methods for beta-arrestin biased agonist of a known GPCR. 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. Beta-arrestin biased agonists are expected to avoid the side effects mediated by G-protein signaling.


Treatment of 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


  • Olefsky, Jerrold M.

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