Discovery of a Potent
and Selective GPR120 Agonist
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Abstract
GPR120 is a receptor of unsaturated long-chain fatty
acids reported
to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory,
and anti-obesity effects and is therefore emerging as a new potential
target for treatment of type 2 diabetes and metabolic diseases. Further
investigation is however hindered by the lack of suitable receptor
modulators. Screening of FFA1 ligands provided a lead with moderate
activity on GPR120 and moderate selectivity over FFA1. Optimization
led to the discovery of the first potent and selective GPR120 agonist