tug-891 and Diabetes-Mellitus--Type-2

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.

Topics: Biphenyl Compounds; Cell Survival; Cinnamates; Diabetes Mellitus, Type 2; Glucagon-Like Peptide 1; HEK293 Cells; Humans; Magnetic Resonance Spectroscopy; Mass Spectrometry; Molecular Structure; Phenylpropionates; Receptors, G-Protein-Coupled; Structure-Activity Relationship