Figure 7. Schematic depicting the identification and characterization of a novel GLP-1R-biased agonist.

Using an autocrine-based system coupled to FACS, we screened large, diverse, combinatorial peptide libraries and identified P5, a potent and selective G-protein-biased GLP-1R agonist. P5 displayed a decreased insulinotropic effect, yet significantly improved glucose tolerance and insulin responsiveness by promoting white adipocyte tissue hyperplasia.