The acute glucose lowering effect of specific GPR120 activation in mice is mainly driven by glucagon-like peptide 1
Fig 1
Structure of AZ13581837 and Metabolex-36 and specificity of the compounds for human and mouse GPR120 and human or mouse GPR40.
A) Chemical structure of AZ13581837 and B) Metabolex-36.C) Effect of AZ13581837 (squares) and Metabolex-36 (circles) on DMR response in CHO-hGPR120 (filled symbols) and CHO (open symbols). D) Activity in CHO-GPR40 cells for AZ13581837 (filled squares), Metabolex-36 (filled circles) and GW9508 (filled triangles). Activity in CHO-hGPR120 cells is shown as reference for AZ13581837 (open squares), Metabolex-36 (open circles) and GW9508 (open triangles). E) Cross species selectivity evaluated in CHO-mGPR120 cells using a DMR assay. Activity of AZ13581837 (squares) and Metabolex-36 (circles) on mouse GPR120 (filled symbols) compared to human GPR120 (open symbols). F) Cross species selectivity for GPR40 evaluated using a calcium mobilization assay. Effect of AZ13581837 (filled squares) and Metabolex-36 (filled circles) on mouse GPR40 with GW9508 (filled triangles) as reference. Activity in CHO-hGPR120 cells is shown as comparison for AZ13581837 (open squares) and Metabolex-36 (open circles). Data are shown as mean ± SEM run in duplicates or more and representative for two or more independent experiments.