Figure 3.

The double effect of GRK2 inhibition in diabetic mice. In db/db mice, the treatment with KRX-C7, a selective inhibitor of GRK2, increases insulin sensitivity by affecting the insulin signaling cascade. Indeed, it induces the phosphorylation of IRS-1 and the activation of AKT and MAPK signaling. This induces the translocation of GLUT-4 to the plasma membrane and increases glucose uptake. Abbreviations: KRX-C7 = cyclic peptide inhibitor of GRK2; GLUT4 = Glucose Transporter type 4; IRS = Insulin Receptor Substrate; AKT = Protein kinase B; ERK = Extracellular signal-Regulated Kinase; NFkappaB = Nuclear Factor kappa-light-chain-enhancer of activated B cells.