Figure 4.

In vitro activity of regioisomeric GLP1–siRNA conjugates. (A) Activation of GLP1R was measured with a CRE/Luciferase reporter assay in BHK cells expressing human GLP1R. EC50 values are presented as mean and 95% CI of n = 3 independent experiments. (B) Fold change in EC50 compared to free peptide. (C) Gene knockdown dose-response with GLP1–siRNA conjugates measured by RT-qPCR. Data points represents mean and SD of n = 5 biological replicates. (D) Gene knockdown with internally modified GLP1–siRNA library at three different concentrations (10 pM, 100 pM and 10 nM) measured by RT-qPCR. Data presented as mean and SD of n = 3 biological replicates.