Figure. 4: Nateglinide is a balanced agonist whereas AG-30/5C is a G protein -biased agonist for MRGPRX4.
(A) Untransfected (HTLA) and stably transfected HTLA-MRGPRX4-Tango (HTLA-MRGPRX4) cells were incubated with anti-FLAG-PE antibody and receptor expression was determined by flow cytometry. A representative overlay histogram of MRGPRX4 expression is shown. (B) Effects of nateglinide (30 μM), AG-30/5C (10 μM), compound 48/80 (30 μg/mL) on β-arrestin-mediated gene expression was determined as described in Figure 3. (C) Representative Ca2+ measurements traces in response to high concentrations of nateglinide (30 μM), AG-30/5C (10 μM) and compound 48/80 (30 μg/mL) are shown. All data points for the Tango assay are expressed as a mean ± SEM of three experiments. Statistical significance was determined by non-parametric t-Test and two way ANOVA (P value<.05). *** indicates P value<.001,** indicates P value <.01 and * indicates P value <.05.