Figure 5.

Effect of combining L203F and G286F on constitutive activity and aplaviroc efficacy. Shown as bar graphs is the ligand-independent activation of PI turnover (A) and inhibition of forskolin-induced cAMP accumulation (B) for CCR5 WT, [L203F]-, [G286F]-and [L203F;G286F]-CCR5 normalized to CCL3 E_max (A) or maximum level of forskolin-stimulated cAMP in untransfected cells (B). (C) CCL3 activation as well as the intrinsic effect of aplaviroc and aplaviroc-induced inhibition of CCL3 activation, normalized to CCL3 E_max. Data from both assays were obtained in COS-7 cells. Statistical significance was calculated using one-way anova, ***P < 0.001; ns, not significant; n = 3–25.