Figure 7.
Type V compounds outcompete LPA in the ATX tunnel, abolishing allostery. (A,B) LPA activation in the absence or presence of 22 or 23. (Left panels) Dose-dependent LPA-related increase in activity of 20 nM ATX pre-incubated with the compounds in a concentration that still allowed residual activity (>50% at the highest inhibitor concentration). (Right panels) Increase of ATX activity with respect to the compound-free control; the data displayed represent the mean value of triplicate measures ± standard error of the mean (SEM).