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. 2022 Apr 20;65(8):6338–6351. doi: 10.1021/acs.jmedchem.2c00368

Figure 7.

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).