Figure 1
Multiple FDA-approved compounds inhibit the phosphatase activity of PRL proteins. (a) Validation of drugs that were positive hits in the initial FDA-drug screen and significantly reduced PRL phosphatase activity across multiple tests. The FDA-approved drug Dexamethasone, which has no effect on PRL-3 phosphatase activity, was used as a negative control (- CTL). (b) ABT-199 demonstrated selectivity in inhibiting PRL-2. (c) Validation of PRL-3 specific inhibitors. All assays were run at a final PRL protein concentration of 2.5 µM, a drug concentration of 40 µM, and DiFMUP concentration at the previously reported KM of the protein. Bars represent the average phosphatase activity of the initial screen plus two additional independent experiments, in triplicate. Error bars represent standard deviation. *p < 0.05, **p < 0.001, ***p < 0.0001 by either two-way ANOVA with Dunnet’s correction (a) or one-way ANOVA with Tukey’s HSD (b, c).
