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. 2016 Oct 31;3(1):34–44. doi: 10.1021/acsinfecdis.6b00078

Figure 4.

Figure 4

PfProRS inhibition dose response: inhibition of PfProRS enzyme activity at various concentrations of glyburide (blue), halofuginone (green), and TCMDC-124506 (orange). Lines are fitted to Hill equation with a slope = 1, and the calculated IC50 values for the compounds in this assay are PfProRS for 34 μM glyburide, 0.28 μM halofuginone, and 73 μM TCMDC-124506 and HsProRS for >700 μM glyburide, 2.13 μM halofuginone, and >700 μM TCMDC-124506. Compounds were counter-screened against HsProRS to determine specificity. Enzyme activity was determined by luciferase ATP depletion assay (75 nM ProRS enzyme, 60 μM proline, 6 μM ATP, and 400 μg/mL yeast tRNA were incubated for 2 h at 37 °C). Inhibition values shown on the graph are the average of three data points.