Figure 5: EE2 and TNC bind cooperatively to PXR. | Nature Communications

Figure 5: EE2 and TNC bind cooperatively to PXR.

From: Synergistic activation of human pregnane X receptor by binary cocktails of pharmaceutical and environmental compounds

Figure 5

(a) Inhibition of FRET between fluorescein-labelled PXR ligand and recombinant GST-PXR by SR12813, TNC and EE2, alone or in combination. Results are expressed as the signal from the fluorescein emission divided by the terbium signal to provide a TR-FRET emission ratio. Data are the mean (±s.e.m.) from three separate experiments. (b-f) Isothermal titration calorimetry (ITC) characterization of PXR interaction with EE2 and TNC. Ligands were titrated either independently (b,c), after pre-incubating the receptor with EE2 (d) or TNC (e), or simultaneously (f). In b–f, representative thermograms (upper row) and corresponding binding isotherms (lower row) are shown. Kd values are expressed as the mean of two independent experiments.

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