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. Author manuscript; available in PMC: 2017 Dec 27.
Published in final edited form as: Biochemistry. 2017 Dec 12;56(51):6700–6712. doi: 10.1021/acs.biochem.7b01025

Figure 4.

Figure 4

Binding and metabolism studies of DOX and 7-de-aDOX. (A-B) Fluorescence polarization measurements of DOX (A) and 7-de-aDOX (B) binding to CYP2J2. Both DOX and 7-de-aDOX demonstrate one-site binding (eq 1). Binding was repeated in the presence of 60 μM ebastine (EBS) or 100 μM AA. DOX data in the presence of EBS or AA fit to a competitive binding model and 7-de-aDOX is fitted to eq 1 (no inhibition). For all experiments, [DOX] and [7-de-aDOX] = 1 μM. (C) EBS metabolism in the presence of DOX, 7-de-aDOX, and a 50:50 mixture of DOX:7-de-aDOX. DOX data fit to eq S1 and 7-de-aDOX data is linear. The theoretical fit based on the linear combination of DOX and 7-de-aDOX is shown as a grey, dashed line to demonstrate the closeness of the theoretical fit to the experimental fit. Concentrations of anthracyclines represent the total amount of anthracyclines present. Error represents ± SEM of 3 experiments.