Figure 4
Structural analysis of BM-3 and human CYP1A2. Model of EPA bound to BM-3 (A) and CYP1A2 (B). The gray surface indicates the binding cavity identified by SiteMap. EPA and heme are shown in green and red, respectively. The residues interacting with the carboxyl group of EPA are colored blue. Located behind the binding cavity, Ser122 (B) is hidden by the surface pocket. Insets in A and B show the enlarged view of the conformation of the metabolized position of EPA. (C) Lipidomic profiles of EPA incubation products from HEK293 cells transiently transfected with mock (white bar) or human CYP1A2 (black bar). Values represent the mean ± SEM; n = 3. *P < 0.05, **P < 0.01. (D) Production of 17,18-EpETE and 17,18-diHETE by HEK293 cells transiently transfected with human CYP1A2 (WT, T118A, S122A, or N312A). Values represent the mean ± SEM; n = 3. **P < 0.01. (E) HEK293 cells were transiently transfected as indicated. Cell lysates were prepared 24 h after transfection, and expression of CYP1A2 was analyzed by western blotting.
