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. Author manuscript; available in PMC: 2012 Oct 1.
Published in final edited form as: Cell Res. 2011 Oct 11;22(4):746–756. doi: 10.1038/cr.2011.162

Figure 6. Functional correlation of the RU-486/ PPARγ interactions.

Figure 6

(A-D) Molecular determinants of the interaction between PPARγ with ligand RU-486. Overlays of the PPARγ-RU-486 structure (blue) with the PPARγ-rosiglitazone (gold) structure, where ligand RU-486 is in green and rosiglitazone is in purple. The hydrophobic interactions and hydrogen bonds are shown with lines and arrows, respectively. The potential hydrophobic interactions and hydrogen bonds, if the corresponding mutations are made as indicated in Figure 5, are shown in dashed lines and dashed arrows, respectively. The blue lines indicate the interactions between PPARγ and RU-486, while the gold lines indicate the interaction between PPARγ and rosiglitazone. (E) Effects of mutations of key PPARγ residues on its transcriptional activity in response to RU-486 in cell-based reporter gene assays. Cos7 cells were cotransfected with plasmids encoding full-length PPARγ or PPARγ mutants as indicated in the figure together with a PPRE luciferase reporter. The cells were treated with 1 μM RU-486 and rosiglitazone, respectively. The dashed line indicates the activation level of wild-type PPARγ by RU-486.