Figure 4

Overall structure of lobeglitazone-bound PPARγ LBD. (a) Ribbon diagram of lobeglitazone-bound PPARγ LBD (salmon) with the SRC-1 coactivator peptide (grey). Lobeglitazone shown as a green stick model occupies LBP of PPARγ. The electron density for lobeglitazon in the mFo-DFc omit map is shown as a light teal-colored mesh (contoured at 2.5σ). The Cdk5-mediated phosphorylation site, Ser245, is represented by red sticks. (b) Close-up view of bound lobeglitazone in sticks with the mFo-DFc omit electron density map (contoured at 2.5σ). (c) Close-up view of interactions between PPARγ LBD and lobeglitazone. The view is 180° rotated from the orientation in (a). Hydrogen bonds are depicted by dashed lines and labeled with donor–acceptor distances in Å. Helix H7 has been omitted to show clear position of lobeglitazone. Cys285 is represented in sticks.