Review of the Structural and Dynamic Mechanisms of PPARγ Partial Agonism

Figure 1

PPARγ domain organization. (a) Primary structure of PPARγ. (b) Crystal structure of the intact PPARγ-RXR heterodimer bound to PPRE DNA with agonist ligands retinoic acid and full agonist rosiglitazone. Proteins and DNA are shown as ribbons while ligands are shown as spheres. RXR is coloured red, the PPARγ ligand binding domain is coloured yellow, the PPARγ DNA binding domain is coloured green, the PPARγ hinge is coloured cyan, and the NCOA2 coactivator peptide is coloured blue. PDB: 3DZY [14].

(a)

(b)