The PPAR Ω Pocket: Renewed Opportunities for Drug Development

Figure 1

Structural overview of the PPAR/RXR heterodimer. AF-1: ligand-independent activation function 1; DBD: DNA-binding domain; LBD: ligand-binding domain; AF-2: activation function 2; H12: helix 12; SRC1: steroid receptor coactivator 1; DR1: direct repeat 1; CTE: carboxy-terminal extension. (a) Schematic overview of the domains in PPAR/RXR. (b) A molecular surface representation of the structure of the PPARγ:RXRα heterodimer bound to rosiglitazone (magenta spheres), 9-cis-retinoic acid (not visible), two peptides derived from SRC1, and a DNA fragment. The DNA fragment is shown as a molecular surface (C, grey; O, red; N, blue; P, orange), extended with a cartoon representation (black). The structural data was taken from PDB ID: 3DZY [12] and presented with PyMOL (ver. 1.8.4.0) [13, 14].

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