Figure 3.

Crystal Structures of Ternary Complexes of PPARα-LBD, Ligand, and SRC1 Coactivator Peptide

(A) Ternary complexes with intrinsic fatty acid (iFA), GW7647, or EPA obtained by co-crystallization.

(B) Ternary complexes with pemafibrate obtained using soaking with iFA/SRC1-bound crystals.

(C) Ternary complexes with clofibric acid or fenofibric acid obtained by co-crystallization of the delipidized proteins. Both fibrates have two binding sites in Arm I and Arm II/X.

(D) Ternary complexes with bezafibrate obtained by soaking with clofibric acid/SRC1-bound crystals.

SRC1 peptides (magenta) and helices 12 (red) are indicated by arrows and arrowheads. The electron density is shown in the mesh by FEMs contoured at 1.0σ. PDB identities and resolutions are labeled, and water molecules are presented as cyan spheres.