Fig. 2

Overall structures of ligand-bound human estrogen receptor α ligand-binding domain complex. X-Ray crystal structures of human estrogen receptor α-ligand binding domain bound to E2 (left; PDB ID 1ERE [19]), 4-OH TAM (center; PDB ID 3ERT [21]) and GW (right; PDB ID 1R5K [26]) were illustrated using NGL software [20] on RCSB PDB website (http://www.rcsb.org/). These structures indicate the difference of helix (H) 12-relocation between three ligands. GW5638-induced H12 positioning increases surface hydrophobicity of ERα LBD, leading to ER instability