Figure 1.
Cartoon representation of traditional vs. CBI antagonism of a nuclear receptor. (a) Conformation of agonist-bound nuclear receptor ligand binding domain (NR-LBD) with helix 12 (α12) forming part of the steroid receptor coactivator (SRC) binding site. (b) Conformation of antagonist-bound NR in which helix 12 occupies the SRC binding site, disrupting the NR/SRC interaction indirectly. (c) Conformation of agonist-bound NR in which a CBI occupies the SRC binding site, disrupting the NR/SRC interaction directly.