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. Author manuscript; available in PMC: 2010 Sep 20.
Published in final edited form as: ACS Chem Biol. 2009 Jun 19;4(6):435–440. doi: 10.1021/cb900043e

Figure 1.

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.