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. 2012 Sep 28;26(11):1836–1846. doi: 10.1210/me.2012-1222

Fig. 1.

Fig. 1.

Structures of AR antagonists and homology model of AR in antagonist conformation. A, Structures of DHT, current AR antagonists, and the chemotype A chemical scaffold. In A61, R1 and R3 are Cl. In A89, R1 and R4 are Cl, and R3 is O-CH2-CH3. B, AR LBD in the agonist conformation and the refined homology model of AR LBD in an antagonist conformation, which features marked displacement of helix 12. These conformations superimpose to approximately 3.6 Å. C, Structure of DHT-liganded AR LBD and predicted structure of the chemotype A compound A61-liganded AR. Structures are rotated approximately 90° along the vertical axis compared with B. The right panel is a close-up of the A61-liganded AR LBD.