Extended Data Figure 4.

D4A has a higher affinity for both mutant type AR (LNCaP cells) and wild-type AR (LAPC4 cells) than abiraterone (Abi) and bicalutamide (Bic) and inhibits AR chromatin occupancy better than Abi. a, Competition plots for D4A, Abi and Bic. b, Competition plots for unlabeled R1881 and D4A. Displacement of [³H]-R1881 is described in the Methods section. Experiments were performed with biological replicates (n = 3) and results are shown as mean ± s.d. c, D4A inhibition of AR chromatin occupancy is superior to Abi. LNCaP cells were treated with the indicated concentrations of DHT, D4A, Abi and enzalutamide (Enz) for 3h. AR chromatin occupancy for PSA, TMPRSS2 and FKBP5 was detected with ChIP. Experiments were performed with technical replicates (n = 3) and results are shown as mean ± s.d. All experiments were repeatedly independently at least 3 times.