Figure 1. Schematic depicting varying mechanisms to block AR signaling in CRPC. (1) Abiraterone inhibits androgen biosynthesis by inhibiting CYP17A1. (2) Enzalutamide competitively antagonizes androgen binding to AR. (3) BET bromodomain inhibitors blocks AR (whether mutated/amplified) and BRD2/3/4 interaction, and co-recruitment to target gene loci as well as the activity and/or expression of the oncogenic transcription factors, including ETS fusions and MYC.