FIGURE 2.
Competitive binding assay of TOK-001 and abiraterone alcohol for the AR. A, competitive binding curve of TOK-001 and abiraterone alcohol for the T877A mutant AR in LNCaP cells. B–F, competitive binding curve of TOK-001 for the wild type AR (LAPC-4 (B)), mutant AR (LNCaP, T877A) (C)), (D–F) AR expressed in PC3 cells: wild type AR (PC3 AR-WT (D)), mutant W741C AR (PC3 AR-741C (E)), mutant W741L (PC3 AR-W741L (F)). In PC3 cells, the WT AR and mutant AR proteins were expressed by transient transfection, as described. Kc was determined by non-linear regression using the One-site fit Ki equation of the GraphPad Prism Software. Plotted are AR-bound counts (cpm) versus [17-HAS] (log [M]). The average kc ± S.D. (n = 3) is shown in the lower left corner of each graph.