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Binding and inhibition studies of WT and the V366M mutant of CYP17A1.
| CYP17A1_WT | CYP17A1_V366M | |
|---|---|---|
| Binding studies | Kd (nM) | Kd (nM) |
| Binding of PROG | 163 ± 29 | 287 ± 35 |
| Binding of PREG | 62 ± 17 | 92 ± 15 |
| Binding of 17OH-PREG | 142 ± 38 | - |
| Binding of Abiraterone | 85 ± 23 | - |
| Inhibition studies | IC50 (µM) | IC50 (µM) |
| Inhibition of PROG 17α-hydroxylation by Abiraterone | 0.04 ± 0.01 | - |
| Inhibition of PROG 17α-hydroxylation by 17OH-PREG | 1.7 ± 0.2 | - |
| Inhibition of PROG 17α-hydroxylation by PREG | 0.9 ± 0.15 | 1.4 ± 0.2 |
