TABLE 4.
Rate constants for raloxifene (RAL) binding to SULT2A1 (WT and MT)
| Enzyme | Enzyme species | kon | koff | Kd (koff/kon) |
|---|---|---|---|---|
| m−1 s−1 | s−1 | μm | ||
| MT | E○a | 3.5 (0.1)b × 105 | 0.43 (0.04) | 1.2 (0.1) |
| PAPS-E· | 3.3 (0.2) × 105 | 0.50 (0.01) | 1.5 (0.2) | |
| WT | E○ | 4.1 (0.1) × 105 | 0.47 (0.03) | 1.1 (0.1) |
| PAPS-E· | 2.2 (0.3) × 104 | 0.54 (0.03) | 25 (5) |
a (·) indicates Raloxifene binding sites.
b S.E. is given in parentheses.