Table 1.
Relative initial activities of wild-type and chimeric KshA1 with a range of steroid substrates
| Steroid substrated | Relative initial KSH activitye |
|||||
|---|---|---|---|---|---|---|
| A1c | A1A5β | A1A5loop | A1A5β201-210 | A1D242W | A1A5TG | |
| 4-Androstene-3,17-dione (AD) | 100 | 100 | 100 | 100 | 100 | 100 |
| 1,4-Androstadiene-3,17-dione (ADD) | 244 ± 24 | 132 ± 9a | 171 ± 10a | 149 ± 3a | 307 ± 28 | 274 ± 22 |
| 4-Androstene-17β-ol-3-one (testosterone) | 158 ± 14 | 144 ± 6 | 191 ± 20 | 117 ± 8a | 205 ± 26 | 193 ± 17a |
| 4-Pregnene-3,20-dione (progesterone) | 372 ± 59 | 213 ± 22a | 294 ± 30 | 231 ± 9a | 499 ± 91 | 468 ± 34a |
| 19-Nor-4-androstene-3,17-dione (nordion) | 24 ± 6 | 19 ± 5 | 24 ± 5 | 18 ± 5 | 23 ± 9 | 23 ± 5 |
| 1-(5α)-Androstene-3,17-dione | 23 ± 4 | 22 ± 3 | 25 ± 5 | 13 ± 1 | 19 ± 4 | 14 ± 5 |
| 5α-Androstane-3,17-dione | 12 ± 10 | — | 10 ± 1 | 5 ± 1 | 11 ± 2 | 12 ± 5 |
| 5β-Androstane-3,17-dione | 19 ± 4 | 8 ± 5 | 6 ± 1a | 5 ± 2a | 13 | 8 ± 2a |
| 5-Cholestene-3β-ol (cholesterol)b | — | — | — | — | — | — |
| 5α-Androstane-17β-ol-3-one (stanolon) | — | 7 ± 3a | 5a | 4 ± 1a | 17 ± 2a | 11 ± 4a |
| 3α-Hydroxy-5α-pregnane-20-oneb | — | — | — | — | — | — |
| 11β-Hydrocortisone | — | 7 ± 5a | 7 ± 1a | 15 ± 4a | 13 ± 3a | 10 ± 3a |
| 3β-Hydroxy-5α-androstane-17-one | — | — | — | — | — | — |
| 23,24-Bisnorcholesta-4-ene-22-oic acid (4-BNC) | 548 ± 63 | 177 ± 36a | 241 ± 12a | 229 ± 24a | 704 ± 141 | 953 ± 137a |
| 9α-Hydroxy-4-androstene-3,17-dione (9OHAD) | — | — | — | — | — | — |
a
P < 0.02 (analysis of variance).
b
The steroid concentration is 25 μM due to low solubility.
c
Data taken from Petrusma et al. (22).
d
For chemical structures of steroids used in this study, see Fig. S1 in the supplemental material.
e
Relative KSH activities (with standard deviations) compared to activity with AD, which is set at 100% (Table 4). Steroid substrates were tested at a concentration of 200 μM. —, no initial KSH activity detectable.