TABLE 1.
RLAs of different estrogens to ERα and ERβ
The RLA of each ligand was calculated as the ratio of IC50 of 17β-E2 and IC50 of competitor, multiplied by 100. Each value is the mean ± S.D. of measurements obtained from three independent experiments. The ratios of RLA for ERβ/ERα are shown. A ratio greater than 1 indicates higher affinity for ERβ, and a ratio less than 1 indicates higher affinity for ERα. Numbers in brackets ([100] or [1]) are the base values on which the RLA values are calculated. A value of 100 represents a Kd = 0.2 nm for ERα and 0.5 nm for ERβ (18).
Ligand name | RLA |
RLA β/α | |
---|---|---|---|
ERα | ERβ | ||
17β-E2 | [100] | [100] | [1.0] |
E1 | 4.5 ± 0.7 | 4.0 ± 1.0 | 0.89 |
E3 | 6.8 ± 0.7 | 11.6 ± 0.6 | 1.7 |
EE2 | 194 ± 22 | 151 ± 27 | 0.78 |
17α-E2 | 13.7 ± 1.6 | 5.3 ± 1.8 | 0.39 |
DES | 290 ± 56 | 278 ± 54 | 0.96 |
DMS | 22.2 ± 4.3 | 237 ± 28 | 10.7 |
Meso-Hex | 314 ± 44 | 697 ± 74 | 2.2 |
dl-Hex | 4.4 ± 0.3 | 60.3 ± 5.3 | 13.7 |
Equ | 2.3 ± 0.2 | 3.2 ± 0.3 | 1.4 |
Eqn | 0.35 ± 0.04 | 2.0 ± 0.3 | 5.7 |
Gen | 0.06 ± 0.01 | 7.4 ± 0.5 | 123 |