Table 3. Affinity (Kd) of identified estrogen receptors as a function of their cellular localization and the system in which they have been measured.
Nuclear | Membrane | |||
---|---|---|---|---|
Kd | Origin | Kd | Origin | |
ERα | 0.1 nM | in vitro synthesized human ERα [139] | 0.30 nM | ERα-GFP–transfected COS7 cells [44] |
0.283 nM | ERα–transfected CHO cells [205] | 0.287 nM | CHO cells [205] | |
ERβ | 0.6 nM | Clone 29, rat prostate cDNA library [140] | 0.38 nM | ERβ-GFP–transfected COS7 cells [44] |
0.6 nM | In vitro synthesized human ERβ [139] | 1.17 nM | CHO cells [205] | |
1.23 nM | ERβ–transfected CHO cells [205] | |||
ER-X | 1.6 nM | |||
GPR30 | 5.7 nM | GPR30-GFP–transfected COS7 cells [44] | ||
6.6 nM | GPR30-GFP–transfected COS7 cells [209] | |||
2.7 nM | ERα-/ERβ-/GPR30+-transfected SKBR3 cells [254] | |||
3.3 nM | ERα-/ERβ-/GPR30+-transfected (HEK)293 cells [254] | |||
E2-BSA | Membrane fraction: | |||
4.5 nM | Hypothalamus [204] | |||
8.7 nM | Olfactory bulbs [204] | |||
30.2 nM | Cerebellum [204] | |||
Abbreviations: ERα, estrogen receptor α ; ERβ, estrogen receptor β ; GFP , green fluorescent protein ; GPR30, G Protein Receptor 30 ; (HEK)293 cells, Human Embryonic Kidney cells; CHO cells; Chinese Hamster Ovary cells; COS7 cells, Monkey Kidney fibroblast; SKBR3 cells, Human Breast Cancer cells.