Binding affinity of different estrogens
• ESTRADIOL binds equally well to both ER-α and ER-β
• ESTRONE binds preferentially to ER-α
• ESTRIOL (postmenopausal estrogen) and genistein (Isoflavones) bind preferentially to ER-β
ER amounts ▼ decrease significantly after menopause
ESTRADIOL increases number of ER-α and AR receptors
- ESTRADIOL stimulates production of both ER-αreceptors and androgen receptors (Ars) - promoting a greater hormonal effect for estrogen and androgens;
- Also, even a low dose of the synthetic estrogen bisphenol A (prolific in our world and bodies today - see xenoestrogens) has the same effect as natural ESTRADIOL.
Richter CA, JA Taylor, RL Ruhlen, WV Welshons and FS vom Saal. 2007. ESTRADIOL and bisphenol a stimulate androgen receptor and estrogen receptor gene expression in fetal mouse prostate mesenchyme cells,. Environmental Health Perspectives, in press. Link
- Stimulation is blocked by estrogen receptor antagonists - E.g. PROGESTERONE , tamoxifen,
ESTRADIOL is a relatively potent androgen receptor (AR) binder;
Nakla AM, Romas NA, Rosner W. ESTRADIOL Activates the Prostate Androgen Receptor and Prostate-specific Antigen Secretion through the Intermediacy of Sex Hormone-binding Globulin March 14, 1997 The Journal of Biological Chemistry, 272, 6838-6841. Jbc Abstract
RichterCA, JA Taylor, RL Ruhlen, WV Welshons and FS vom Saal. 2007. ESTRADIOL and bisphenol a stimulate androgen receptor and estrogen receptor gene expression in fetal mouse prostate mesenchyme cells,. Environmental Health Perspectives, in press. Link
Leslie Baumann. Cosmetic Dermatology: Principles and Practice, Second EditionMcGraw Hill Professional,Apr 8, 2009
