This study (Melatonin blocks the activation of estrogen receptor for DNA binding - PubMed) seems to show that melatonin hinders the action of estrogen-bound estrogen receptors.
"The present study shows that melatonin prevents, within the first cell cycle, the estradiol-induced growth of synchronized MCF7 breast cancer cells. By using nuclear extracts of these cells, we first examined the binding of estradiol-estrogen receptor complexes to estrogen-responsive elements and found that the addition of estradiol to whole cells activates the binding of the estrogen receptor to DNA whereas melatonin blocks this interaction. By contrast, melatonin neither affects the binding of estradiol to its receptor nor the receptor nuclear localization. Moreover, we also show that addition of estradiol to nuclear extracts stimulates the binding of estrogen receptor to DNA, but this activation is also prevented by melatonin."
In other words:
1) Melatonin does not prevent estradiol from binding to the estrogen receptor
2) Melatonin DOES, HOWEVER, interfere with the signaling mechanism mediated by the estrogen receptor which affects gene transcription.
This is analogous to how DHT derivatives like masteron appear to exert uniquely anti-estrogenic effects. They do this by not only suppressing estradiol production, but also by inhibiting estrogen-mediated gene transcription
Let's get some thoughts on this!
"The present study shows that melatonin prevents, within the first cell cycle, the estradiol-induced growth of synchronized MCF7 breast cancer cells. By using nuclear extracts of these cells, we first examined the binding of estradiol-estrogen receptor complexes to estrogen-responsive elements and found that the addition of estradiol to whole cells activates the binding of the estrogen receptor to DNA whereas melatonin blocks this interaction. By contrast, melatonin neither affects the binding of estradiol to its receptor nor the receptor nuclear localization. Moreover, we also show that addition of estradiol to nuclear extracts stimulates the binding of estrogen receptor to DNA, but this activation is also prevented by melatonin."
In other words:
1) Melatonin does not prevent estradiol from binding to the estrogen receptor
2) Melatonin DOES, HOWEVER, interfere with the signaling mechanism mediated by the estrogen receptor which affects gene transcription.
This is analogous to how DHT derivatives like masteron appear to exert uniquely anti-estrogenic effects. They do this by not only suppressing estradiol production, but also by inhibiting estrogen-mediated gene transcription
Let's get some thoughts on this!
