Article
The estrogen receptor antagonist ICI 182,780 can act both as an agonist and an inverse agonist when estrogen receptor α AF-2 is modified.
Proceedings of the National Academy of Sciences of the United States of America - 21 Jan 2014
Movérare-Skrtic Sofia, Börjesson Anna E, Farman Helen H, Sjögren Klara, Windahl Sara H, Lagerquist Marie K, Andersson Annica, Stubelius Alexandra, Carlsten Hans, Gustafsson Jan-Åke, Ohlsson Claes
Abstract excerpt
The bone-sparing effect of estrogen is primarily mediated via estrogen receptor (ER) α, which stimulates target gene transcription through two activation functions (AFs), AF-1 in the N-terminal and AF-2 in the ligand-binding domain. It was recently demonstrated that the ER antagonist ICI 182,780 (ICI) acts as an ER agonist in uterus of mice with mutations in the ERα AF-2. To evaluate the estrogen-like effects of...
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