Article
Raloxifene and ICI182,780 increase estrogen receptor-alpha association with a nuclear compartment via overlapping sets of hydrophobic amino acids in activation function 2 helix 12.
Molecular endocrinology (Baltimore, Md.) - 1 Apr 2007
Lupien Mathieu, Jeyakumar M, Hébert Elise, Hilmi Khalid, Cotnoir-White David, Loch Caroline, Auger Anick, Dayan Guila, Pinard Geneviève-Anne, Wurtz Jean-Marie, Moras Dino, Katzenellenbogen John, Mader Sylvie
Abstract excerpt
The basis for the differential repressive effects of antiestrogens on transactivation by estrogen receptor-alpha (ERalpha) remains incompletely understood. Here, we show that the full antiestrogen ICI182,780 and, to a lesser extent, the selective ER modulator raloxifene (Ral), induce accumulation...
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