Article
An antiestrogen-responsive estrogen receptor-alpha mutant (D351Y) shows weak AF-2 activity in the presence of tamoxifen.
The Journal of biological chemistry - 1 Dec 2000
Webb P, Nguyen P, Valentine C, Weatherman R V, Scanlan T S, Kushner P J
Abstract excerpt
Antiestrogens, including tamoxifen and raloxifene, block estrogen receptor (ER) action by blocking the interactions of an estrogen-dependent activation function (AF-2) with p160 coactivators. Although tamoxifen does show some agonist activity in the presence of ERalpha, this stems from a distinct constitutive activation function (AF-1) that lies within the ERalpha N terminus. Previous studies identified a...
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