Article
Differential SERM effects on corepressor binding dictate ERalpha activity in vivo.
The Journal of biological chemistry - 28 Feb 2003
Webb Paul, Nguyen Phuong, Kushner Peter J
Abstract excerpt
Selective estrogen receptor modulators (SERMs) show differential effects upon ERalpha activation function 1 (AF-1). Tamoxifen allows strong ERalpha AF-1 activity, whereas raloxifene allows less and ICI 182,780 (ICI) allows none. Here, we show that blockade of corepressor histone de-acetylase (HDAC) activity reverses the differential inhibitory effect of SERMs upon AF-1 activity in MCF-7 cells. This suggests that...
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