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Example sentences for: serms

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Control binding experiments performed in parallel confirmed that ERα bound to N-CoR in the presence of SERMs, and not estradiol (Fig.
ERα enhances AP-1 activity in response to estrogens, [ 28 29 ] but ERβ inhibits AP-1 activity in response to estrogens [ 29 30 31 ] . ERβ also completely suppresses ERα activity at the cyclin D1 promoter and even suppresses the activity of an ERα mutant that is selectively superactive at AP-1 sites and CREs [ 29 ] . Finally, ERβ shows a unique capacity to enhance AP-1 activity in response to selective estrogen receptor modulators (SERMs) such as raloxifene, tamoxifen and ICI 182,780/Faslodex (ICI) [ 30 31 32 ] . Together, these observations suggest that there are fundamental differences in the way that the ERs bind unspecified cofactors that modulate gene expression, and that some of these cofactors must play a role in differential ER activity at AP-1 sites.
SERMs such as tamoxifen can upregulate TGF-β production and activation by many cell types, including human breast cancer cell lines [ 12, 13, 14, 15].
Thus, ERβ binds the N-CoR C-terminal NR interacting region in the presence of agonists, but not SERMs, and does so in vitro and in mammalian cells.
The search is now on for agents with improved risk-benefit profiles, and for agents that will prevent the subclass of estrogen receptor-negative tumors, the incidence of which was unaffected by the SERMS.