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Example sentences for: serms

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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.
Moreover, these interactions were suppressed by SERMs (ICI, raloxifene and tamoxifen).
Provocative mechanistic connections have been made between the steroid hormone superfamily, including the SERMS and retinoids, and the TGF-β family of multifunctional growth factors [ 8].
It is plausible, therefore, that upregulation of endogenous TGF-β could contribute to the chemopreventive efficacy of SERMs and retinoids.
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.