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Example sentences for: serms

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NRs generally interact with the corepressors N-CoR and SMRT either in the absence of ligand, or in the presence of receptor antagonists, and agonists promote corepressor release [ 4 ] . In this study, we demonstrated that ERβ binds to N-CoR in the presence of ER agonists such as estradiol and DES and the phytoestrogens genistein and coumestrol, but not in the presence of SERMs.
Control binding experiments performed in parallel confirmed that ERα bound to N-CoR in the presence of SERMs, and not estradiol (Fig.
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].
While the ER isoforms have contrasting effects on AP-1 activity in the presence of estrogens, ERα truncations that lack the NTD and ERβ both enhance AP-1 activity in the presence of SERMs [ 30 31 ] . Mutational analysis of ERα action at AP-1 sites suggests these effects may be related to N-CoR binding [ 39 ] , and we have proposed that SERM action at AP-1 sites may therefore involve contacts with corepressors [ 31 51 ] . The fact that ERα and ERβ show completely different ligand preferences of interaction with N-CoR suggests that the target for SERM activation at AP-1 sites may not be N-CoR in both cases.
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.