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Example sentences for: serms
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Moreover, these interactions were suppressed by SERMs (ICI, raloxifene and tamoxifen).
The PGC-1 related protein PERC also binds ERα preferentially, and potentiates ERα activity more strongly than that of ERβ [ 38 ] . We recently observed that ERα binds the C-terminal NR interacting regions of N-CoR and SMRT in the presence of SERMs but not estrogens [ 39 ] . In this study, we report that ERβ interactions with N-CoR and SMRT are promoted by agonists and inhibited by SERMs.
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.
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.
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.
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