Antiestrogens corepressors

Smith CL, Nawaz Z, O Malley BW (1997) Coactivator and corepressor regulation of the agonist/antagonist activity of the mixed antiestrogen, 4-hydroxytamoxifen. Mol Endocrinol 11 657... 

Fig. 8. Schematic representation of the ligand-induced changes in the confirmation of ER that lead to activities ranging from pure estrogenic (A) to pure antiestrogenic (D) effects. In addition to the ligand-induced changes in the three-dimensional structure of ER, the multiple interactions with cell-specific coactivators and corepressors determine the final activity of each ER-ligand complex in each cell type.

The antiestrogenic and some of the estrogen-iike actions of SERMs can be expiained by the different conformations of the ER-a compiexes attracting novei coactivators or corepressors (CoR) (Fig. 46.5) to moduiate estrogen action at different sites, in this modei, the receptor wouid be the same at each site, yet the coactivators and corepressors wouid be distributed differentiy at different targets (130). 

Smith CL, Nawaz Z, O Malley BW (1997) Coactivator and corepressor regulation of the agonist/antagonist activity of the mixed antiestrogen, 4-hydroxytamoxifen. Mol Endocrinol 11 657-666 Xu L, Lavinsky RM, Dasen JS, Flynn SE, Mclnemey EM, Mullen TM, Heinzel T, Szeto D, Korzus E, Kurokawa R et al (1998) Signal-specific co-activator domain requirements for Pit-1 activation. Nature 395 301-306... 

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