1994/06/03 by Shlomit Halachmi, Emily Marden, Glover Martin +3 · 8 citations
Biochemistry, Genetics and Molecular Biology · Medicine · #Estrogen and related hormone effects #Inflammatory mediators and NSAID effects #Glutathione Transferases and Polymorphisms
paper · doi:10.1126/science.8197458
openalex publication_date 1994/06/03 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/23
The estrogen receptor is a transcription factor which, when bound to estradiol, binds DNA and regulates expression of estrogen-responsive genes. A 160-kilodalton estrogen receptor-associated protein, ERAP160, was identified that exhibits estradiol-dependent binding to the receptor. Mutational analysis of the receptor shows that its ability to activate transcription parallels its ability to bind ERAP160. Antiestrogens are unable to promote ERAP160 binding and can block the estrogen-dependent interaction of the receptor and ERAP160 in a dose-dependent manner. This evidence suggests that ERAP160 may mediate estradiol-dependent transcriptional activation by the estrogen receptor. Furthermore, the ability of antiestrogens to block estrogen receptor-ERAP160 complex formation could account for their therapeutic effects in breast cancer.