Journal article

2-methoxyestradiol is an estrogen receptor agonist that supports tumor growth in murine xenograft models of breast cancer

TE Sutherland, M Schuliga, T Harris, BL Eckhardt, RL Anderson, L Quan, AG Stewart

Clinical Cancer Research | AMER ASSOC CANCER RESEARCH | Published : 2005


PURPOSE: 2-Methoxyestradiol (2MEO) is being developed as a novel antitumor agent based on its antiangiogenic activity, tumor cell cytotoxicity, and apparent lack of toxicity. However, pharmacologic concentrations of 2MEO bind to estrogen receptors (ER). We have therefore examined the ER activity of 2MEO. EXPERIMENTAL DESIGN: Estrogenic actions of 2MEO were evaluated by changes in gene expression of the ER-positive (MCF7) breast tumor cell line and, in vivo, estrogenicity was assessed in breast tumor xenograft models and by measuring endocrine responses in uterus and liver. RESULTS: In the ER-positive breast tumor cell line (MCF7), microarray experiments revealed that 269 of 279 changes in ge..

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