Estrogen receptor β binds to and regulates three distinct classes of target genes

Abstract

Estrogen receptor β (ERβ) has potent antiproliferative and anti-inflammatory properties, suggesting that ERβ-selective agonists might be a new class of therapeutic and chemopreventative agents. To understand how ERβ regulates genes, we identified genes regulated by the unliganded and liganded forms of ERα and ERβ in U2OS cells. Microarray data demonstrated that virtually no gene regulation occurred with unliganded ERα, whereas many genes were regulated by estradiol (E2). These results demonstrated that ERα requires a ligand to regulate a single class of genes. In contrast, ERβ regulated three classes of genes. Class I genes were regulated primarily by unliganded ERβ. Class II genes were regu..