Estrogen receptor-beta sensitizes breast cancer cells to the anti-estrogenic actions of endoxifen.

ABSTRACT:

Introduction

We have previously demonstrated that endoxifen is the most important tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). However, the relevance of ERβ in mediating endoxifen action has yet to be explored. Here, we characterize the molecular actions of endoxifen in breast cancer cells expressing ERβ and examine its effectiveness as an anti-estrogenic agent in these cell lines.

Methods

MCF7, Hs578T and U2OS cells were stably transfected with full-length ERβ. ERβ protein stability, dimer formation with ERα and expression of known ER target genes were characterized following endoxifen exposure. The ability of various endoxifen concentrations to block estrogen-induced

SUBMITTER: Wu X 

PROVIDER: S-EPMC3219188 | biostudies-literature | 2011 Mar

REPOSITORIES: biostudies-literature