MIBE acts as antagonist ligand of both estrogen receptor α and GPER in breast cancer cells.

ABSTRACT:

Introduction

The multiple biological responses to estrogens are mainly mediated by the classical estrogen receptors ERα and ERβ, which act as ligand-activated transcription factors. ERα exerts a main role in the development of breast cancer; therefore, the ER antagonist tamoxifen has been widely used although its effectiveness is limited by de novo and acquired resistance. Recently, GPR30/GPER, a member of the seven-transmembrane G protein-coupled receptor family, has been implicated in mediating the effects of estrogens in various normal and cancer cells. In particular, GPER triggered gene expression and proliferative responses induced by estrogens and even ER antagonists in hormone-sensitive tumor cells. Likewise, additional ER ligands showed the ability to bind to GPER eliciting

SUBMITTER: Lappano R 

PROVIDER: S-EPMC3496129 | biostudies-literature | 2012 Jan

REPOSITORIES: biostudies-literature