Figure 1.

Schematic representation of the current understanding of ERα regulation of epigenetic modifications of histones. ERα–mediated transcription involves coordinated interactions of ERα with acetylases and deacetylases, methylases and demethylases. Ligand stimulation uniquely modulates ERα interactions with histone modifying enzymes. In addition, estrogen signaling has the potential to activate extranuclear signaling that activates several kinase cascades that either directly modifies histone tails or indirectly influence functions and/or recruitment of histone modifying enzymes. Deregulation of ERα-mediated epigenetic signaling will have implications in hormonal tumor progression and therapy resistance.