Barlier, Céline et al.
Epigenetic dysregulations are linked to various diseases, including cancer. Among them, breast cancer is the second leading cause of cancer-related deaths in women with 50% of mortalities attributable to estrogen receptor-positive (ER+) tumors. Endocrine therapies targeting the Estrogen Receptor (ER) such as Tamoxifen, Fulvestrant and Aromatase inhibitors, are widely used in the clinic. Among these therapeutic agents, Fulvestrant has been shown to fully antagonize ER activity, primarily through the rapid degradation and elimination of ER from target tissues. However, recent findings indicate that ER, when engaged with Fulvestrant, retains the ability to translocate to the nucleus and bind DNA whereas appearing transcriptionally inert.
