Introduction Estrogens used in women's healthcare have been associated with increased
risks of venous thromboembolism (VTE) and breast cancer. Estetrol (E4), an estrogen …

Oestrogen receptor-α (ERα), a key driver of breast cancer, normally requires oestrogen for
activation. Mutations that constitutively activate ERα without the need for hormone binding …

Human breast cancers that exhibit high proportions of immune cells and elevated levels of
pro-inflammatory cytokines predict poor prognosis. Here, we demonstrate that treatment of …

Estrogen receptor alpha (ERα) is a ligand-dependent master transcriptional regulator and
key driver of breast cancer pathology. Small molecule hormones and competitive …

Efforts to improve estrogen receptor-α (ER)–targeted therapies in breast cancer have relied
upon a single mechanism, with ligands having a single side chain on the ligand core that …

Zearalenone (ZEN) is a mycoestrogenic polyketide produced by Fusarium graminearum and
other phytopathogenic members of the genus Fusarium. Contamination of cereals with ZEN …

The origin of ancient ligand/receptor couples is often analyzed via reconstruction of ancient
receptors and, when ligands are products of metabolic pathways, they are not supposed to …

Resistance to endocrine therapies remains a major clinical problem for the treatment of
estrogen receptor-α (ERα)-positive breast cancer. On-target side effects limit therapeutic …

Sex hormones play important roles in the onset and progression of several cancers, such as
breast, ovarian, and prostate cancer. Although drugs targeting sex hormone function are …

Multi-target compounds have become increasingly important for the development of safer
and more effective drug candidates. In this work, we devised a combined ligand-based and …