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Updated: Feb 19, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Allosteric Induction of Estrogen Receptor Ligand Binding Domain Tetramerization by a Distinct Complete Estrogen
Emma C Fink1, Reena Chawla2, Govinda R Hancock1
1Department of Cancer Biology, Loyola University Chicago Stritch School of Medicine, Maywood, Illinois 60546, United States.
Abstract:
Complete estrogen receptor antagonists (CERANs) are effective against advanced estrogen receptor-positive (ER+) breast cancers, but current chemical scaffolds limit our ability to explore the full range of ER pharmacology. We report the synthesis of OP-1690 (2), a CERAN featuring a distinct unconstrained core. Structural and biophysical studies reveal that 2 uniquely promotes estrogen receptor alpha (ERα) ligand binding domain (LBD) tetramer formation, which goes beyond the conventional homodimer. This study shows how new CERAN scaffolds can reveal unrecognized mechanisms of action.
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