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Updated: Aug 17, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Potent estrogen receptor ligands based on bisphenols with a globular hydrophobic core
Yasuyuki Endo1, Tomohiro Yoshimi, Kiminori Ohta
1Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, Komatsushima, Aoba-ku, Sendai, Japan. yendo@tohoku-pharma.ac.jp
Abstract:
Candidate estrogen receptor (ER) ligands with two phenolic residues on a three-dimensional hydrophobic core structure (carborane, bicyclo[2.2.2]octene, or adamantane) were synthesized and biologically evaluated. The biological properties of the ligands were markedly dependent on the nature of the hydrophobic core structure. Bis(4-hydroxyphenyl)-o-carborane (6) was a partial agonist/antagonist for ER. 1,2-Bis(4-hydroxyphenyl)bicyclo[2.2.2]octene (10) exhibited potent agonist activity for ER, even though the two phenolic groups are located similarly to those of 6.
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