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Updated: Jul 14, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Aza analogues of equol: novel ligands for estrogen receptor beta
Wuhong Chen1, Zhaohu Lin, Mengmeng Ning
1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai, China.
Abstract:
3-Aryl-tetrahydroquinolines, aza analogues of equol, are synthesized and evaluated for their binding properties to the estrogen receptors ERalpha and ERbeta. Several of these compounds exhibited binding selectivity for ER similar to that of genistein. Compounds 8c and 8d were found to have dual actions: antagonists for ERalpha and agonists for ERbeta in a yeast two-hybrid assay. These compounds have no estrogenic effects on the uterus and bone in vivo.
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