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Updated: Jan 1, 2026

Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay
Published on: June 7, 2020
Constrained phytoestrogens and analogues as ERbeta selective ligands
Chris P Miller1, Michael D Collini, Heather A Harris
1Chemical Sciences, Wyeth Research, 500 Arcola Road, PA 19426, Collegeville, USA.
Abstract:
A new series of ERbeta (ERbeta) selective ligands has been prepared. One of the compounds 6, structurally related to the phytoestrogen apigenin 4, displays a binding preference for ERbeta over ERalpha of over 40-fold. In addition to its binding selectivity, 6 was able to potently induce metallothionein (an ERbeta specific response in human SAOS-2 cells) while demonstrating low potency in an ERalpha dependant ERE-tk luciferase assay in MCF-7 cells. Such receptor and cell selectivity could make 6 a useful molecular probe for better understanding the role of ERbeta in mammalian physiology.
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