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A 155-plex high-throughput in vitro coregulator binding assay for (anti-)estrogenicity testing evaluated with 23
Si Wang1, René Houtman, Diana Melchers
1Division of Toxicology, Wageningen University and Research Centre, Wageningen, The Netherlands. si.wang@wur.nl
ALTEX
|May 14, 2013
Summary
This study developed an in vitro estrogenicity test using coregulator interactions with estrogen receptor alpha. The assay accurately predicts in vivo potencies and distinguishes between estrogen receptor agonists and antagonists, aiding animal testing replacement.
Area of Science:
- Endocrinology
- Toxicology
- Biochemistry
Background:
- In vitro methods are needed to replace animal testing for estrogenicity assessment.
- Estrogen receptor alpha (ERα) plays a key role in mediating estrogenic effects.
- Coregulator interactions with ERα are critical for transcriptional regulation.
Purpose of the Study:
- To develop and validate an in vitro assay for assessing (anti-)estrogenicity.
- To evaluate the correlation between in vitro ERα-coregulator binding and in vivo estrogenic potency.
- To determine if the assay can differentiate between ER agonists and antagonists.
Main Methods:
- Utilized a PamChip® array to assess ligand-modulated coregulator interactions with ERα.
- Determined relative estrogenic potencies based on ERα binding to coregulator peptides.
- Compared in vitro potency predictions with results from the in vivo uterotrophic assay.
Main Results:
- In vitro estrogenic potencies predicted by 57 coactivators strongly correlated with in vivo potencies (R² ≥ 0.85 for 30 coactivators).
- The assay successfully distinguished ER agonists from ER antagonists, with distinct profiles for selective estrogen receptor modulators like tamoxifen.
- A high goodness of fit (≥ 0.90) was observed for compounds with clear E2 dose-dependent responses.
Conclusions:
- The ERα-coregulator binding assay is a reliable in vitro method for predicting estrogenic potency.
- This assay can differentiate between ER agonists and antagonists, crucial for comprehensive estrogenicity testing.
- Integration into a test panel with other in vitro assays will support the replacement of animal testing for (anti-)estrogenic effects.
