The Estrogen Receptor Relative Binding Affinities of 188 Natural and Xenochemicals: Structural Diversity of Ligands

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2000
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Ranked #81 of 123 articles by views in toxicological sciences : an official journal of the society of toxicology

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Abstract
We have utilized a validated (standardized) estrogen receptor (ER) competitive-binding assay to determine the ER affinity for a large, structurally diverse group of chemicals. Uteri from ovariectomized Sprague-Dawley rats were the ER source for the competitive-binding assay. Initially, test chemicals were screened at high concentrations to determine whether a chemical competed with [3H]-estradiol for the ER. Test chemicals that exhibited affinity for the ER in the first tier were subsequently assayed using a wide range of concentrations to characterize the binding curve and to determine each chemical's IC50 and relative binding affinity (RBA) values. Overall, we assayed 188 chemicals, covering a 1 × 106-fold range of RBAs from several different chemical or use categories, including steroidal estrogens, synthetic estrogens, antiestrogens, other miscellaneous steroids, alkylphenols, diphenyl derivatives, organochlorines, pesticides, alkylhydroxybenzoate preservatives (parabens), phthalates, benzophenone compounds, and a number of other miscellaneous chemicals. Of the 188 chemicals tested, 100 bound to the ER while 88 were non-binders. Included in the 100 chemicals that bound to the ER were 4-benzyloxyphenol, 2,4-dihydroxybenzophenone, and 2,2′-methylenebis(4-chlorophenol), compounds that have not been shown previously to bind the ER. It was also evident that certain structural features, such as an overall ring structure, were important for ER binding. The current study provides the most structurally diverse ER RBA data set with the widest range of RBA values published to date.
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openalex_W2151063137 Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors R. Blair, Haoyu Fang, William S. Branham, Bruce S. Hass, Stacy L. Dial, Carrie L. Moland, Weida Tong, Leming Shi, Roger Perkins, Daniel M. Sheehan
Journal toxicological sciences : an official journal of the society of toxicology
Year 2000
DOI
10.1093/toxsci/54.1.138
URL
https://doi.org/10.1093/toxsci/54.1.138
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