Estrogen receptors activity assessment

An example of a TIE approach is that described by Desbrow et al. [7]. In this work, the endocrine disrupting activity detected in effluents of seven UK WWTPs by means of a yeast-based screening assay [52] was mainly attributed to the presence of estradiol, estrone, and ethynylestradiol. However, to assess the estrogenic activity different bioassays may be used, e.g., the yeast-based recombinant estrogen receptor-reporter assay (YES), the MCF-7 cell proliferation (E-screen), and the estrogen receptor-mediated chemically activated... 

Bradbury, S.P., Mekenyan, O.G., and Ankley, G.T, Quantitative structure-activity relationships for polychlorinated hydroxybiphenyl estrogen receptor binding affinity an assessment of conformer flexibility, Environ. Toxicol. Chem., 15, 1945-1954, 1996. 

Tong W, Xie Q, Hong H, Shi LM, Fang H, Perkins R. Assessment of prediction confidence and domain extrapolation of two structure-activity relationship models for predicting estrogen receptor binding activity. Environ Health Perspect 2004 112 1249-54. 

Scientists at the National Institute of Environmental Health Sciences report that a set of three existing tests, when used in combination, provides a rapid assessment of a chemical s potential to mimic the hormone estrogen. One test determines whether the chemical can bind to an estrogen receptor site the second determines whether it activates estrogen-responsive genes in a cell hne and the third determines whether the chemical causes the proliferation of estrogen-responsive uterine tissue in female mice. Using these tests, results can be obtained in 3-5 weeks at a cost of about 15,000, versus 1-2 million for conventional cancer bioassays. ... 

The yeast reporter gene assays not only assess for the interaction of the chemical with the hormone receptor, but also the ability of that receptor-chemical ligand interaction to activate the hormone DNA response element. It should be realized, however, that most of these systems have been developed with human and mammalian hormone receptors and differences in ligand potencies can occur between different animal species. A comprehensive review of in vitro assays for measuring estrogenic activity, and some of the issues of comparability, is provided by Zacharewski (1997). 

Michallet-Ferrier, P., Ait-Aissa, S., Balaguer, P. et al. (2004). Assessment of estrogen (ER) and aryl hydrocarbon receptor (AhR) mediated activities in organic sediment extracts of the Detroit River, using in vitro bioassays based on human MELN and teleost PLHC-1 cell lines. Journal of Great Lakes Research, 30, 82-92. 

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