Considerations when assessing antagonism in vitro: why standardizing the agonist concentration matters

Neale, Peta A. and Leusch, Frederic D. L. (2015) Considerations when assessing antagonism in vitro: why standardizing the agonist concentration matters. Chemosphere, 135 20-23. doi:10.1016/j.chemosphere.2015.03.054


Author Neale, Peta A.
Leusch, Frederic D. L.
Title Considerations when assessing antagonism in vitro: why standardizing the agonist concentration matters
Journal name Chemosphere   Check publisher's open access policy
ISSN 1879-1298
0045-6535
Publication date 2015-09
Sub-type Article (original research)
DOI 10.1016/j.chemosphere.2015.03.054
Open Access Status Not Open Access
Volume 135
Start page 20
End page 23
Total pages 4
Place of publication Kidlington, Oxford, United Kingdom
Publisher Pergamon Press
Collection year 2016
Language eng
Formatted abstract
There is increasing recognition of the importance of assessing both agonism and antagonism in parallel for environmental samples. Cell-based in vitro assays have the advantage over receptor binding assays as they are able to differentiate between agonist and antagonist activity, but at present there is no standardized approach to assess antagonism in vitro, and in particular the competing agonist concentration can vary in the literature anywhere from half maximal to maximal effect concentrations. In this study, we investigated the influence of changing agonist concentrations in the estrogen receptor alpha (ERα), progesterone receptor (PR) and glucocorticoid receptor (GR) assays run in antagonist mode. The antagonistic effect varied by over two orders of magnitude when using the range of agonist concentrations applied in the literature, clearly indicating the need for standardization. By comparing antagonist EC50 values with different background agonist concentrations, an EC80 background agonist concentration is recommended when assessing antagonism in vitro to optimise both assay sensitivity and reproducibility.
Keyword Antagonist
Estrogen receptor
Glucocorticoid receptor
In vitro
Progesterone receptor
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Non HERDC
National Research Centre for Environmental Toxicology Publications
 
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