In house validation of recombinant yeast estrogen and androgen receptor agonist and antagonist screening assays

Kolle, Susanne N.; Kamp, Hennicke; Huener, Hans-Albrecht; Knickel, J.; Verlohner, Andreas; Woitkowiak, Claudia; Landsiedel, Robert; Ravenzwaay, B. van

doi:10.1016/j.tiv.2010.08.008

Cited by 54 publications

(39 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A similar conclusion was presented by Pedersen et al (1999) studying the induction of plasma vitellogenin in rainbow trout by linear and technical nonyl-and octylphenol. In a more recent study, p-n-nonylphenol was even used as a negative control for the validation of a recombinant yeast estrogen receptor agonist assay (Kolle et al, 2010). Moreover, butylbenzyl phthalate, di-n-butyl phthalate, and ethyl paraben were reported to bind weakly to the ER and were also slightly active in the BG1luc eR transcriptional activation assay (ICCVAM, 2003(ICCVAM, , 2011.…”

Section: Discussionmentioning

confidence: 99%

A 155-plex high-throughput in vitro coregulator binding assay for (anti-)estrogenicity testing evaluated with 23 reference compounds

Wang

Melchers

Aarts

et al. 2013

ALTEX

View full text Add to dashboard Cite

show abstract

Section: Discussionmentioning

confidence: 99%

A 155-plex high-throughput in vitro coregulator binding assay for (anti-)estrogenicity testing evaluated with 23 reference compounds

Wang

Melchers

Aarts

et al. 2013

ALTEX

View full text Add to dashboard Cite

show abstract

“…NP has many scientific evidences in in vivo and in vitro studies as agonist. However some publications presented no estrogenic activity on hERα yeast assay (Kolle et al, 2010). Estrogenic activity of certain chemical such as NP has no consensus on which species and types of ER.…”

Section: Estrogenic Activities Of Phthalates and Alkylphenolsmentioning

confidence: 99%

“…These results suggest that TBBPA may not bind or limitation of bind to ERα. BBP and BPA were well known as ERα bounded weak agonists (Soto et al, 1995;Miller et al, 2001) while DBP was known that it did not bind to recombinant human ERα protein (Seidlová -Wuttke et al, 2005;Kolle et al, 2010). Additionally, the difference of ranking order for BPA and NP was resulted in the assay principle between transcriptional assay and binding affinity.…”

Section: Estrogenic Activities Of Phthalates and Alkylphenolsmentioning

confidence: 99%

Evaluation of <i>in vitro</i> screening system for estrogenicity: comparison of stably transfected human estrogen receptor-α transcriptional activation (OECD TG455) assay and estrogen receptor (ER) binding assay

Lee

Kim

et al. 2012

J. Toxicol. Sci.

View full text Add to dashboard Cite

-The estrogenic activity of industrial chemicals, di(2-ethylhexyl) phthalate (DEHP), di(n-butyl) phthalate (DBP), benzylbutyl phthalate (BBP), diethyl phthalate (DEP), tetrabromobisphenol A (TBBPA), bisphenol A (BPA), and nonylphenol (NP), was compared using OECD test guideline 455(TG455), stably transfected transcriptional activation (STTA) and estrogen receptor (ER) binding assays. The estrogenic activity of BBP, BPA and NP were approximately 180,000-fold (PC 50 , 4.32 x 10 -6 M), 5,000-fold (PC 50 , 1.26 x 10 -7 M) and 120,000-fold (PC 50 , 2.92 x 10 -6 M) less than 17β-estradiol (PC 50 , 2.43 x 10 -11 M), whereas DEHP, DBP and DEP did not show any estrogenicity activity in the STTA assay. Moreover, binding affinities to human ERα of BBP, BPA, and NP were approximately 200,000-fold (IC 50 , 4.91 x 10 -4 M), 8000-fold (IC 50 , 1.92 x 10 -5 M) and 1400-fold (IC 50 , 3.34 x 10 -6 M) less than 17β-estradiol (IC 50 , 2.45 x 10 -9 M) in competitive human ERα binding assay. The relative potencies of STTA assay were very similar to ER binding, E-screen, and Yeast screening assays. Therefore, our results suggested that OECD test guideline TG455 may be useful as a screening test for potential endocrine disruptors.

show abstract

“…However, considering that less E2 can reduce the response intensity and the signal-to-noise ratio of the test, we chose the EC submax concentration of E2 to achieve a compromise effect, and this choice was applied in all the antagonistic activity tests in this study. The concentration causing the sub-maximum effect has been used by many researchers in the antagonist tests (Bovee et al, 2008;Kolle et al, 2010;Wang et al, 2005), as well as in previous studies by our lab (Li et al, 2008a;Li et al, 2010). Therefore, our selection of EC submax is consistent with these studies and conducive for comparisons.…”

Section: Discussionmentioning

confidence: 68%

Combined action of estrogen receptor agonists and antagonists in two-hybrid recombinant yeast in vitro

Yang

Rao

et al. 2015

Ecotoxicology and Environmental Safety

View full text Add to dashboard Cite

a b s t r a c tEstrogen receptor (ER) antagonistic chemicals in aquatic environments are believed to influence the binding of both endogenous and exogenous estrogens to ERs in aquatic organisms. Although the combined effects of estrogenic compounds have attracted much scientific concern, little work has been done on the influence of such antiestrogens on the biological effects of estrogens. This study focused on how the presence of different amounts of antagonists affects the results of ER agonist activity tests. To achieve this, three questions were stated and answered in sequence. A two-hybrid recombinant yeast assay mediated by ER was adopted, providing a single mode of action and single target of action for this study. Mixtures created by an ER agonist and three antagonists following the fixed-ratio principle were assessed. The concentration of 17β-estradiol causing maximum induction was set as the fixed dose of estrogen in the antagonist activity test (question 1). When the two classes of chemicals coexisted, antiestrogens, which as a whole behaved according to the concentration addition model (question 2), decreased the response of estrogen and compressed the concentration-response curves along the y-axis in the agonist activity test (question 3). This may cause the estradiol equivalent to be underestimated and potentially mask the action of estrogenic effects in toxicity evaluation of environmental samples.

show abstract

In house validation of recombinant yeast estrogen and androgen receptor agonist and antagonist screening assays

Cited by 54 publications

References 28 publications

A 155-plex high-throughput in vitro coregulator binding assay for (anti-)estrogenicity testing evaluated with 23 reference compounds

A 155-plex high-throughput in vitro coregulator binding assay for (anti-)estrogenicity testing evaluated with 23 reference compounds

Evaluation of <i>in vitro</i> screening system for estrogenicity: comparison of stably transfected human estrogen receptor-α transcriptional activation (OECD TG455) assay and estrogen receptor (ER) binding assay

Combined action of estrogen receptor agonists and antagonists in two-hybrid recombinant yeast in vitro

Contact Info

Product

Resources

About