scholarly journals Chemical space, diversity and activity landscape analysis of estrogen receptor binders

RSC Advances ◽  
2018 ◽  
Vol 8 (67) ◽  
pp. 38229-38237 ◽  
Author(s):  
J. Jesús Naveja ◽  
Ulf Norinder ◽  
Daniel Mucs ◽  
Edgar López-López ◽  
Josė L. Medina-Franco
Keyword(s):  
Estrogen Receptor ◽  
Chemical Space ◽  
Endocrine Disrupting Chemicals ◽  
Landscape Analysis ◽  
Space Diversity ◽  
Global Diversity ◽  
Structure Level ◽  
Endocrine Disrupting ◽  
Activity Cliffs

Global diversity and activity landscape analysis of endocrine-disrupting chemicals identifies activity cliffs that are rationalized at the structure level.

scholarly journals The Effects of Endocrine Disrupting Chemicals on Biomarkers of Inflammation Produced by Lipopolysaccharide Stimulated RAW264.7 Macrophages

2019 ◽  
Vol 16 (16) ◽  
pp. 2914
Author(s):  
Vedastus W. Makene ◽  
Edmund J. Pool
Keyword(s):  
Estrogen Receptor ◽  
Receptor Antagonist ◽  
Cell Cultures ◽  
Endocrine Disrupting Chemicals ◽  
Raw264.7 Cells ◽  
Inhibitory Effects ◽  
Receptor Antagonists ◽  
Estrogen Receptor Antagonist ◽  
Endocrine Disrupting ◽  
Raw264.7 Cell

Endocrine disrupting chemicals (EDCs) are common pollutants in the environment and can induce disruption of the endocrine and immune systems. The present study evaluated the effects of selected common environmental EDCs on secretion of inflammatory biomarkers by RAW264.7 cells. The EDCs investigated were Estradiol (E2), 5α-dihydrotestosterone (DHT), and Bisphenol A (BPA). To evaluate if the effects caused by EDCs were modulated by steroid hormone receptors, antagonists of estrogen and androgen receptors were used. The steroid receptor antagonists used were Tamoxifen, an estrogen receptor antagonist, and Flutamide, an androgen receptor antagonist. Secretion of biomarkers of inflammation, namely nitric oxide (NO) and interleukin 6 (IL-6), were monitored. The NO was determined using Griess reaction and IL-6 was measured by enzyme linked immunosorbent assay (ELISA). Although 5 μg/mL E2, DHT, and BPA were not toxic to RAW264.7 cell cultures, the same treatments significantly (p < 0.001) reduced both NO and IL-6 secretion by lipopolysaccharide (LPS)-stimulated RAW264.7 cell cultures. The suppression of NO and IL-6 secretion indicate inhibition of inflammation by DHT, E2, and BPA. The inhibitory effects of DHT, E2 and BPA are partially mediated via their cellular receptors, because the effects were reversed by their respective receptor antagonists. Flutamide reversed the effects of DHT, while Tamoxifen reversed the effects of E2 and BPA. In conclusion, E2, BPA, and DHT inhibit the synthesis of inflammation biomarkers by LPS-stimulated RAW264.7 cells. The inhibitory effects of EDCs can be partially reversed by the addition of an estrogen receptor antagonist for E2 and BPA, and an androgenic receptor antagonist for DHT. The inhibition of inflammatory response in stimulated RAW264.7 cells may be a useful bioassay model for monitoring estrogenic and androgenic pollutants.

scholarly journals Differentiation of PC12 cells expressing estrogen receptor alpha: A new bioassay for endocrine-disrupting chemicals evaluation

Chemosphere ◽  
2014 ◽  
Vol 112 ◽  
pp. 240-247 ◽  
Author(s):  
Denis Habauzit ◽  
François Ferrière ◽  
Nadine Botherel ◽  
Gilles Flouriot ◽  
Farzad Pakdel ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Pc12 Cells ◽  
Estrogen Receptor Alpha ◽  
Endocrine Disrupting Chemicals ◽  
Receptor Alpha ◽  
Endocrine Disrupting ◽  
New Bioassay

scholarly journals Differential Activation of a Mouse Estrogen Receptor β Isoform (mER β 2) with Endocrine-Disrupting Chemicals (EDCs)

2017 ◽  
Vol 125 (4) ◽  
pp. 634-642 ◽  
Author(s):  
Lauren J. Donoghue ◽  
Thomas I. Neufeld ◽  
Yin Li ◽  
Yukitomo Arao ◽  
Laurel A. Coons ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Endocrine Disrupting Chemicals ◽  
Estrogen Receptor Β ◽  
Differential Activation ◽  
Endocrine Disrupting
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