Study on interactions of endocrine disruptors with estrogen receptor using fluorescence polarization
Literature Information
Publication Date
2003-07-07
DOI
10.1039/B303985D
Impact Factor
4.616
Authors
Sachiko Suzuki, Takeshi Fukushima, Masako Maeda, Tomofumi Santa, Kazuhiro Imai
View Original
Abstract
In this study, we examined the affinities of many (21) compounds such as hormones, pharmaceuticals, industrial chemicals, and phytoestrogens to the estrogen receptor (ER) by ER binding assay using fluorescence polarization (FP). This method is based on the competitive binding assay using fluorescein-labeled estradiol (F–E2), in which the polarization values decreased with the addition of the compounds (competitors). The obtained sigmoidal inhibition curves were transformed into the pseudo-Hill plots, and the concentrations at 50% inhibition (IC50) and Hill coefficients were obtained from the regression equations. We examined the relationship between the chemical structures and estrogenic activities, and finally classified the tested compounds into three categories, agonists, partial agonists and antagonists based on their Hill coefficients.
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Source Journal
Analyst
CiteScore:
7.8
Self-citation Rate:
5.6%
Articles per Year:
653
Analyst publishes analytical and bioanalytical research that reports premier fundamental discoveries and inventions, and the applications of those discoveries, unconfined by traditional discipline barriers.
Recommended Compounds
N-phenyl-4-(quinolin-3-ylmethyl)piperidine-1-carboxamide
CAS Number:
959151-50-9
Molecular Formula:
C22H23N3O
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