Development of a Human Estrogen Receptor Dimerization Assay for the Estrogenic Endocrine-Disrupting Chemicals Using Bioluminescence Resonance Energy Transfer

Hye Mi Kim, Hyeyeong Seo, Yooheon Park, Hee-Seok Lee, Seok-Hee Lee and Kwang Suk Ko
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Hye Mi Kim: Department of Nutritional Science and Food Management, Ewha Womans University, Seoul 03760, Korea
Hyeyeong Seo: Department of Integrated Biomedical and Life Science, Korea University, Seoul 02841, Korea
Yooheon Park: Department of Food Science and Biotechnology, Dongguk University, Goyang 10326, Korea
Hee-Seok Lee: Department of Food Science and Technology, Chung-Ang University, Anseong 17546, Korea
Seok-Hee Lee: Department of Food Science and Biotechnology, Dongguk University, Goyang 10326, Korea
Kwang Suk Ko: Department of Nutritional Science and Food Management, Ewha Womans University, Seoul 03760, Korea

IJERPH, 2021, vol. 18, issue 16, 1-13

Abstract: Endocrine-disrupting chemicals (EDCs) are found in food and various other substances, including pesticides and plastics. EDCs are easily absorbed into the body and have the ability to mimic or block hormone function. The radioligand binding assay based on the estrogen receptors binding affinity is widely used to detect estrogenic EDCs but is limited to radioactive substances and requires specific conditions. As an alternative, we developed a human cell-based dimerization assay for detecting EDC-mediated ER-alpha (ER?) dimerization using bioluminescence resonance energy transfer (BRET). The resultant novel BRET-based on the ER? dimerization assay was used to identify the binding affinity of 17?-estradiol (E2), 17?-estradiol, corticosterone, diethylhexyl phthalate, bisphenol A, and 4-nonylphenol with ER? by measuring the corresponding BRET signals. Consequently, the BRET signals from five chemicals except corticosterone showed a dose-dependent sigmoidal curve for ER?, and these chemicals were suggested as positive chemicals for ER?. In contrast, corticosterone, which induced a BRET signal comparable to that of the vehicle control, was suggested as a negative chemical for ER?. Therefore, these results were consistent with the results of the existing binding assay for ER? and suggested that a novel BRET system can provide information about EDCs-mediated dimerization to ER?.

Keywords: estrogenic endocrine-disrupting chemical; estrogen receptor; bioluminescence resonance energy transfer; risk assessment (search for similar items in EconPapers)
JEL-codes: I I1 I3 Q Q5 (search for similar items in EconPapers)
Date: 2021
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