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Human cell-based estrogen receptor beta dimerization assay.
Seo, Hyeyeong; Seo, Huiwon; Byrd, Nick; Kim, Hyejin; Lee, Kwang-Geun; Lee, Seok-Hee; Park, Yooheon.
Afiliación
  • Seo H; Department of Food Science and Biotechnology, Dongguk University, Goyang, 10326, Republic of Korea.
  • Seo H; Department of Food Science and Biotechnology, Dongguk University, Goyang, 10326, Republic of Korea.
  • Byrd N; Department of Chemistry and Biochemistry, Campden BRI, Chipping Campden, GL55 6LD, UK.
  • Kim H; Department of Food Science and Biotechnology, Dongguk University, Goyang, 10326, Republic of Korea.
  • Lee KG; Department of Food Science and Biotechnology, Dongguk University, Goyang, 10326, Republic of Korea.
  • Lee SH; Department of Food Science and Biotechnology, Dongguk University, Goyang, 10326, Republic of Korea.
  • Park Y; Department of Food Science and Biotechnology, Dongguk University, Goyang, 10326, Republic of Korea. Electronic address: ypark@dongguk.edu.
Chem Biol Interact ; 369: 110264, 2023 Jan 05.
Article en En | MEDLINE | ID: mdl-36402211
Estrogen is not only responsible for important functions in the human body, such as cell growth, reproduction, differentiation, and development, but it is also deeply related to pathological processes, such as cancer, metabolic and cardiovascular diseases, and neurodegeneration. Estrogens and other estrogenic compounds have transcriptional activities through binding with the estrogen receptor (ER) to induce ER dimerization. The two estrogen receptor subtypes, estrogen receptor alpha (ERα) and estrogen receptor beta (ERß), show structural differences and have different expression ratios in specific cells and tissues. Currently, the methods for confirming the estrogenic properties of compounds are the binding (Test guideline no. 493) and transactivation (Test guideline no. 455) assays provided by the Organization for Economic Co-operation and Development (OECD). In a previous study, we developed an ERα dimerization assay based on the bioluminescence resonance energy transfer (BRET) system, but there are currently no available tests that can confirm the effect of estrogenic compounds on ERß. Therefore, in this study, we developed a BRET-based ERß dimerization assay to confirm the estrogenic prosperities of compounds. The BRET-based ERß dimerization assay was verified using nine representative ER ligands and the results were compared with the dimerization activity of ERα. In conclusion, our BRET-based ERß dimerization assay can provide information on the ERß dimerization potential of estrogenic compounds.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Estrógenos / Receptor beta de Estrógeno Límite: Humans Idioma: En Revista: Chem Biol Interact Año: 2023 Tipo del documento: Article Pais de publicación: Irlanda

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Estrógenos / Receptor beta de Estrógeno Límite: Humans Idioma: En Revista: Chem Biol Interact Año: 2023 Tipo del documento: Article Pais de publicación: Irlanda