Mechanistic insight into human androgen receptor-mediated endocrine-disrupting potentials by a stable bioluminescence resonance energy transfer-based dimerization assay

Seok Hee Lee, Kyung Youn Hong, Hyeyeong Seo, Hee Seok Lee, Yooheon Park

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

To develop a novel cell-based assay to evaluate the androgenic endocrine-disrupting properties of chemical substances, we established a method to detect ligand-mediated androgen receptor (AR) dimerization in stably transfected human cell lines using a bioluminescence resonance energy transfer (BRET) system. Using stably transfected human embryonic kidney (HEK-293) cells, the BRET-based AR dimerization assay was optimized as a novel test method and was validated using test chemicals recommended by the Interagency Coordinating Committee on the Validation of Alternative Methods (ICCVAM). The BRET-based AR dimerization assay showed high accuracy, sensitivity, and specificity for the detection of androgenic endocrine-disrupting chemicals (EDCs), and the assay protocol is adequate for practical use. This dimerization assay is based on ligand-mediated hormone receptor dimerization and can provide accurate information about androgenic endocrine-disrupting properties at the cellular level, complementing conventional binding and transactivation assays.

Original languageEnglish
Article number109655
JournalChemico-Biological Interactions
Volume349
DOIs
StatePublished - 1 Nov 2021

Keywords

  • Androgen receptor (AR)
  • Bioluminescence resonance energy transfer (BRET)
  • Dimerization assay
  • Endocrine-disrupting chemicals (EDCs)

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