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ERRγ tethers strongly bisphenol A and 4-α-cumylphenol in an induced-fit manner

Authors
  • Matsushima, Ayami
  • Teramoto, Takamasa
  • Okada, Hiroyuki
  • Liu, Xiaohui
  • Tokunaga, Takatoshi
  • Kakuta, Yoshimitsu
  • Shimohigashi, Yasuyuki
Type
Published Article
Journal
Biochemical and Biophysical Research Communications
Publication Date
Jan 01, 2008
Volume
373
Issue
3
Pages
408–413
Identifiers
DOI: 10.1016/j.bbrc.2008.06.050
Source
Elsevier
Keywords
License
Unknown

Abstract

A receptor-binding assay and X-ray crystal structure analysis demonstrated that the endocrine disruptor bisphenol A (BPA) strongly binds to human estrogen-related receptor γ (ERRγ). BPA is well anchored to the ligand-binding pocket, forming hydrogen bonds with its two phenol-hydroxyl groups. In this study, we found that 4-α-cumylphenol lacking one of its phenol-hydroxyl groups also binds to ERRγ very strongly. The 2.0 Å crystal structure of the 4-α-cumylphenol/ERRγ complex clearly revealed that ERRγ’s Leu345-β-isopropyl plays a role in the tight binding of 4-α-cumylphenol and BPA, rotating in a back-and-forth induced-fit manner.

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