High-throughput system for analyzing ligand-induced cofactor recruitment by vitamin D receptor

Midori A. Arai, Ken Ichi Takeyama, Saya Ito, Shigeaki Kato, Tai C. Chen, Atsushi Kittaka

研究成果: Article査読

12 被引用数 (Scopus)

抄録

A high-throughput screening system for analyzing small molecule-induced coactivator (CoA) recruitment by the vitamin D receptor (VDR) has been developed. The vitamin D-induced protein-protein interactions between VDR and fluorophore (Cy3 or Cy5)-labeled TIF2 or SRC-1 were successfully detected by using a new HCHO fixing method of the protein complex on microplates. The results obtained from this screening of our synthetic vitamin D analogues suggest that the CoA-recruiting activities play an important role in determining the biological activity of various vitamin D analogues and explain the discrepancies between the VDR binding affinity and their biological activity.

本文言語English
ページ(範囲)614-620
ページ数7
ジャーナルBioconjugate Chemistry
18
3
DOI
出版ステータスPublished - 2007
外部発表はい

ASJC Scopus subject areas

  • バイオテクノロジー
  • バイオエンジニアリング
  • 生体医工学
  • 薬理学
  • 薬科学
  • 有機化学

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