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

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)614-620
Number of pages7
JournalBioconjugate Chemistry
Volume18
Issue number3
DOIs
Publication statusPublished - 2007 May 1
Externally publishedYes

ASJC Scopus subject areas

  • Biotechnology
  • Bioengineering
  • Biomedical Engineering
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry

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