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

doi:10.1021/bc0601121

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 journal › Article › peer-review

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 language	English
Pages (from-to)	614-620
Number of pages	7
Journal	Bioconjugate Chemistry
Volume	18
Issue number	3
DOIs	https://doi.org/10.1021/bc0601121
Publication status	Published - 2007 May 1
Externally published	Yes

ASJC Scopus subject areas

Biotechnology
Bioengineering
Biomedical Engineering
Pharmacology
Pharmaceutical Science
Organic Chemistry

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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.",

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AU - Arai, Midori A.

AU - Takeyama, Ken Ichi

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AU - Kato, Shigeaki

AU - Chen, Tai C.

AU - Kittaka, Atsushi

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