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 | |
| 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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Cite this
Arai, M. A., Takeyama, K. I., Ito, S., Kato, S., Chen, T. C., & Kittaka, A. (2007). High-throughput system for analyzing ligand-induced cofactor recruitment by vitamin D receptor. Bioconjugate Chemistry, 18(3), 614-620. https://doi.org/10.1021/bc0601121