Abstract
Hereditary vitamin D-resistant rickets (HVDRR) is a genetic disorder caused by mutations in the vitamin D receptor, which lead to resistance to 1 α,25-dihydroxyvitamin D3 [1 α,25(OH)2D 3]. We found that the A ring-modified analogues, 2 α-(3-hydroxypropyl)-and 2 α-(3-hydroxypropoxy)-1 α,25(OH) 2D3, (O1C3 and O2C3) can bind better than the natural hormone to the mutant VDR (R274A), which similar to the HVDRR mutant, R274L, had lost the hydrogen bond to the 1 α-hydroxyl group of 1 α,25(OH) 2D3.
| Original language | English |
|---|---|
| Pages (from-to) | 357-358 |
| Number of pages | 2 |
| Journal | Chemical and Pharmaceutical Bulletin |
| Volume | 51 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 2003 Mar |
Keywords
- 2 α-substituted 1 α,25-dihydroxyvitamin D
- Docking study
- Mutant vitamin D receptor
- Potent ligand
- Rickets
ASJC Scopus subject areas
- Chemistry(all)
- Drug Discovery
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Kittaka, A., Kurihara, M., Peleg, S., Suhara, Y., & Takayama, H. (2003). 2 α-(3-hydroxypropyl)- and 2 α-(3-hydroxypropoxy)-1 α,25-dihydroxyvitamin D3 accessible to vitamin D receptor mutant related to hereditary vitamin D-resistant rickets. Chemical and Pharmaceutical Bulletin, 51(3), 357-358. https://doi.org/10.1248/cpb.51.357