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Please use this identifier to cite or link to this item:
https://tkuir.lib.tku.edu.tw/dspace/handle/987654321/25015
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| Title: | Inhibitors of 25-hydroxyvitamin D3-1α-hydroxylase: Thiavitamin D analogs and biological evaluation |
| Authors: | 李世元;Lee, Adam Shih-yuan;Muralidharan, K. Raman;Rowland-Goldsmith, Melissa;Park, Gyoosoon;Norman, Anthony W.;Henry, Helen L.;Okamura, William H. |
| Contributors: | 淡江大學化學學系 |
| Date: | 1997-05-01 |
| Issue Date: | 2009-12-01 |
| Publisher: | Elsevier |
| Abstract: | Six A-ring analogs of 1α,25-dihydroxyvitamin D3 (1, 1α,25-(OH)2-D3) 3-deoxy-3-thia-1α,25-(OH)2-D3 (3), 3-deoxy-3-thia-1α,25-(OH)2-D3-3α-oxide (6), 3-deoxy-3-thia-1α,25-(OH)2-D3-3β-oxide (7) and the 5,6-trans counterparts 5, 8, and 9, respectively—were tested for their ability to inhibit 25-hydroxy-D3-1α-hydroxylase (1-OH-ase) in vitro in mitochondria isolated from kidneys of vitamin D deficient chicks. The six analogs were also evaluated in terms of their ability to bind to the chicken intestinal nuclear receptor (VDR) in comparison to the natural hormone 1α,25-(OH)2-D3. Analog 7 is not only the best inhibitor of the 1-OH-ase but it also binds effectively to the chick intestinal receptor. It is established that vitamin D analogs must have a 1α oxygen group for effective inhibition of the 1-OH-ase. This functional group is also needed for effective binding to the chick intestinal VDR. |
| Relation: | Journal of steroid biochemistry and molecular biology 62(1), pp.73-78 |
| DOI: | 10.1016/S0960-0760(97)00015-0 |
| Appears in Collections: | [Graduate Institute & Department of Chemistry] Journal Article
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