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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.|
|Issue Date: ||2009-12-01|
|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|
|Appears in Collections:||[化學學系暨研究所] 期刊論文|
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