Inhibitors of 25-hydroxyvitamin D3-1α-hydroxylase: Thiavitamin D analogs and biological evaluation
學年 85
學期 2
出版（發表）日期 1997-05-01
作品名稱 Inhibitors of 25-hydroxyvitamin D3-1α-hydroxylase: Thiavitamin D analogs and biological evaluation
作品名稱（其他語言）
著者 李世元; Lee, Adam Shih-yuan; Muralidharan, K. Raman; Rowland-Goldsmith, Melissa; Park, Gyoosoon; Norman, Anthony W.; Henry, Helen L.;Okamura, William H.
單位 淡江大學化學學系
出版者 Elsevier
著錄名稱、卷期、頁數 Journal of steroid biochemistry and molecular biology 62(1), pp.73-78
摘要 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.
關鍵字
語言 en
ISSN 0960-0760
期刊性質 國內
收錄於
產學合作
通訊作者
審稿制度 否
國別 TWN
公開徵稿
出版型式 ,電子版
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