Potent, low-calcemic, selective inhibitors of CYP24 hydroxylase: 24-sulfone analogs of the hormone 1α,25-dihydroxyvitamin D 3

The new 24-phenylsulfone 4a, a low-calcemic analog of the natural hormone 1α,25-dihydroxyvitamin D 3, is a potent (IC 50 = 28 nM) and highly selective inhibitor of the human 24-hydroxylase enzyme CYP24.

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Bibliographic Details
Published inThe Journal of steroid biochemistry and molecular biology Vol. 89; pp. 5 - 12
Main Authors Posner, Gary H., Crawford, Kenneth R., Yang, Hong Woon, Kahraman, Mehmet, Jeon, Heung Bae, Li, Hongbin, Lee, Jae Kyoo, Suh, Byung Chul, Hatcher, Mark A., Labonte, Tanzina, Usera, Aimee, Dolan, Patrick M., Kensler, Thomas W., Peleg, Sara, Jones, Glenville, Zhang, Anqi, Korczak, Bozena, Saha, Uttam, Chuang, Samuel S.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 01.05.2004
Subjects
Catabolism inhibitor
Low-calcemic
Vitamin D analogs
Low-calcemic
Vitamin D analogs
Catabolism inhibitor
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Summary:The new 24-phenylsulfone 4a, a low-calcemic analog of the natural hormone 1α,25-dihydroxyvitamin D 3, is a potent (IC 50 = 28 nM) and highly selective inhibitor of the human 24-hydroxylase enzyme CYP24.
ISSN:0960-0760
1879-1220
DOI:10.1016/j.jsbmb.2004.03.044