Potent, low-calcemic, selective inhibitors of CYP24 hydroxylase: 24-sulfone analogs of the hormone 1alpha,25-dihydroxyvitamin D3

The new 24-phenylsulfone 4a, a low-calcemic analog of the natural hormone 1alpha,25-dihydroxyvitamin D(3), is a potent (IC(50) = 28nM) 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. 89-90; no. 1-5; 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 England 01.05.2004
Subjects
Animals
Calcitriol - analogs & derivatives
Calcitriol - pharmacology
Cell Line
Chromatography, High Pressure Liquid
Chromatography, Thin Layer
Cytochrome P-450 Enzyme Inhibitors
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Humans
Spectrum Analysis
Steroid Hydroxylases - antagonists & inhibitors
Sulfones - chemistry
Transcription, Genetic - drug effects
Vitamin D3 24-Hydroxylase
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Summary:The new 24-phenylsulfone 4a, a low-calcemic analog of the natural hormone 1alpha,25-dihydroxyvitamin D(3), is a potent (IC(50) = 28nM) and highly selective inhibitor of the human 24-hydroxylase enzyme CYP24.
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ISSN:0960-0760