Bioactivation of vitamin D(3) involves 25-hydroxylation and subsequent 1α-hydroxylation to produce 1α,25-dihydroxyvitamin D(3) [1,25(OH)(2)D(3)], the active hormone. Six cytochrome P450 enzymes (CYP27A1, CYP2R1, CYP2J2/3, CYP3A4, CYP2D25 and CYP2C11) catalyzing the initial 25-hydroxylation step are reviewed, and their physiological relevance as vitamin D 25-hydroxylases in vivo is discussed.
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