Synonyms 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial, 24-OHase, CP24 + [10] |
Introduction A cytochrome P450 monooxygenase with a key role in vitamin D catabolism and calcium homeostasis. Via C24- and C23-oxidation pathways, catalyzes the inactivation of both the vitamin D precursor calcidiol (25-hydroxyvitamin D(3)) and the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:24893882, PubMed:15574355, PubMed:8679605, PubMed:11012668, PubMed:16617161, PubMed:29461981). With initial hydroxylation at C-24 (via C24-oxidation pathway), performs a sequential 6-step oxidation of calcitriol leading to the formation of the biliary metabolite calcitroic acid (PubMed:24893882, PubMed:15574355). With initial hydroxylation at C-23 (via C23-oxidation pathway), catalyzes sequential oxidation of calcidiol leading to the formation of 25(OH)D3-26,23-lactone as end product (PubMed:11012668, PubMed:8679605). Preferentially hydroxylates at C-25 other vitamin D active metabolites, such as CYP11A1-derived secosteroids 20S-hydroxycholecalciferol and 20S,23-dihydroxycholecalciferol (PubMed:25727742). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via FDXR/adrenodoxin reductase and FDX1/adrenodoxin (PubMed:8679605). |
Target |
Mechanism CYP24A1 inhibitors [+1] |
Active Org.- |
Originator Org. |
Active Indication- |
Inactive Indication |
Drug Highest PhaseDiscontinued |
First Approval Ctry. / Loc.- |
First Approval Date20 Jan 1800 |
Target |
Mechanism CYP24A1 inhibitors [+2] |
Active Org.- |
Originator Org. |
Active Indication- |
Inactive Indication |
Drug Highest PhaseDiscontinued |
First Approval Ctry. / Loc.- |
First Approval Date20 Jan 1800 |
Start Date01 Jan 2013 |
Sponsor / Collaborator |
Start Date01 Oct 2008 |
Sponsor / Collaborator |
Start Date01 Sep 2006 |
Sponsor / Collaborator |