General Information of the Protein
Protein ID
PT03062
Protein Name
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Secondarily
Protein Name
Cytochrome P450 24A1
Cytochrome P450-CC24
Gene Name
CYP24A1
Secondarily
Gene Name
CYP24
Sequence
MSSPISKSRSLAAFLQQLRSPRQPPRLVTSTAYTSPQPREVPVCPLTAGGETQNAAALPGPTSWPLLGSLLQILWKGGLKKQHDTLVEYHKKYGKIFRMKLGSFESVHLGSPCLLEALYRTESAYPQRLEIKPWKAYRDYRKEGYGLLILEGEDWQRVRSAFQKKLMKPGEVMKLDNKINEVLADFMGRIDELCDERGHVEDLYSELNKWSFESICLVLYEKRFGLLQKNAGDEAVNFIMAIKTMMSTFGRMMVTPVELHKSLNTKVWQDHTLAWDTIFKSVKACIDNRLEKYSQQPSADFLCDIYHQNRLSKKELYAAVTELQLAAVETTANSLMWILYNLSRNPQVQQKLLKEIQSVLPENQVPRAEDLRNMPYLKACLKESMRLTPSVPFTTRTLDKATVLGEYALPKGTVLMLNTQVLGSSEDNFEDSSQFRPERWLQEKEKINPFAHLPFGVGKRMCIGRRLAELQLHLALCWIVRKYDIQATDNEPVEMLHSGTLVPSRELPIAFCQR
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Cytochrome P450
>
Cytochrome P450 family 24
>
Cytochrome P450 family 24A
>
Cytochrome P450 24A1
Function
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).
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Uniprot ID
Primary ID:
Q07973

Secondarily ID:
Q15807
Q32ML3
Q5I2W7
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Ensembl ID
ENSG00000019186
HGNC ID
HGNC:2602
Subcellular Location
Mitochondrion
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0005212
US8987315, Ketoconazole
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C26H28Cl2N4O4
 1
1
IC50 = 520 nM
   TI
   LI
   LO
   TS
CP0476431
6-Methoxy-2-(2-methyl-benzyl)-3,4-dihydro-2H-naphthalen-1-one
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C19H20O2
 1
1
IC50 = 900 nM
   TI
   LI
   LO
   TS
CP0467417
2-(2-Ethylbenzyl)-6-methoxy-tetralone
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C20H22O2
 1
1
IC50 = 1920 nM
   TI
   LI
   LO
   TS
CP0467416
2-(2-Trifluoromethylbenzyl)-6-methoxy-tetralone
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C19H17F3O2
 1
1
IC50 = 2080 nM
   TI
   LI
   LO
   TS
CP0504379
(E)-2-(2-(E)-Styrylbenzylidene)-6-methoxy-tetralone
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C26H22O2
 1
1
IC50 = 5080 nM
   TI
   LI
   LO
   TS
CP0514826
(E)-2-(2-Ethylbenzylidene)-6-methoxy-tetralone
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C20H20O2
 1
1
IC50 = 10760 nM
   TI
   LI
   LO
   TS
CP0476430
(E)-2-(2-Trifluoromethylbenzylidene)-6-methoxy-tetralone
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C19H15F3O2
 1
1
IC50 = 11220 nM
   TI
   LI
   LO
   TS
CP0469828
2-(2-Bromobenzyl)-6-methoxy-tetralone
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C18H17BrO2
 1
1
IC50 = 16300 nM
   TI
   LI
   LO
   TS
CP0374359
2-(2-Phenethylbenzyl)-6-methoxy-tetralone
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C26H26O2
 1
1
IC50 = 25570 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0005212
US8987315, Ketoconazole
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C26H28Cl2N4O4
 3
1 IC50 = 470 nM
2 IC50 = 500 nM
3 Ki = 35 nM
Clinical Information about the Protein
Target 1 ( Cytochrome P450 24 (CYP24A1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Psoriasis vulgaris [ICD-11: EA90]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Lunacalcipol Phase 2
Psoriasis vulgaris