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
Show/Hide
|
||||
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).
Show/Hide
|
||||
Uniprot ID |
Show/Hide
|
||||
Ensembl ID | |||||
HGNC ID | |||||
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
Biochemical Assays
Compound ID | Compound Name | Compound Formula | |
CP0005212 |
US8987315, Ketoconazole
Show/Hide
|
C26H28Cl2N4O4
|
3 |
1 | IC50 = 470 nM | ||
---|---|---|---|
2 | IC50 = 500 nM | ||
3 | Ki = 35 nM |
Clinical Information about the Protein