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Literature summary extracted from

  • Zhu, J.; Barycki, R.; Chiellini, G.; Deluca, H.F.
    Screening of selective inhibitors of 1alpha,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli (2010), Biochemistry, 49, 10403-10411.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.15.16 expressed in Escherichia coli BL21-Gold(DE3) and Rosetta 2(DE3) cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.15.16 (1R,3S,5Z,7E,14x)-17-[(2R)-1-(1H-imidazol-1-yl)propan-2-yl]-2-methylidene-9,10-secoestra-5,7-diene-1,3-diol potent and selective CYP24A1 inhibitor Homo sapiens
1.14.15.16 (1R,3S,5Z,7E,14x)-17-[(2S)-7-cyclopropylheptan-2-yl]-2-methylidene-9,10-secoestra-5,7-diene-1,3-diol potent and selective CYP24A1 inhibitor Homo sapiens
1.14.15.16 (2R)-2-[(4E,7aR)-4-[(2Z)-2-[(5R)-5-hydroxy-2-methylidenecyclohexylidene]ethylidene]-7a-methyloctahydro-1H-inden-1-yl]propyl bromoacetate
-
Homo sapiens
1.14.15.16 (3R,5Z,7E,14x,17x,20S)-3-hydroxy-9,10-secochola-5,7,10-trien-24-yl 4-methylbenzenesulfonate
-
Homo sapiens
1.14.15.16 24-carboxyl-25-hydroxyvitamin D3
-
Homo sapiens
1.14.15.16 24-difluoro-1,25-dihydroxyvitamin D3
-
Homo sapiens
1.14.15.16 ketoconazole nonspecific CYP24A1 inhibitor Homo sapiens
1.14.15.16 liarozole nonspecific CYP24A1 inhibitor Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.14.15.16 0.00014
-
2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 0.00019
-
1alpha,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 0.00033
-
25-hydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 0.00034
-
2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.14.15.16 55000
-
about 55000 Da, SDS-PAGE Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.14.15.16 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.14.15.16 Talon metal affinity column chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.15.16 1alpha,25-dihydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens 1alpha,24R,25-trihydroxyvitamin D3 + NADP+ + H2O
-
?
1.14.15.16 2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens ? + NADP+ + H2O
-
?
1.14.15.16 2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens ? + NADP+ + H2O
-
?
1.14.15.16 25-hydroxyvitamin D3 + NADPH + H+ + O2
-
Homo sapiens 24R,25-dihydroxyvitamin D3 + NADP+ + H2O
-
?

Synonyms

EC Number Synonyms Comment Organism
1.14.15.16 1alpha,25-dihydroxyvitamin D3 24-hydroxylase
-
Homo sapiens
1.14.15.16 CYP24A1
-
Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.14.15.16 0.00025
-
2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 0.0017
-
2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 0.002
-
1alpha,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 0.002
-
25-hydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.14.15.16 heme CYP24A1 has a heme content of 77-85% Homo sapiens
1.14.15.16 NADPH
-
Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.14.15.16 1.8
-
2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 4.9
-
2-methylene-19-nor-(20R)-1,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 6.1
-
25-hydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens
1.14.15.16 10
-
1alpha,25-dihydroxyvitamin D3 in 20 mM Tris (pH 7.5), at 37°C Homo sapiens