Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Bae, S.H.; Paik, Y.K.
    Cholesterol biosynthesis from lanosterol: development of a novel assay method and characterization of rat liver microsomal lanosterol DELTA24-reductase (1997), Biochem. J., 326, 609-616.
    View publication on PubMedView publication on EuropePMC

Activating Compound

EC Number Activating Compound Comment Organism Structure
1.3.1.72 cholestyramine 120fold induction and activation by feeding 5% cholestyramine plus 0.1% lovastatin, CL-diet, and by modulating diurnal variation Rattus norvegicus
1.3.1.72 CO substrate lanosterol: required to inhibit 14alpha-methyl demethylase, 14alpha-demethylation of lanosterol. 14alpha-methyl demethylase activity is dominant over 24-reductase activity, and blockade or removal of 14alpha-methyl demethylase activity is absolutely required for the detection of maximal 24-reductase activity when lanosterol substrate is present. 24-reductase activity is activated in time-dependent manner when 14alpha-methyl demethylase is blocked by CO treatment Rattus norvegicus
1.3.1.72 ketoconazole substrate lanosterol: dose-dependent activation, less effective than miconazole, required to inhibit 14alpha-methyl demethylase, 14alpha-demethylation of lanosterol. 14alpha-methyl demethylase activity is dominant over 24-reductase activity, and blockade or removal of 14alpha-methyl demethylase activity is absolutely required for the detection of maximal 24-reductase activity when lanosterol substrate is present Rattus norvegicus
1.3.1.72 lovastatin 120fold induction and activation by feeding 5% cholestyramine plus 0.1% lovastatin, CL-diet, and by modulating diurnal variation Rattus norvegicus
1.3.1.72 miconazole substrate lanosterol: dose-dependent activation, maximum activation with about 0.01 mM miconazole, required to inhibit 14alpha-methyl demethylase, 14alpha-demethylation of lanosterol. 14alpha-methyl demethylase activity is dominant over 24-reductase activity, and blockade or removal of 14alpha-methyl demethylase activity is absolutely required for the detection of maximal 24-reductase activity when lanosterol substrate is present Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.1.72 3-beta-(2-(diethylamino)ethoxy)androst-5-en-17-one U18666A, non-competitive inhibition, Ki: 0.000157 mM, IC50 about 0.00015 mM, 690fold higher affinity for the enzyme than substrate lanosterol Rattus norvegicus
1.3.1.72 additional information no inhibition by lovastatin, mevalonolactone, Squalestatin 1, (E)-N-ethyl-N-(6,6-dimethyl-2-hepten-4-ynyl)-3-((3,3'-bithiophen-5-yl)methoxy)benzenemethanamine, NB-598, trans-1,4-bis(2-chlorobenzylaminomethyl)cyclohexane dihydrochloride, AY-9944 and CN- ion Rattus norvegicus
1.3.1.72 Triparanol 4-chloro-alpha-[4-[2-diethylaminoethoxy]phenyl]-alpha-(4-methylphenyl)benze-methanol; non-competitive inhibition, specific inhibitor, Ki: 0.000523 mM, IC50 about 0.0008 mM, 208fold higher affinity for the enzyme than substrate lanosterol Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.3.1.72 additional information
-
 additional information kinetic behaviour and kinetic data Rattus norvegicus
1.3.1.72 0.037
-
 5alpha-cholesta-7,24-dien-3beta-ol
-
 Rattus norvegicus
1.3.1.72 0.109
-
 4,4',14alpha-trimethyl-5alpha-cholesta-8,24-dien-3beta-ol lanosterol Rattus norvegicus
1.3.1.72 0.163
-
 5alpha-cholesta-5,24-dien-3beta-ol desmosterol Rattus norvegicus
1.3.1.72 0.176
-
 5alpha-cholesta-8,24-dien-3beta-ol zymosterol Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.3.1.72 membrane membrane-bound Rattus norvegicus 16020
-
1.3.1.72 microsome microsome-bound Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.3.1.72 5alpha-cholesta-7,24-dien-3beta-ol + NADPH Rattus norvegicus C-24 reduction of sterols probably takes place straight after sterol DELTA8-7 isomerization of zymosterol, which occurs several steps after C-32 demethylation of lanosterol in the 19-step pathway of cholesterol biosynthesis from lanosterol 5alpha-cholesta-7-en-3beta-ol + NADP+
-
 ?
1.3.1.72 5alpha-cholesta-7,24-dien-3beta-ol + NADPH Rattus norvegicus C-24 reduction of DELTA7,24-diene 5alpha-cholesta-7-en-3beta-ol + NADP+
-
 ?
1.3.1.72 5alpha-cholesta-7,24-dien-3beta-ol + NADPH Rattus norvegicus most reactive, probably natural substrate 5alpha-cholesta-7-en-3beta-ol + NADP+
-
 ?
1.3.1.72 additional information Rattus norvegicus anaerobic reduction of 24(25)-enes of lanosterol and other obligatory intermediates of cholesterol biosynthesis from lanosterol in mammals to produce 24(25)-dihydrosterols ?
-
 ?
1.3.1.72 additional information Rattus norvegicus C-24 reduction of sterols probably takes place straight after sterol DELTA8-7 isomerization of zymosterol, which occurs several steps after C-32 demethylation of lanosterol in the 19-step pathway of cholesterol biosynthesis from lanosterol ?
-
 ?
1.3.1.72 additional information Rattus norvegicus cholesterogenic enzyme ?
-
 ?
1.3.1.72 additional information Rattus norvegicus important enzyme in the 19-step pathway of cholesterol biosynthesis from lanosterol ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.3.1.72 Rattus norvegicus
-
 male sprague-dawley rats
-

Reaction

EC Number Reaction Comment Organism Reaction ID
1.3.1.72 5alpha-cholest-7-en-3beta-ol + NADP+ = 5alpha-cholesta-7,24-dien-3beta-ol + NADPH + H+ anaerobic reduction of 24(25)-enes of lanosterol and other obligatory intermediates of cholesterol biosynthesis from lanosterol Rattus norvegicus
a
1.3.1.72 5alpha-cholest-7-en-3beta-ol + NADP+ = 5alpha-cholesta-7,24-dien-3beta-ol + NADPH + H+ regulation, enzyme induction, dietary induction Rattus norvegicus
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.3.1.72 hepatocyte
-
 Rattus norvegicus
-
1.3.1.72 liver
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.3.1.72 additional information
-
-
 Rattus norvegicus
1.3.1.72 0.0015
-
 substrate: 5alpha-cholesta-7,24-dien-3beta-ol Rattus norvegicus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.1.72 4,4-dimethyl-5alpha-cholesta-8,24-dien-3beta-ol + NADPH
-
 Rattus norvegicus 4,4-dimethyl-5alpha-cholesta-8-en-3beta-ol + NADP+
-
 ?
1.3.1.72 5alpha-cholesta-7,24-dien-3beta-ol + NADPH most reactive, best substrate, 17.8fold activity compared with lanosterol, 4,4',14alpha-trimethyl-5alpha-cholesta-8,24-dien-3beta-ol Rattus norvegicus 5alpha-cholesta-7-en-3beta-ol + NADP+ lathosterol ?
1.3.1.72 5alpha-cholesta-7,24-dien-3beta-ol + NADPH C-24 reduction of sterols probably takes place straight after sterol DELTA8-7 isomerization of zymosterol, which occurs several steps after C-32 demethylation of lanosterol in the 19-step pathway of cholesterol biosynthesis from lanosterol Rattus norvegicus 5alpha-cholesta-7-en-3beta-ol + NADP+
-
 ?
1.3.1.72 5alpha-cholesta-7,24-dien-3beta-ol + NADPH C-24 reduction of DELTA7,24-diene Rattus norvegicus 5alpha-cholesta-7-en-3beta-ol + NADP+
-
 ?
1.3.1.72 5alpha-cholesta-7,24-dien-3beta-ol + NADPH most reactive, probably natural substrate Rattus norvegicus 5alpha-cholesta-7-en-3beta-ol + NADP+
-
 ?
1.3.1.72 cholesta-5,7,24-trien-3beta-ol + NADPH + H+
-
 Rattus norvegicus cholesta-5,7-dien-3beta-ol + NADP+
-
 ?
1.3.1.72 desmosterol + NADPH 5.5fold activity compared with lanosterol, 4,4',14alpha-trimethyl-5alpha-cholesta-8,24-dien-3beta-ol Rattus norvegicus cholesterol + NADP+
-
 ?
1.3.1.72 desmosterol + NADPH 5alpha-cholesta-5,24-dien-3beta-ol Rattus norvegicus cholesterol + NADP+
-
 ?
1.3.1.72 lanosterol + NADPH 14alpha-methyl demethylase activity is dominant over 24-reductase activity, and blockade or removal of 14alpha-methyl demethylase activity is absolutely required for the detection of maximal 24-reductase activity when lanosterol substrate is present Rattus norvegicus 4,4,14alpha-trimethyl-5alpha-cholesta-8-en-3beta-ol + NADP+
-
 ?
1.3.1.72 lanosterol + NADPH 4,4',14alpha-trimethyl-5alpha-cholesta-8,24-dien-3beta-ol Rattus norvegicus 4,4,14alpha-trimethyl-5alpha-cholesta-8-en-3beta-ol + NADP+
-
 ?
1.3.1.72 additional information substrate specificity Rattus norvegicus ?
-
 ?
1.3.1.72 additional information anaerobic reduction of 24(25)-enes of lanosterol and other obligatory intermediates of cholesterol biosynthesis from lanosterol in mammals to produce 24(25)-dihydrosterols Rattus norvegicus ?
-
 ?
1.3.1.72 additional information C-24 reduction of sterols probably takes place straight after sterol DELTA8-7 isomerization of zymosterol, which occurs several steps after C-32 demethylation of lanosterol in the 19-step pathway of cholesterol biosynthesis from lanosterol Rattus norvegicus ?
-
 ?
1.3.1.72 additional information substrate specificity studies Rattus norvegicus ?
-
 ?
1.3.1.72 additional information cholesterogenic enzyme Rattus norvegicus ?
-
 ?
1.3.1.72 additional information important enzyme in the 19-step pathway of cholesterol biosynthesis from lanosterol Rattus norvegicus ?
-
 ?
1.3.1.72 zymosterol + NADPH 6.1fold activity compared with lanosterol, 4,4',14alpha-trimethyl-5alpha-cholesta-8,24-dien-3beta-ol Rattus norvegicus 5alpha-cholesta-8-en-3beta-ol + NADP+
-
 ?
1.3.1.72 zymosterol + NADPH 5alpha-cholesta-8,24-dien-3beta-ol Rattus norvegicus 5alpha-cholesta-8-en-3beta-ol + NADP+
-
 ?

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.3.1.72 37
-
 assay at, anaerobically Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.3.1.72 6.2
-
 assay at, anaerobically Rattus norvegicus
1.3.1.72 6.5
-
-
 Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
1.3.1.72 NADPH
-
 Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.3.1.72 0.000157
-
 3-beta-(2-(diethylamino)ethoxy)androst-5-en-17-one
-
 Rattus norvegicus
1.3.1.72 0.000523
-
 Triparanol
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.1.72 0.00015
-
 U18666A, non-competitive inhibition, Ki: 0.000157 mM, IC50 about 0.00015 mM, 690fold higher affinity for the enzyme than substrate lanosterol Rattus norvegicus 3-beta-(2-(diethylamino)ethoxy)androst-5-en-17-one
1.3.1.72 0.0008
-
 non-competitive inhibition, specific inhibitor, Ki: 0.000523 mM, IC50 about 0.0008 mM, 208fold higher affinity for the enzyme than substrate lanosterol Rattus norvegicus Triparanol