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Literature summary extracted from

  • Korosec, T.; Acimovic, J.; Seliskar, M.; Kocjan, D.; Tacer, K.F.; Rozman, D.; Urleb, U.
    Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51) (2008), Bioorg. Med. Chem., 16, 209-221.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.14.14.154 drug development CYP51 is a potential anticholesterolemic drug target Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.154 1-(phenethyl(propyl)amino)-3-(pyridin-3-yloxy)propan-2-ol
-
Homo sapiens
1.14.14.154 2-(2-(naphthalen-2-yl)ethyl](propyl)amino]-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(2-chlorophenethyl(propyl)amino)-1-(pyridin-4-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(3,4-dichlorophenethyl(methyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(3,4-dichlorophenethyl(methyl)amino)-1-(pyridin-4-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(3,4-dichlorophenethyl(propyl)amino)-1-(4-methylpyridin-2-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(3,4-dichlorophenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(3,4-dichlorophenethyl(propyl)amino)-1-phenylethanol
-
Homo sapiens
1.14.14.154 2-(3,4-difluorophenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(3,4-dimethoxyphenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(4-chlorophenethyl(propyl)amino)-1-(pyridin-4-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(4-nitrophenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(phenethyl(propyl)amino)-1-(pyridin-3-yl) ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(propyl(2-(trifluoromethyl)phenethyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-(propyl(4-(trifluoromethyl)phenethyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
Homo sapiens
1.14.14.154 2-{propyl[2-(pyridin-3-yl)ethyl]amino}-1-(pyridin-3-yl)ethanol
-
Homo sapiens
1.14.14.154 4-(2-(2-hydroxy-2-(pyridin-3-yl)ethyl)(propyl)amino)ethylbenzene-1,2-diol dihydrobromide
-
Homo sapiens
1.14.14.154 fluconazole
-
Homo sapiens
1.14.14.154 ketoconazole
-
Homo sapiens
1.14.14.154 additional information structure–activity relationship study of enzyme-ligand binding, pyridine binds within the heme binding pocket in an analogy with azoles, overview Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.14.154 endoplasmic reticulum
-
Homo sapiens 5783
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.14.14.154 Fe2+ a cytochrome P450 enzyme Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.14.154 24,25-dihydrolanosterol + [reduced NADPH-hemoprotein reductase] + O2 Homo sapiens
-
(3beta,5alpha)-4,4-dimethylcholesta-8,14-dien-3-ol + formate + [oxidized NADPH-hemoprotein reductase] + H2O
-
?
1.14.14.154 lanosterol + [reduced NADPH-hemoprotein reductase] + O2 Homo sapiens
-
4,4-dimethyl-5alpha-cholesta-8,14,24-trien-3beta-ol + formate + [oxidized NADPH-hemoprotein reductase] + H2O
-
?
1.14.14.154 additional information Homo sapiens the enzyme catalyzes a step in the cholesterol biosynthesis via the mevalonate pathway, overview ?
-
?

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.14.154 Hep-G2 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.154 24,25-dihydrolanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Homo sapiens (3beta,5alpha)-4,4-dimethylcholesta-8,14-dien-3-ol + formate + [oxidized NADPH-hemoprotein reductase] + H2O
-
?
1.14.14.154 lanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Homo sapiens 4,4-dimethyl-5alpha-cholesta-8,14,24-trien-3beta-ol + formate + [oxidized NADPH-hemoprotein reductase] + H2O
-
?
1.14.14.154 additional information the enzyme catalyzes a step in the cholesterol biosynthesis via the mevalonate pathway, overview Homo sapiens ?
-
?
1.14.14.154 additional information structure-activity relationship study of enzyme-ligand binding, pyridine binds within the heme binding pocket in an analogy with azoles, overview Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
1.14.14.154 CYP51
-
Homo sapiens
1.14.14.154 lanosterol 14alpha-demethylase
-
Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.14.14.154 cytochrome P450 a cytochrome P450 enzyme Homo sapiens