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

BRENDA support

Literature summary for 1.14.14.154 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
Search for more literature for 1.14.14.154

Application

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

Inhibitors

Inhibitors Comment Organism Structure
1-(phenethyl(propyl)amino)-3-(pyridin-3-yloxy)propan-2-ol
-
 Homo sapiens
2-(2-(naphthalen-2-yl)ethyl](propyl)amino]-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(2-chlorophenethyl(propyl)amino)-1-(pyridin-4-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(3,4-dichlorophenethyl(methyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(3,4-dichlorophenethyl(methyl)amino)-1-(pyridin-4-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(3,4-dichlorophenethyl(propyl)amino)-1-(4-methylpyridin-2-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(3,4-dichlorophenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(3,4-dichlorophenethyl(propyl)amino)-1-phenylethanol
-
 Homo sapiens
2-(3,4-difluorophenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(3,4-dimethoxyphenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(4-chlorophenethyl(propyl)amino)-1-(pyridin-4-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(4-nitrophenethyl(propyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(phenethyl(propyl)amino)-1-(pyridin-3-yl) ethanol dihydrobromide
-
 Homo sapiens
2-(propyl(2-(trifluoromethyl)phenethyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-(propyl(4-(trifluoromethyl)phenethyl)amino)-1-(pyridin-3-yl)ethanol dihydrobromide
-
 Homo sapiens
2-{propyl[2-(pyridin-3-yl)ethyl]amino}-1-(pyridin-3-yl)ethanol
-
 Homo sapiens
4-(2-(2-hydroxy-2-(pyridin-3-yl)ethyl)(propyl)amino)ethylbenzene-1,2-diol dihydrobromide
-
 Homo sapiens
fluconazole
-
 Homo sapiens
ketoconazole
-
 Homo sapiens
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

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

Metals/Ions

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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
-
 ?
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
-
 ?
additional information Homo sapiens the enzyme catalyzes a step in the cholesterol biosynthesis via the mevalonate pathway, overview ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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
-
 ?
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
-
 ?
additional information the enzyme catalyzes a step in the cholesterol biosynthesis via the mevalonate pathway, overview Homo sapiens ?
-
 ?
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

Synonyms Comment Organism
CYP51
-
 Homo sapiens
lanosterol 14alpha-demethylase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
cytochrome P450 a cytochrome P450 enzyme Homo sapiens