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Literature summary extracted from

  • Lepesheva, G.I.; Zaitseva, N.G.; Nes, W.D.; Zhou, W.; Arase, M.; Liu, J.; Hill, G.C.; Waterman, M.R.
    CYP51 from Trypanosoma cruzi: a phyla-specific residue in the B helix defines substrate preferences of sterol 14alpha-demethylase (2006), J. Biol. Chem., 281, 3577-3585.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.14.14.154 medicine the enzyme is a potential drug target for treatment of Chagas disease Trypanosoma cruzi

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.14.154 gene CYP51, DNA and amino acid sequence determination and analysis, sequence comparisons, phylogenetic analysis, expression of His-tagged enzyme in Escherichia coli Trypanosoma cruzi

Protein Variants

EC Number Protein Variants Comment Organism
1.14.14.154 I105F sited-directed mutagenesis, exchange of the animal/fungi-like I105 B' helix residue for the F105 found in this position in all plant and the other six CYP51 sequences from Trypanosomatidae dramatically alters the mutant substrate specificity, activity with C4-methylsterol substrate is 3.5fold reduced and activity with norlanosterol and obtusifoliol is increased 150fold and 60fold, respectively, overview Trypanosoma cruzi

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.154 14alpha-aminomethyl-lanosterol derivatives competitive Trypanosoma cruzi
1.14.14.154 fluconazole and analogues Trypanosoma cruzi
1.14.14.154 additional information inhibition kinetics and mechanism Trypanosoma cruzi

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.14.154 membrane
-
Trypanosoma cruzi 16020
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.14.14.154 Iron a heme iron, DELTA7–8 double bond location is more favorable for coordination of the amino nitrogen to the heme iron Trypanosoma cruzi

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 Trypanosoma cruzi
-
?
-
?
1.14.14.154 24-methylenedihydrolanosterol + [reduced NADPH-hemoprotein reductase] + O2 Trypanosoma cruzi
-
?
-
?
1.14.14.154 lanosterol + [reduced NADPH-hemoprotein reductase] + O2 Trypanosoma cruzi
-
?
-
?
1.14.14.154 norlanosterol + [reduced NADPH-hemoprotein reductase] + O2 Trypanosoma cruzi i.e. 4alpha,4alpha-dimethylcholesta-8,24-dien-3beta-ol ?
-
?
1.14.14.154 obtusifoliol + [reduced NADPH-hemoprotein reductase] + O2 Trypanosoma cruzi preferred substrate 4alpha-methyl-5alpha-ergost-8,14,24(28)-trien-3beta-ol + formate + [oxidized NADPH-hemoprotein reductase] + H2O
-
?

Organism

EC Number Organism UniProt Comment Textmining
1.14.14.154 Trypanosoma cruzi Q7Z1V1 gene CYP51
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.14.14.154 recombinant His-tagged enzyme from Escherichia coli by nickel affinity chromatography, and anion and cation exchange chromatography Trypanosoma cruzi

Reaction

EC Number Reaction Comment Organism Reaction ID
1.14.14.154 a 14alpha-methylsteroid + 3 [reduced NADPH-hemoprotein reductase] + 3 O2 = a DELTA14-steroid + formate + 3 [oxidized NADPH-hemoprotein reductase] + 4 H2O reaction mechanism, phyla-specific residues in CYP51 Trypanosoma cruzi

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.14.14.154 additional information
-
substrate specificities of recombinant wild-type and mutant I105F enzymes, overview Trypanosoma cruzi

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
-
Trypanosoma cruzi ?
-
?
1.14.14.154 24-methylenedihydrolanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Trypanosoma cruzi ?
-
?
1.14.14.154 lanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
Trypanosoma cruzi ?
-
?
1.14.14.154 additional information substrate specificity, the Trypanosoma cruzi enzyme prefers C4-dimethylsterols substrates, overview Trypanosoma cruzi ?
-
?
1.14.14.154 norlanosterol + [reduced NADPH-hemoprotein reductase] + O2 i.e. 4alpha,4alpha-dimethylcholesta-8,24-dien-3beta-ol Trypanosoma cruzi ?
-
?
1.14.14.154 obtusifoliol + [reduced NADPH-hemoprotein reductase] + O2 preferred substrate Trypanosoma cruzi 4alpha-methyl-5alpha-ergost-8,14,24(28)-trien-3beta-ol + formate + [oxidized NADPH-hemoprotein reductase] + H2O
-
?

Synonyms

EC Number Synonyms Comment Organism
1.14.14.154 CYP51
-
Trypanosoma cruzi
1.14.14.154 sterol 14alpha-demethylase
-
Trypanosoma cruzi