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Literature summary extracted from

  • Hargrove, T.Y.; Friggeri, L.; Wawrzak, Z.; Qi, A.; Hoekstra, W.J.; Schotzinger, R.J.; York, J.D.; Guengerich, F.P.; Lepesheva, G.I.
    Structural analyses of Candida albicans sterol 14alpha-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis (2017), J. Biol. Chem., 292, 6728-6743 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.14.154 expression in Escherichia coli Candida albicans

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.14.14.154 crystals are grown using a hanging drop vapor diffusion technique. Enzyme complexes with posaconazole and VT-1161 are crystallized in the monoclinic C121 space group, and the structures are refined to 2.86 and 2.0 A. X-ray structures of Candida albicans CYP51 complexes with posaconazole and VT-1161, providing a molecular mechanism for the potencies of these drugs Candida albicans

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.154 (R)-2-(2,4-difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)propan-2-ol i.e. oteseconazole, i.e. VT-1161. 98% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
1.14.14.154 clotrimazole 78% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
1.14.14.154 fluconazole 54% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
1.14.14.154 itraconazole 91% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
1.14.14.154 ketoconazole 85% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
1.14.14.154 miconazole 79% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
1.14.14.154 posaconazole 98% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
1.14.14.154 voriconazole 84% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.14.14.154 0.0063
-
 lanosterol pH and temperature not specified in the publication Candida albicans

Organism

EC Number Organism UniProt Comment Textmining
1.14.14.154 Candida albicans Q9P4W0
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.14.14.154
-
 Candida albicans

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.154 lanosterol + [reduced NADPH-hemoprotein reductase] + O2
-
 Candida albicans ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.14.154 CYP51
-
 Candida albicans

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.14.14.154 0.55
-
 lanosterol pH and temperature not specified in the publication Candida albicans

Cofactor

EC Number Cofactor Comment Organism Structure
1.14.14.154 cytochrome P-450
-
 Candida albicans
1.14.14.154 NADPH-hemoprotein reductase A flavoprotein containing both FMN and FAD. This enzyme catalyses the transfer of electrons from NADPH, an obligatory two-electron donor, to microsomal P-450 monooxygenases, EC 1.14.14._ Candida albicans

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.14.14.154 87.3
-
 lanosterol pH and temperature not specified in the publication Candida albicans