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Literature summary for 1.14.14.154 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
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Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Candida albicans

Crystallization (Commentary)

Crystallization (Comment) Organism
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

Inhibitors Comment Organism Structure
(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
clotrimazole 78% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
fluconazole 54% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
itraconazole 91% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
ketoconazole 85% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
miconazole 79% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
posaconazole 98% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans
voriconazole 84% inhibition, molar ratio of enzyme/inhibitor/lanosterol was 1:2:50 Candida albicans

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Candida albicans Q9P4W0
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Candida albicans

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
CYP51
-
 Candida albicans

Turnover Number [1/s]

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

Cofactor

Cofactor Comment Organism Structure
cytochrome P-450
-
 Candida albicans
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]

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