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Literature summary for 1.14.14.154 extracted from

  • Friggeri, L.; Hargrove, T.Y.; Rachakonda, G.; Williams, A.D.; Wawrzak, Z.; Di Santo, R.; De Vita, D.; Waterman, M.R.; Tortorella, S.; Villalta, F.; Lepesheva, G.I.
    Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14alpha-demethylase two regions of the enzyme molecule potentiate its inhibition (2014), J. Med. Chem., 57, 6704-6717 .
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine Chagas disease is caused by the protozoan parasite Trypanosoma cruzi, which depends on the production of endogenous sterols, and therefore can be blocked by sterol 14alpha-demethylase inhibitors Trypanosoma cruzi
pharmacology Chagas disease is caused by the protozoan parasite Trypanosoma cruzi, which depends on the production of endogenous sterols, and therefore can be blocked by sterol 14alpha-demethylase inhibitors Trypanosoma cruzi

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli strain HMS174(DE3) Trypanosoma cruzi

Crystallization (Commentary)

Crystallization (Comment) Organism
for crystallization purposes, an N-terminal truncated construct is used where the membrane anchor sequence is replaced with the 5-amino acid sequence fragment MAKKT-. Crystals are grown at 23°C using the hanging-drop vapor diffusion method Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
(R)-N-(1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)-benzamide
-
Trypanosoma cruzi
(R)-N-(2-(1H-imidazol-1-yl)-1-phenylethyl)-4'-chlorobiphenyl-4-carboxamide
-
Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi Q7Z1V1
-
-
Trypanosoma cruzi CL Brener Q7Z1V1
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
eburicol + [reduced NADPH-hemoprotein reductase] + O2
-
Trypanosoma cruzi ?
-
?
eburicol + [reduced NADPH-hemoprotein reductase] + O2
-
Trypanosoma cruzi CL Brener ?
-
?

Synonyms

Synonyms Comment Organism
CYP51
-
Trypanosoma cruzi

Cofactor

Cofactor Comment Organism Structure
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._ Trypanosoma cruzi