BRENDA - Enzyme Database
show all sequences of 1.14.13.70

Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14alpha-demethylase two regions of the enzyme molecule potentiate its inhibition

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.; J. Med. Chem. 57, 6704-6717 (2014)

Data extracted from this reference:

Application
Application
Commentary
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 (Commentary)
Organism
expression in Escherichia coli strain HMS174(DE3)
Trypanosoma cruzi
Crystallization (Commentary)
Crystallization (Commentary)
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
Commentary
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
Commentary
Textmining
Trypanosoma cruzi
Q7Z1V1
-
-
Trypanosoma cruzi CL Brener
Q7Z1V1
-
-
Purification (Commentary)
Purification (Commentary)
Organism
-
Trypanosoma cruzi
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
Substrate Product ID
eburicol + NADPH + H+ + O2
-
745522
Trypanosoma cruzi
?
-
-
-
?
eburicol + NADPH + H+ + O2
-
745522
Trypanosoma cruzi CL Brener
?
-
-
-
?
Synonyms
Synonyms
Commentary
Organism
CYP51
-
Trypanosoma cruzi
Application (protein specific)
Application
Commentary
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) (protein specific)
Commentary
Organism
expression in Escherichia coli strain HMS174(DE3)
Trypanosoma cruzi
Crystallization (Commentary) (protein specific)
Crystallization
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 (protein specific)
Inhibitors
Commentary
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
Purification (Commentary) (protein specific)
Commentary
Organism
-
Trypanosoma cruzi
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
ID
eburicol + NADPH + H+ + O2
-
745522
Trypanosoma cruzi
?
-
-
-
?
eburicol + NADPH + H+ + O2
-
745522
Trypanosoma cruzi CL Brener
?
-
-
-
?
Other publictions for EC 1.14.13.70
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Synonyms
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
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-
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5
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1
1
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3
1
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4
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1
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4
4
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3
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1
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5
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1
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3
1
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3
3
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Structural basis for rational ...
Trypanosoma cruzi, Trypanosoma cruzi CL Brener
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57
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2014
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2
1
1
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2
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2
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1
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