BRENDA - Enzyme Database show
show all sequences of 1.14.14.74

Terfenadone is a strong inhibitor of CYP2J2 present in the human liver and intestinal microsomes

Lee, E.; Kim, J.H.; Shon, J.C.; Wu, Z.; Kim, H.J.; Gim, M.; Lee, T.; Liu, K.H.; Drug Metab. Pharmacokinet. 33, 159-163 (2018)

Data extracted from this reference:

Cloned(Commentary)
Commentary
Organism
coexpression with NADPH-cytochrome P450 reductase in Sf9 cells
Homo sapiens
Engineering
Amino acid exchange
Commentary
Organism
G312R
natural genetic variant, almost complete loss of enzymatic activity. Loss of CO binding to the heme, molecular modelling predicts a spatial hindrance between heme and the bulky side chain of the R312 residue in G312R
Homo sapiens
additional information
identification of 12 genetic variations from 93 Korean subjects
Homo sapiens
P351L
natural genetic variant, activity similar to wild-type
Homo sapiens
Inhibitors
Inhibitors
Commentary
Organism
Structure
danazol
-
Homo sapiens
hydroxyebastine
-
Homo sapiens
telmisartan
-
Homo sapiens
terfenadone
-
Homo sapiens
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
P51589
-
-
Source Tissue
Source Tissue
Commentary
Organism
Textmining
liver
-
Homo sapiens
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
albendazole + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
4'-hydroxyalbendazole + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
astemizole + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
hydroxyastemizole + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
ebastine + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
hydroxyebastine + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
terfenadine + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
terfenadine alcohol + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.00015
-
substrate astemizole, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00031
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00195
-
substrate ebastine, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.0021
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00214
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.004
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
hydroxyebastine
0.00427
-
substrate ebastine, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00928
-
substrate astemizole, liver microsome, pH 7.4, 37C
Homo sapiens
hydroxyebastine
0.0111
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
hydroxyebastine
0.0138
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.0183
-
substrate astemizole, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.0238
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
telmisartan
0.0472
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
telmisartan
Cloned(Commentary) (protein specific)
Commentary
Organism
coexpression with NADPH-cytochrome P450 reductase in Sf9 cells
Homo sapiens
Engineering (protein specific)
Amino acid exchange
Commentary
Organism
G312R
natural genetic variant, almost complete loss of enzymatic activity. Loss of CO binding to the heme, molecular modelling predicts a spatial hindrance between heme and the bulky side chain of the R312 residue in G312R
Homo sapiens
additional information
identification of 12 genetic variations from 93 Korean subjects
Homo sapiens
P351L
natural genetic variant, activity similar to wild-type
Homo sapiens
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.00015
-
substrate astemizole, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00031
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00195
-
substrate ebastine, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.0021
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00214
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.004
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
hydroxyebastine
0.00427
-
substrate ebastine, liver microsome, pH 7.4, 37C
Homo sapiens
terfenadone
0.00928
-
substrate astemizole, liver microsome, pH 7.4, 37C
Homo sapiens
hydroxyebastine
0.0111
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
hydroxyebastine
0.0138
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.0183
-
substrate astemizole, liver microsome, pH 7.4, 37C
Homo sapiens
danazol
0.0238
-
substrate terfenadine, liver microsome, pH 7.4, 37C
Homo sapiens
telmisartan
0.0472
-
substrate albendazole, liver microsome, pH 7.4, 37C
Homo sapiens
telmisartan
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
danazol
-
Homo sapiens
hydroxyebastine
-
Homo sapiens
telmisartan
-
Homo sapiens
terfenadone
-
Homo sapiens
Source Tissue (protein specific)
Source Tissue
Commentary
Organism
Textmining
liver
-
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
albendazole + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
4'-hydroxyalbendazole + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
astemizole + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
hydroxyastemizole + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
ebastine + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
hydroxyebastine + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
terfenadine + [reduced NADPH-hemoprotein reductase] + O2
-
744774
Homo sapiens
terfenadine alcohol + [oxidized NADPH-hemoprotein reductase] + H2O
-
-
-
?
Other publictions for EC 1.14.14.74
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
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)
744774
Lee
Terfenadone is a strong inhib ...
Homo sapiens
Drug Metab. Pharmacokinet.
33
159-163
2018
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744049
Wu
CYP2J2 and CYP2C19 are the ma ...
Homo sapiens
Antimicrob. Agents Chemother.
57
5448-5456
2013
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