Literature summary for 1.14.14.74 extracted from

Lee, E.; Kim, J.H.; Shon, J.C.; Wu, Z.; Kim, H.J.; Gim, M.; Lee, T.; Liu, K.H.
Terfenadone is a strong inhibitor of CYP2J2 present in the human liver and intestinal microsomes (2018), Drug Metab. Pharmacokinet., 33, 159-163 .

Search for more literature for 1.14.14.74

Cloned(Commentary)

Cloned (Comment)	Organism
coexpression with NADPH-cytochrome P450 reductase in Sf9 cells	Homo sapiens

Protein Variants

Protein Variants	Comment	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	Comment	Organism	Structure
danazol	-	Homo sapiens
hydroxyebastine	-	Homo sapiens
telmisartan	-	Homo sapiens
terfenadone	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P51589	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
liver	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
albendazole + [reduced NADPH-hemoprotein reductase] + O2	-	Homo sapiens	4'-hydroxyalbendazole + [oxidized NADPH-hemoprotein reductase] + H2O	-	?
astemizole + [reduced NADPH-hemoprotein reductase] + O2	-	Homo sapiens	hydroxyastemizole + [oxidized NADPH-hemoprotein reductase] + H2O	-	?
ebastine + [reduced NADPH-hemoprotein reductase] + O2	-	Homo sapiens	hydroxyebastine + [oxidized NADPH-hemoprotein reductase] + H2O	-	?
terfenadine + [reduced NADPH-hemoprotein reductase] + O2	-	Homo sapiens	terfenadine alcohol + [oxidized NADPH-hemoprotein reductase] + H2O	-	?

Synonyms

Synonyms	Comment	Organism
CYP2J2	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00015	-	substrate astemizole, liver microsome, pH 7.4, 37°C	Homo sapiens	terfenadone
0.00031	-	substrate albendazole, liver microsome, pH 7.4, 37°C	Homo sapiens	terfenadone
0.00195	-	substrate ebastine, liver microsome, pH 7.4, 37°C	Homo sapiens	danazol
0.0021	-	substrate terfenadine, liver microsome, pH 7.4, 37°C	Homo sapiens	terfenadone
0.00214	-	substrate terfenadine, liver microsome, pH 7.4, 37°C	Homo sapiens	danazol
0.004	-	substrate terfenadine, liver microsome, pH 7.4, 37°C	Homo sapiens	hydroxyebastine
0.00427	-	substrate ebastine, liver microsome, pH 7.4, 37°C	Homo sapiens	terfenadone
0.00928	-	substrate astemizole, liver microsome, pH 7.4, 37°C	Homo sapiens	hydroxyebastine
0.0111	-	substrate albendazole, liver microsome, pH 7.4, 37°C	Homo sapiens	hydroxyebastine
0.0138	-	substrate albendazole, liver microsome, pH 7.4, 37°C	Homo sapiens	danazol
0.0183	-	substrate astemizole, liver microsome, pH 7.4, 37°C	Homo sapiens	danazol
0.0238	-	substrate terfenadine, liver microsome, pH 7.4, 37°C	Homo sapiens	telmisartan
0.0472	-	substrate albendazole, liver microsome, pH 7.4, 37°C	Homo sapiens	telmisartan

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Release 2023.1 (January 2023)