Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.14.14.1 extracted from

  • Nair, P.C.; Gillani, T.B.; Rawling, T.; Murray, M.
    Differential inhibition of human CYP2C8 and molecular docking interactions elicited by sorafenib and its major N-oxide metabolite (2021), Chem. Biol. Interact., 338, 109401 .
    View publication on PubMed
Search for more literature for 1.14.14.1

Inhibitors

Inhibitors Comment Organism Structure
sorafenib
-
 Homo sapiens
sorafenib N-oxide both sorafenib and sorafenib N-oxide interacts with active site residues in CYP2C8, but four additional major hydrogen and halogen bonding interactions are identified between sorafenib N-oxide and amino acids in the B-B' loop region and helixes F' and I of the the catalytic region Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P10632 isoform CYP2C8
-
Homo sapiens P11712 isoform CYP2C9
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
losartan + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens ? + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
paclitaxel + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens 6alpha-hydroxypaclitaxel + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

Synonyms

Synonyms Comment Organism
CYP2C8
-
 Homo sapiens
CYP2C9
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.014
-
 pH 7.4, 37°C Homo sapiens sorafenib N-oxide
0.036
-
 pH 7.4, 37°C Homo sapiens sorafenib
0.04
-
 pH 7.4, 37°C Homo sapiens sorafenib N-oxide
0.051
-
 pH 7.4, 37°C Homo sapiens sorafenib