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Literature summary for 3.1.8.1 extracted from

  • Ekinci, D.; Beydemir, S.
    Effect of some analgesics on paraoxonase-1 purified from human serum (2009), J. Enzyme Inhib. Med. Chem., 24, 1034-1039.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
diclofenac sodium uncompetitive inhibition Homo sapiens
indomethacin competitive inhibition Homo sapiens
Ketoprofen noncompetitive inhibition Homo sapiens
lincomycine uncompetitive inhibition, weakest inhibitor Homo sapiens
lornoxicam uncompetitive inhibition, strongest inhibitor Homo sapiens
tenoxicam competitive inhibition Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required for the catalysis Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
by ammonium sulfate fractionation, anion exchange and hydrophobic interaction chromatography, 314.9fold with a yield of 25.3% Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
serum
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
3840
-
in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
paraoxon + H2O
-
Homo sapiens 4-nitrophenol + diethyl phosphate
-
?

Synonyms

Synonyms Comment Organism
paraoxonase-1
-
Homo sapiens
PON1
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.009
-
lornoxicam in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens
0.097
-
indomethacin in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens
0.306
-
tenoxicam in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens
0.805
-
diclofenac sodium in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens
11.12
-
lincomycine in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens
13.01
-
Ketoprofen in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.136
-
in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens lornoxicam
0.195
-
in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens indomethacin
0.34
-
in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens tenoxicam
1.639
-
in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens diclofenac sodium
6.23
-
in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens Ketoprofen
9.638
-
in 50 mM glycine/NaOH, pH 10.5, 1 mM CaCl2, at 25°C Homo sapiens lincomycine