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Literature summary for 3.1.1.7 extracted from

  • Poyot, T.; Nachon, F.; Froment, M.; Loiodice, M.; Wieseler, S.; Schopfer, L.M.; Lockridge, O.; Masson, P.
    Mutant of Bungarus fasciatus acetylcholinesterase with low affinity and low hydrolase activity toward organophosphorus esters (2006), Biochim. Biophys. Acta, 1764, 1470-1478.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
stable expression of mutant enzyme in CHO cells Homo sapiens
stable expression of wild-type and mutant enzymes in CHO-K1 cells Bungarus fasciatus

Protein Variants

Protein Variants Comment Organism
G117H site-directed mutagenesis, the mutant enzyme hydrolyzes organophosphorous compounds in contrast to the wild-type enzyme Homo sapiens
G122H/Y124Q/S125T site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme, but does not show substrate inhibition up to 80 mM acetylthiocholine concentration, the mutant enzyme hydrolyzes organophosphorous compounds in contrast to the wild-type enzyme Bungarus fasciatus

Inhibitors

Inhibitors Comment Organism Structure
chlorpyrifos-oxon complete inhibition of wild-type enzyme Bungarus fasciatus
demeton complete inhibition of wild-type enzyme Bungarus fasciatus
diisopropyl phosphofluoridate complete inhibition of wild-type enzyme, not of mutant G122H/Y124Q/S125T Bungarus fasciatus
Echothiophate complete inhibition of wild-type enzyme, not of mutant G122H/Y124Q/S125T Bungarus fasciatus
additional information inhibition mechanism, overview Bungarus fasciatus
paraoxon complete inhibition of wild-type enzyme, not of mutant G122H/Y124Q/S125T Bungarus fasciatus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics, wild-type and mutant enzymes Bungarus fasciatus
0.052
-
acetylthiocholine pH 7.0, 25°C, wild-type enzyme Bungarus fasciatus
34
-
acetylthiocholine pH 7.0, 25°C, mutant G122H/Y124Q/S125T Bungarus fasciatus

Organism

Organism UniProt Comment Textmining
Bungarus fasciatus
-
-
-
Homo sapiens
-
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Bungarus fasciatus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Homo sapiens thiocholine + acetate
-
?
acetylthiocholine + H2O
-
Bungarus fasciatus thiocholine + acetate
-
?
diisopropyl phosphofluoridate + H2O mutant G117H, no activity with the wild-type enzyme Homo sapiens ?
-
?
diisopropyl phosphofluoridate + H2O mutant G122H/Y124Q/S125T, no activity with the wild-type enzyme Bungarus fasciatus ?
-
?
echothiophate + H2O mutant G117H, no activity with the wild-type enzyme Homo sapiens ?
-
?
echothiophate + H2O mutant G122H/Y124Q/S125T, no activity with the wild-type enzyme Bungarus fasciatus ?
-
?
paraoxon + H2O mutant G117H, no activity with the wild-type enzyme Homo sapiens diethylphosphate + 4-nitrophenol
-
?
paraoxon + H2O mutant G122H/Y124Q/S125T, no activity with the wild-type enzyme Bungarus fasciatus diethylphosphate + 4-nitrophenol
-
?

Synonyms

Synonyms Comment Organism
AChE
-
Homo sapiens
AChE
-
Bungarus fasciatus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens
25
-
assay at Bungarus fasciatus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
64.8
-
acetylthiocholine pH 7.0, 25°C, mutant G122H/Y124Q/S125T Bungarus fasciatus
293.3
-
acetylthiocholine pH 7.0, 25°C, mutant G122H/Y124Q/S125T Bungarus fasciatus
4417
-
acetylthiocholine pH 7.0, 25°C, wild-type enzyme Bungarus fasciatus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Homo sapiens
7
-
assay at Bungarus fasciatus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics Bungarus fasciatus