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Literature summary for 3.1.1.7 extracted from

  • Ilg, T.; Schmalz, S.; Werr, M.; Cramer, J.
    Acetylcholinesterases of the cat flea Ctenocephalides felis: identification of two distinct genes and biochemical characterization of recombinant and in vivo enzyme activities (2010), Insect Biochem. Mol. Biol., 40, 153-164.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Pichia pastoris and in HEK-293 cells Ctenocephalides felis

Inhibitors

Inhibitors Comment Organism Structure
Carbaryl i.e. N-methyl-1-naphthylcarbamate, complete inhibition at concentrations exceeding 100 nM; i.e. N-methyl-1-naphthylcarbamate, complete inhibition at concentrations exceeding 100 nM Ctenocephalides felis
galanthamine
-
Ctenocephalides felis
propoxur i.e. 2-isopropoxyphenyl-N-methylcarbamate, complete inhibition at concentrations exceeding 100 nM; i.e. 2-isopropoxyphenyl-N-methylcarbamate, complete inhibition at concentrations exceeding 100 nM Ctenocephalides felis
tacrine
-
Ctenocephalides felis

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0158
-
propionylthiocholine isoform AChE2, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis
0.0243
-
acetylthiocholine isoform AChE2, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis
0.0244
-
butyrylthiocholine isoform AChE2, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis
0.0376
-
propionylthiocholine isoform AChE1, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis
0.0484
-
acetylthiocholine isoform AChE1, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis
0.0684
-
butyrylthiocholine isoform AChE1, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis

Localization

Localization Comment Organism GeneOntology No. Textmining
cell surface isoform AChE1 possesses glycosylphosphatidylinositol membrane anchors and are transported to the cell surface Ctenocephalides felis 9986
-
cell surface isoform AChE2 possesses glycosylphosphatidylinositol membrane anchors and is transported to the cell surface Ctenocephalides felis 9986
-
membrane the majority (81%) of the AChE activity in fleas is membrane-bound Ctenocephalides felis 16020
-

Organism

Organism UniProt Comment Textmining
Ctenocephalides felis D2U6X5 cat flea
-
Ctenocephalides felis D2U6X6 cat flea
-

Purification (Commentary)

Purification (Comment) Organism
Ni2+-NTA agarose column chromatography Ctenocephalides felis

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Ctenocephalides felis thiocholine + acetate
-
?
butyrylthiocholine + H2O
-
Ctenocephalides felis thiocholine + butyrate
-
?
additional information isoform AChE1 is the dominant activity in Ctenocephalides felis imagoes Ctenocephalides felis ?
-
?
propionylthiocholine + H2O
-
Ctenocephalides felis thiocholine + propionate
-
?

Synonyms

Synonyms Comment Organism
AChE1 isoform Ctenocephalides felis
AChE2 isoform Ctenocephalides felis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000009
-
isoform AChE2, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis Carbaryl
0.000012
-
isoform AChE2, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis propoxur
0.000024
-
isoform AChE1, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis propoxur
0.000038
-
isoform AChE1, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis Carbaryl
0.000126
-
isoform AChE1, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis tacrine
0.00208
-
isoform AChE2, in 10 mM Na2HPO4/NaH2PO4, pH 7.4, pH, at 22°C Ctenocephalides felis tacrine