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Literature summary for 3.1.1.7 extracted from

  • Bosak, A.; Gazic, I.; Vinkovic, V.; Kovarik, Z.
    Amino acid residues involved in stereoselective inhibition of cholinesterases with bambuterol (2008), Arch. Biochem. Biophys., 471, 72-76.
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
F295L/Y337A site-directed mutagenesis, the mutant an altered inhibition rate with inhibitor bambuterol compared to the wild-type enzyme Mus musculus
F295L/Y337A site-directed mutagenesis, the mutant shows a 13fold increased inhibition rate with inhibitor bambuterol compared to the wild-type enzyme Mus musculus
F296L/F297I/Y337A site-directed mutagenesis, the mutant shows a 14fold decreased inhibition rate with inhibitor bambuterol compared to the wild-type enzyme Mus musculus
F297I/Y337A site-directed mutagenesis, the mutant shows an altered inhibition rate with inhibitor bambuterol compared to the wild-type enzyme Mus musculus
Y124Q site-directed mutagenesis, the mutant shows an altered inhibition rate with inhibitor bambuterol compared to the wild-type enzyme Mus musculus
Y337A site-directed mutagenesis, the mutant shows an altered inhibition rate with inhibitor bambuterol compared to the wild-type enzyme Mus musculus
Y72N/Y124Q/Y337A site-directed mutagenesis, the mutant shows an altered inhibition rate with inhibitor bambuterol compared to the wild-type enzyme Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
bambuterol a specific and stereoselective inhibitor of butyrylcholinesterase, which is about 8000times faster inhibited than acetylcholinesterase. AChE wild-type enzyme, and mutants F297I/Y337A and F295L/F297I/Y337A show a deviation from linearity, either enzymes are inhibited by racemate or enantiomers, indicating the presence of reversible enzyme-inhibitor complex, overview Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus P21836
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Mus musculus acetate + thiocholine
-
?

Synonyms

Synonyms Comment Organism
AChE
-
Mus musculus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Mus musculus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Mus musculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics, wild-type and mutant enzymes, overview Mus musculus