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Literature summary extracted from

  • Bourne, Y.; Radic, Z.; Sulzenbacher, G.; Kim, E.; Taylor, P.; Marchot, P.
    Substrate and product trafficking through the active center gorge of acetylcholinesterase analyzed by crystallography and equilibrium binding (2006), J. Biol. Chem., 281, 29256-29267.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.1.7 expression of soluble wild-type and mutant enzymes in HEK-293 cells Mus musculus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.1.1.7 purified wild-type enzyme and mutant S203A in complex with substrates acetylcholine, acetylthiocholine, succinyldicholine, and butyrylthiocholine, and two nonhydrolyzable substrate analogues (m-N,N,N-trimethylammonio)-trifluoroacetophenone and 4-ketoamyltrimethylammonium, by hanging drop vapor diffusion at 4°C, using a protein-to-well solution ratio of 1:1, with well solution containing 25–32% v/v P550MME or P600 in either 60-100 mM HEPES or sodium acetate, pH 6.5-pH 8.0, he TMTFA-mAChE complex is formed in solution using apo-mAChE at 5.0 mg/ml, and a 3-fold molar excess of the ligand over the enzyme, concentrated prior to crystallization, the other seven complexes are generated by crystal soaking, carried out at 4 °C in 0.02 ml sitting drops made of well solution supplemented with the 250 mM ligand and polyethylene glycol up to 35%, X-ray diffraction structure determination and anaylsis at 2.05-2.65 A resolution Mus musculus

Protein Variants

EC Number Protein Variants Comment Organism
3.1.1.7 S203A site-directed mutagenesis of the catalytic site residue, inactive mutant Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.7 4-ketoamyltrimethylammonium binding structure analysis Mus musculus
3.1.1.7 choline product inhibition, binding structure analysis Mus musculus
3.1.1.7 m-(N,N,N-trimethylammonio)-trifluoroacetophenone binding structure analysis Mus musculus
3.1.1.7 succinyldicholine substrate inhibition, binding structure analysis Mus musculus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.7 additional information
-
 additional information ligand binding kinetics, overview Mus musculus
3.1.1.7 0.046
-
 acetylthiocholine pH 7.0, 22°C, recombinant wild-type enzyme Mus musculus
3.1.1.7 0.093
-
 butyrylthiocholine pH 7.0, 22°C, recombinant wild-type enzyme Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.1.7 acetylcholine + H2O Mus musculus
-
 choline + acetate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.7 Mus musculus P21836
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.1.7 recombinant soluble wild-type and mutant enzymes from HEK-293 cells by by affinity chromatography with elution using either propidium diiodide or SCh dichloride, followed by dialysis Mus musculus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.7 acetylcholine + H2O
-
 Mus musculus choline + acetate
-
 ?
3.1.1.7 acetylthiocholine + H2O
-
 Mus musculus thiocholine + acetate
-
 ?
3.1.1.7 butyrylthiocholine + H2O
-
 Mus musculus thiocholine + butyrate
-
 ?
3.1.1.7 additional information substrate and product trafficking through the active center gorge of the enzyme analyzed by crystallography and equilibrium binding, binding structures, overview Mus musculus ?
-
 ?
3.1.1.7 succinyldicholine + H2O
-
 Mus musculus 2 choline + succinate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.7 AChE
-
 Mus musculus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.1.7 22
-
 assay at Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.1.7 7
-
 assay at Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.1.7 0.021
-
 succinyldicholine pH 7.0, 22°C, recombinant wild-type enzyme Mus musculus
3.1.1.7 0.023
-
 4-ketoamyltrimethylammonium pH 7.0, 22°C, recombinant wild-type enzyme Mus musculus
3.1.1.7 1.4
-
 choline pH 7.0, 22°C, recombinant wild-type enzyme Mus musculus