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Literature summary for 3.1.1.8 extracted from

  • Sun, H.; Pang, Y.P.; Lockridge, O.; Brimijoin, S.
    Re-engineering butyrylcholinesterase as a cocaine hydrolase (2002), Mol. Pharmacol., 62, 220-224.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Protein Variants

Protein Variants Comment Organism
A328W increased kcat Homo sapiens
A328W/Y332A mutant reduces cocain burden in tissues, accelerates plasma clearance by 20fold and prevents cocaine-induced hyperactivity in mice Homo sapiens
Y332A increased Km Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0031
-
(-)-cocaine pH 7.4, A328W mutant Homo sapiens
0.0045
-
(-)-cocaine pH 7.4, wild-type enzyme Homo sapiens
0.018
-
(-)-cocaine pH 7.4, A328W/Y332A mutant Homo sapiens
0.0245
-
(-)-cocaine pH 7.4, Y332A mutant Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P06276
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(+)-cocaine + H2O
-
Homo sapiens ?
-
?
(-)-cocaine + H2O
-
Homo sapiens ?
-
?
butyrylthiocholine + H2O
-
Homo sapiens thiocholine + butyrate
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.068
-
(-)-cocaine pH 7.4, wild-type enzyme Homo sapiens
0.83
-
(-)-cocaine pH 7.4, A328W mutant Homo sapiens
1.83
-
(-)-cocaine pH 7.4, Y332A mutant Homo sapiens
2.6
-
(-)-cocaine pH 7.4, A328W/Y332A mutant Homo sapiens
2.94
-
(-)-cocaine pH 7.4, Y332A mutant Homo sapiens
6.08
-
(-)-cocaine pH 7.4, A328W mutant Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
5.5 8.5 kcat with both cocaine stereoisomers is pH dependent in A328W/Y332A mutant, whereas that of wild-type enzyme is pH dependent only with the unnatural isomer, kcat increases with increasing pH Homo sapiens