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Literature summary 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)

EC Number Cloned (Comment) Organism
3.1.1.8
-
 Homo sapiens

Protein Variants

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

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.8 0.0031
-
 (-)-cocaine pH 7.4, A328W mutant Homo sapiens
3.1.1.8 0.0045
-
 (-)-cocaine pH 7.4, wild-type enzyme Homo sapiens
3.1.1.8 0.018
-
 (-)-cocaine pH 7.4, A328W/Y332A mutant Homo sapiens
3.1.1.8 0.0245
-
 (-)-cocaine pH 7.4, Y332A mutant Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.8 Homo sapiens P06276
-
-

Substrates and Products (Substrate)

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.1.1.8 0.068
-
 (-)-cocaine pH 7.4, wild-type enzyme Homo sapiens
3.1.1.8 0.83
-
 (-)-cocaine pH 7.4, A328W mutant Homo sapiens
3.1.1.8 1.83
-
 (-)-cocaine pH 7.4, Y332A mutant Homo sapiens
3.1.1.8 2.6
-
 (-)-cocaine pH 7.4, A328W/Y332A mutant Homo sapiens
3.1.1.8 2.94
-
 (-)-cocaine pH 7.4, Y332A mutant Homo sapiens
3.1.1.8 6.08
-
 (-)-cocaine pH 7.4, A328W mutant Homo sapiens

pH Range

EC Number pH Minimum pH Maximum Comment Organism
3.1.1.8 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