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Literature summary for 3.1.1.84 extracted from

  • Xue, L.; Ko, M.; Tong, M.; Yang, W.; Hou, S.; Fang, L.; Liu, J.; Zheng, F.; Woods, J.; Tai, H.; Zhan, C.
    Design, preparation, and characterization of high-activity mutants of human butyrylcholinesterase specific for detoxification of cocaine (2011), Mol. Pharmacol., 79, 290-297.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.1.84

Cloned(Commentary)

Cloned (Comment) Organism
wild type and mutant enzymes are expressed in HEK-293T/17 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
A199S/F227A/S287G/A328W/E441D the mutant shows 1730fold improved (-)-cocaine-hydrolyzing activity compared to the wild type enzyme Homo sapiens
A199S/F227A/S287G/A328W/Y332G/E441D the mutant shows 1390fold improved (-)-cocaine-hydrolyzing activity compared to the wild type enzyme Homo sapiens
A199S/S287G/A328W/Y332G the mutant shows 1080fold improved (-)-cocaine-hydrolyzing activity compared to the wild type enzyme Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0011
-
 (-)-cocaine mutant enzyme A199S/F227A/S287G/A328W/E441D, pH not specified in the publication, at 25°C Homo sapiens
0.0031
-
 (-)-cocaine mutant enzyme A199S/S287G/A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens
0.0035
-
 (-)-cocaine mutant enzyme A199S/F227A/S287G/A328W/Y332G/E441D, pH not specified in the publication, at 25°C Homo sapiens
0.0045
-
 (-)-cocaine wild type enzyme, pH not specified in the publication, at 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
QFF resin anion-exchange chromatography and Hypatite C column chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(-)-cocaine + H2O
-
 Homo sapiens benzoic acid + methyl (1R,2R,3S,5S)-3-hydroxy-8-methyl-8-azabicyclo[3.2.1]-octane-2-carboxylate i.e. ecgonine methyl ester ?

Synonyms

Synonyms Comment Organism
BChE
-
 Homo sapiens
butyrylcholinesterase
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.002
-
 (-)-cocaine wild type enzyme, pH not specified in the publication, at 25°C Homo sapiens
28.83
-
 (-)-cocaine mutant enzyme A199S/F227A/S287G/A328W/E441D, pH not specified in the publication, at 25°C Homo sapiens
51
-
 (-)-cocaine mutant enzyme A199S/S287G/A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens
73.83
-
 (-)-cocaine mutant enzyme A199S/F227A/S287G/A328W/Y332G/E441D, pH not specified in the publication, at 25°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
15.17
-
 (-)-cocaine wild type enzyme, pH not specified in the publication, at 25°C Homo sapiens
16500
-
 (-)-cocaine mutant enzyme A199S/S287G/A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens
21670
-
 (-)-cocaine mutant enzyme A199S/F227A/S287G/A328W/Y332G/E441D, pH not specified in the publication, at 25°C Homo sapiens
26670
-
 (-)-cocaine mutant enzyme A199S/F227A/S287G/A328W/E441D, pH not specified in the publication, at 25°C Homo sapiens