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Literature summary for 3.1.1.84 extracted from

  • Zheng, F.; Yang, W.; Xue, L.; Hou, S.; Liu, J.; Zhan, C.
    Design of high-activity mutants of human butyrylcholinesterase against (-)-cocaine: Structural and energetic factors affecting the catalytic efficiency (2010), Biochemistry, 49, 9113-9119.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293T/17 cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
-
 Homo sapiens

Protein Variants

Protein Variants Comment Organism
A199S/F227A/S287G/A328W/Y332G the mutant has a 2020fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A199S/F227A/S287G/A328W/Y332G/F329V the mutant has a 121fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A199S/F227I/S287G/A328W/Y332G the mutant has a 1170fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A199S/F227L/S287G/A328W/Y332G the mutant has a 1130fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A199S/F227V/S287G/A328W/Y332G the mutant has a 1490fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A199S/S287G/A328W/Y332G the mutant has a 1080fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A199S/S287G/A328W/Y332G/L286I the mutant has a 242fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A328W/Y332A the mutant has a 9.4fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
A328W/Y332G the mutant has a 15fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens
F227A/S287G/A328W/Y332M the mutant has a 34fold improved catalytic efficiency against (-)-cocaine compared to the wild type enzyme Homo sapiens

Organism

Organism UniProt Comment Textmining
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

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
141.7
-
 (-)-cocaine mutant enzyme A328W/Y332A, pH not specified in the publication, at 25°C Homo sapiens
233.3
-
 (-)-cocaine mutant enzyme A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens
516.7
-
 (-)-cocaine mutant enzyme F227A/S287G/A328W/Y332M, 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
16670
-
 (-)-cocaine mutant enzyme A199S/F227L/S287G/A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens
18330
-
 (-)-cocaine mutant enzyme A199S/F227I/S287G/A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens
23330
-
 (-)-cocaine mutant enzyme A199S/F227V/S287G/A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens
30000
-
 (-)-cocaine mutant enzyme A199S/F227A/S287G/A328W/Y332G, pH not specified in the publication, at 25°C Homo sapiens