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Literature summary for 3.1.1.8 extracted from

  • Masson, P.; Xie, W.; Froment, M.T.; Lockridge, O.
    Effects of mutations of active site residues and amino acids interacting with the W loop on substrate activation of butyrylcholinesterase (2001), Biochim. Biophys. Acta, 1544, 166-176.
    View publication on PubMed
Search for more literature for 3.1.1.8

Protein Variants

Protein Variants Comment Organism
A328F no substrate activation Homo sapiens
A328Y no substrate activation Homo sapiens
E197D moderately reduced substrate activation Homo sapiens
E197G strongly reduced substrate activation Homo sapiens
E197Q strongly reduced substrate activation Homo sapiens
G328G retained substrate activation Homo sapiens
K339M retained substrate activation Homo sapiens
N83A loss of substrate activation Homo sapiens
N83Q loss of substrate activation Homo sapiens
W430A retained substrate activation, strongly reduced affinity for tetramethylammonium, bimolecular rate constant for reaction with diisopropyl fluorophosphate is reduced 10000fold Homo sapiens
W82A apparent substrate activation at butytylthiocholine concentrations greater than 2 mM Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
tetraethylammonium
-
 Homo sapiens
Tetramethylammonium
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.003
-
 succinylthiocholine wild-type, pH 7, 25°C Homo sapiens
0.011
-
 butyrylthiocholine A328Y mutant, pH 7, 25°C Homo sapiens
0.017
-
 butyrylthiocholine A328F mutant, pH 7, 25°C Homo sapiens
0.019
-
 succinylthiocholine K339M mutant, pH 7, 25°C Homo sapiens
0.02
-
 butyrylthiocholine wild-type, pH 7, 25°C Homo sapiens
0.028
-
 butyrylthiocholine G328G mutant, pH 7, 25°C Homo sapiens
0.05
-
 butyrylthiocholine N83A mutant, pH 7, 25°C Homo sapiens
0.06
-
 butyrylthiocholine N83Q and K339M mutant, pH 7, 25°C Homo sapiens
0.1
-
 butyrylthiocholine E197D and E197Q mutant, pH 7, 25°C Homo sapiens
0.12
-
 2-Nitrophenyl butyrate wild-type, pH 7, 25°C Homo sapiens
0.16
-
 2-Nitrophenyl butyrate K339M mutant, pH 7, 25°C Homo sapiens
0.2
-
 butyrylthiocholine E197G mutant, pH 7, 25°C Homo sapiens
0.4
-
 butyrylthiocholine W82A mutant, pH 7, 25°C Homo sapiens
1.4
-
 2-Nitrophenyl butyrate W82A mutant, pH 7, 25°C Homo sapiens
1.9
-
 2-Nitrophenyl butyrate W430A mutant, pH 7, 25°C Homo sapiens
6
-
 butyrylthiocholine W430A mutant, pH 7, 25°C Homo sapiens
11
-
 succinylthiocholine W430A mutant, pH 7, 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-nitrophenyl butyrate
-
 Homo sapiens 2-nitrophenol + butyrate
-
 ?
butyrylthiocholine + H2O
-
 Homo sapiens thiocholine + butyrate
-
 ?
succinylthiocholine + H2O
-
 Homo sapiens thiocholine + succinate
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2
-
 butyrylthiocholine W82A mutant, pH 7, 25°C Homo sapiens
3
-
 succinylthiocholine K339M and W430A mutant, pH 7, 25°C Homo sapiens
6
-
 succinylthiocholine wild-type, pH 7, 25°C Homo sapiens
67
-
 butyrylthiocholine E197D mutant, pH 7, 25°C Homo sapiens
83
-
 butyrylthiocholine W430A mutant, pH 7, 25°C Homo sapiens
150
-
 butyrylthiocholine E197Q mutant, pH 7, 25°C Homo sapiens
250
-
 butyrylthiocholine K339M mutant, pH 7, 25°C Homo sapiens
250
-
 2-Nitrophenyl butyrate K339M mutant, pH 7, 25°C Homo sapiens
333
-
 butyrylthiocholine G328G mutant, pH 7, 25°C Homo sapiens
333
-
 2-Nitrophenyl butyrate W430A mutant, pH 7, 25°C Homo sapiens
416
-
 2-Nitrophenyl butyrate W82A mutant, pH 7, 25°C Homo sapiens
450
-
 butyrylthiocholine wild-type, pH 7, 25°C Homo sapiens
533
-
 butyrylthiocholine A328F mutant, pH 7, 25°C Homo sapiens
600
-
 2-Nitrophenyl butyrate wild-type, pH 7, 25°C Homo sapiens
617
-
 butyrylthiocholine N83A mutant, pH 7, 25°C Homo sapiens
667
-
 butyrylthiocholine A328Y mutant, pH 7, 25°C Homo sapiens
767
-
 butyrylthiocholine N83Q mutant, pH 7, 25°C Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2
-
 tetraethylammonium wild-type, pH 7, 25°C Homo sapiens
4
-
 Tetramethylammonium wild-type, pH 7, 25°C Homo sapiens
11
-
 Tetramethylammonium K339M mutant, pH 7, 25°C Homo sapiens
70
-
 Tetramethylammonium E197G mutant, pH 7, 25°C Homo sapiens
400
-
 tetraethylammonium W82A mutant, pH 7, 25°C Homo sapiens
500
-
 Tetramethylammonium W430A mutant, pH 7, 25°C Homo sapiens
600
-
 Tetramethylammonium W82A mutant, pH 7, 25°C Homo sapiens