Mutation

Kinetic parameters

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Kinetic parameters for mutation D70G_human-BCHE

Substrate

MoleculeKmKcatExp. conditionsReference
1-Naphtylacetate 370 uM 36000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Acetylcholine 9000 uM 33200 /min   Lockridge_1990_Pharmacol.Ther_47_35
Aspirin 1600 uM 7200 /min   Lockridge_1990_Pharmacol.Ther_47_35
Benzoylcholine 22 uM 15000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Butyrylcholine 1700 uM 80000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Butyrylthiocholine 3.8 & 0.4 mM 30000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Heptanoylcholine 1110 uM 35000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Heroin 450 uM 500 /min   Lockridge_1990_Pharmacol.Ther_47_35
Hexanoylcholine 820 uM -   Lockridge_1990_Pharmacol.Ther_47_35
Hexanoylcholine - 36000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Methylprednisolone-acetate - 25 /min   Lockridge_1990_Pharmacol.Ther_47_35
O-Nitrophenylbutyrate 400 uM 48000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Pentanoylcholine 1500 uM 63000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Procaine 100 uM 255 /min   Lockridge_1990_Pharmacol.Ther_47_35
Propionylcholine 3100 uM 55000 /min   Lockridge_1990_Pharmacol.Ther_47_35
Succinyldithiocholine 1080 uM 600 /min   Lockridge_1990_Pharmacol.Ther_47_35
Tetracaine 8 uM 74 /min   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor

MoleculeKiKsiIc50Exp. conditionsSubstrateReference
17-desoxypancuronium - - 24 uM   Lockridge_1990_Pharmacol.Ther_47_35
BW284C51 2540 uM - - 50mM NaPhosphate pH7.4 Butyrylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Chlorpromazine - - 74 uM   Lockridge_1990_Pharmacol.Ther_47_35
Choline - - 59 mM   Lockridge_1990_Pharmacol.Ther_47_35
Cocaine 3200 & 100 uM - - 50mM NaPhosphate pH7.4 Butyrylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Decamethonium - - 1800 uM   Lockridge_1990_Pharmacol.Ther_47_35
Dibucaine 182 & 100 uM - - 50mM NaPhosphate pH7.4 Butyrylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Dibucaine - - 54 uM   Lockridge_1990_Pharmacol.Ther_47_35
Dibutyrate-pancuronium - - 4.2 uM   Lockridge_1990_Pharmacol.Ther_47_35
Meperidine - - 1800 uM   Lockridge_1990_Pharmacol.Ther_47_35
Neostigmine~Prostigmine - - 24 uM   Lockridge_1990_Pharmacol.Ther_47_35
Pancuronium - - 22 uM   Lockridge_1990_Pharmacol.Ther_47_35
Physostigmine~Eserine - - 270 nM   Lockridge_1990_Pharmacol.Ther_47_35
Procaine - - 590 uM   Lockridge_1990_Pharmacol.Ther_47_35
Ro-2-0683 - - 170 nM   Lockridge_1990_Pharmacol.Ther_47_35
Solanine 78.0 & 2.5 uM - - 50mM NaPhosphate pH7.4 Butyrylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Succinylcholine~Suxamethonium 52000 & 13000 uM - - 50mM NaPhosphate pH7.4 Butyrylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Succinylcholine~Suxamethonium - - 9500 uM   Lockridge_1990_Pharmacol.Ther_47_35
Tacrine 9.1 & 2.4 uM - - 50mM NaPhosphate pH7.4 Butyrylthiocholine Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Tetracaine - - 6.3 uM   Lockridge_1990_Pharmacol.Ther_47_35
Tetramethylammonium - - 71 mM   Lockridge_1990_Pharmacol.Ther_47_35
Vecuronium - - 1.7 uM   Lockridge_1990_Pharmacol.Ther_47_35
Win4510 - - 5.4 uM   Lockridge_1990_Pharmacol.Ther_47_35
Win5303 - - 21 uM   Lockridge_1990_Pharmacol.Ther_47_35

Send your questions or comments to :
Mail to: Nicolas Lenfant, Thierry Hotelier, Yves Bourne, Pascale Marchot and Arnaud Chatonnet.
Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
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