Torpedo_number
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Kinetic parameters for torpedo number 72 for human-BCHE

Substrates: 1-Naphtylacetate, Acetylcholine, Aspirin, Benzoylcholine, Butyrylcholine, Butyrylthiocholine, Heptanoylcholine, Heroin, Hexanoylcholine, Methylprednisolone-acetate, O-Nitrophenylbutyrate, Pentanoylcholine, Procaine, Propionylcholine, Succinyldithiocholine, Tetracaine

Inhibitors: 17-desoxypancuronium, BW284C51, Chlorpromazine, Choline, Cocaine, Decamethonium, Dibucaine, Dibutyrate-pancuronium, Meperidine, Neostigmine~Prostigmine, Pancuronium, Physostigmine~Eserine, Procaine, Ro-2-0683, Solanine, Succinylcholine~Suxamethonium, Tacrine, Tetracaine, Tetramethylammonium, Vecuronium, Win4510, Win5303

Substrates

Substrate: 1-Naphtylacetate
EnzymeKmKcatExp. conditionsReference
D70G 370 uM 36000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 1000 uM 36000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Acetylcholine
EnzymeKmKcatExp. conditionsReference
D70G 9000 uM 33200 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 1400 uM 33200 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Aspirin
EnzymeKmKcatExp. conditionsReference
D70G 1600 uM 7200 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 4200 uM 7200 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Benzoylcholine
EnzymeKmKcatExp. conditionsReference
D70G 22 uM 15000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 8 & 1 uM 15000 & 700 /min 100mM K phosphate pH7.0 T25C Blong_1997_Biochem.J_327_747
WT 4 uM 15000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Butyrylcholine
EnzymeKmKcatExp. conditionsReference
D70G 1700 uM 80000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 91 uM 80000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Butyrylthiocholine
EnzymeKmKcatExp. conditionsReference
D70G 3.8 & 0.4 mM 30000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
WT 7 & 0.7 uM 24000 & 10000 /min 100mM K phosphate pH7.0 T25C Blong_1997_Biochem.J_327_747
WT 2.2 mM - 100mM Na phosphate pH7.4 T22C Gnatt_1994_J.Neurochem_62_749
WT 0.05 mM 1.1 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
WT 2.8 & 0.7 mM 98000 & 33000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Substrate: Heptanoylcholine
EnzymeKmKcatExp. conditionsReference
D70G 1110 uM 35000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 380 uM 35000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Heroin
EnzymeKmKcatExp. conditionsReference
D70G 450 uM 500 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 110 uM 500 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Hexanoylcholine
EnzymeKmKcatExp. conditionsReference
D70G 820 uM -   Lockridge_1990_Pharmacol.Ther_47_35
WT - 36000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 570 uM 36000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Methylprednisolone-acetate
EnzymeKmKcatExp. conditionsReference
D70G - 25 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 1000 uM 25 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: O-Nitrophenylbutyrate
EnzymeKmKcatExp. conditionsReference
D70G 400 uM 48000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 110 & 20 uM 36000 & 5000 /min 100mM K phosphate pH7.0 T25C Blong_1997_Biochem.J_327_747
WT 330 uM 48000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Pentanoylcholine
EnzymeKmKcatExp. conditionsReference
D70G 1500 uM 63000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 720 uM 63000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Procaine
EnzymeKmKcatExp. conditionsReference
D70G 100 uM 255 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 66 uM 255 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Propionylcholine
EnzymeKmKcatExp. conditionsReference
D70G 3100 uM 55000 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 970 uM 55000 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Succinyldithiocholine
EnzymeKmKcatExp. conditionsReference
D70G 1080 uM 600 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 35 uM 600 /min   Lockridge_1990_Pharmacol.Ther_47_35

Substrate: Tetracaine
EnzymeKmKcatExp. conditionsReference
D70G 8 uM 74 /min   Lockridge_1990_Pharmacol.Ther_47_35
WT 0.14 uM 74 /min   Lockridge_1990_Pharmacol.Ther_47_35


Inhibitors

Inhibitor: 17-desoxypancuronium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 24 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.13 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: BW284C51
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G 2540 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
WT 14000 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 480 & 110 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Chlorpromazine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 74 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 4.4 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Choline
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 59 mM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 30 mM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Cocaine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G 3200 & 100 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
WT 390 & 30 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Decamethonium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 1800 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT 2.5 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT - - 13 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Dibucaine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G 182 & 100 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
D70G - - 54 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT 6.9 & 4.6 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
WT - - 2.7 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Dibutyrate-pancuronium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 4.2 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.015 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Meperidine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 1800 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 760 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Neostigmine~Prostigmine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 24 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.13 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Pancuronium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 22 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.15 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Physostigmine~Eserine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 270 nM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 14 nM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Procaine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 590 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 44 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Ro-2-0683
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 170 nM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 1.4 nM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Solanine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G 78.0 & 2.5 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
WT 3.3 & 2.8 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Succinylcholine~Suxamethonium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G 52000 & 13000 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
D70G - - 9500 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT 4000 & 2600 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Tacrine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G 9.1 & 2.4 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
WT 12 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 0.06 & 0.03 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Tetracaine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 6.3 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.28 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Tetramethylammonium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 71 mM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 28 mM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Vecuronium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 1.7 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.34 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Win4510
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 5.4 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.15 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Win5303
EnzymeKiKsiIc50SubstrateExp. conditionsReference
D70G - - 21 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 0.79 uM   Lockridge_1990_Pharmacol.Ther_47_35
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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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