Torpedo_number

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Kinetic parameters for torpedo number 70 for human-BCHE

Substrates: Butyrylthiocholine

Inhibitors: BW284C51, Cocaine, Dibucaine, Solanine, Succinylcholine~Suxamethonium, Tacrine

Substrates

Substrate: Butyrylthiocholine
EnzymeKmKcatExp. conditionsReference
N68A 1.1 & 0.6 mM - 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68D 1.1 & 0.4 mM - 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68K 2.5 & 1.1 mM - 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R 4.6 & 1.0 mM - 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68Y 3.4 & 2.0 mM - 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


Inhibitors

Inhibitor: BW284C51
EnzymeKiKsiIc50SubstrateExp. conditionsReference
N68A 179 & 91 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68D 18 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68K >700 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R >800 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68Y 112 & 50 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: Cocaine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
N68K 430 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R 200 & 70 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: Dibucaine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
N68A 10 & 6 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68D 10.0 & 0.2 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68K 17 & 6 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R 4.3 & 0.9 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68Y 39 & 2 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
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: Solanine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
N68A 0.7 & 0.2 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68D 1.26 & 0.05 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68K 3.7 & 1.3 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R 6.5 & 3.3 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68Y 0.5 & 0.3 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
N68A 700 & 300 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68D 260 & 50 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68K 4300 & 600 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R 11200 & 700 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68Y 2900 & 900 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
WT 4000 & 2600 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Inhibitor: Tacrine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
N68A 0.04 & 0.03 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68D 0.03 & 0.01 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68K 0.01 & 0.005 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R 0.06 & 0.03 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68Y 0.04 & 0.02 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

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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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