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Kinetic parameters for torpedo number 288,290,330 for human-ACHE

Substrates: Acetylthiocholine, Butyrylthiocholine

Inhibitors: Decamethonium, Edrophonium, HuperzineA, Tacrine

Substrates

Substrate: Acetylthiocholine
EnzymeKmKcatExp. conditionsReference
F295L/F297V/Y337A 2900 uM 0.8 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
WT 120 uM 420000/min 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
WT 140 uM 4.0 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
WT 140 & 10 uM 400000 & 50000/min 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
WT 140 uM 370000/min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
WT 140 uM 400000/min 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
WT 140 & 50 uM 370000 & 10000/min pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
WT 80 & 10 uM 400000 & 60000/min IS 5mM Shafferman_1994_EMBO.J_13_3448
WT 117 uM 390000 /min 50mM Na phosphate pH8.0 T27C Velan_1991_J.Biol.Chem_266_23977
WT 0.30 mM - IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
WT 2.5 mM - 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Substrate: Butyrylthiocholine
EnzymeKmKcatExp. conditionsReference
F295L/F297V/Y337A 0.90 mM 0.55 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
WT 0.30 mM 0.08 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
WT 2.5 mM 70000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423


Inhibitors

Inhibitor: Decamethonium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
F295L/F297V/Y337A 210 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
Y72N/Y124Q/W286A 260 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 6 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
WT 360 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 6.0 uM 5.7 uM - Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
WT - - 8.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561

Inhibitor: Edrophonium
EnzymeKiKsiIc50SubstrateExp. conditionsReference
F295L/F297V/Y337A 53 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 0.6 & 0.1 uM - - 3.3-dimethylbutylthioacetate 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
WT 0.75 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
WT 50 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 0.7 & 0.1 uM - - Acetylthiocholine 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
WT 0.3 uM - - Acetylthiocholine IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
WT 0.6 uM 4.8 uM - Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
WT - - 1.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
WT 0.32 & 0.05 uM - - Acetylthiocholine IS 5mM Shafferman_1994_EMBO.J_13_3448
WT 0.4 uM - - Paranitrophenylacetate IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
WT 0.24 uM - - S-N-Propylthioacetate IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083

Inhibitor: HuperzineA
EnzymeKiKsiIc50SubstrateExp. conditionsReference
F295L/F297V/Y337A 20000 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 16 & 1 nM 12 & 4 nM - Acetylthiocholine 50mM Na phosphate pH8 T22C Ariel_1998_Biochem.J_335_95
WT 16 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433

Inhibitor: Tacrine
EnzymeKiKsiIc50SubstrateExp. conditionsReference
F295L/F297V/Y337A 9 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 85 & 12 nM 90 & 20 nM - Acetylthiocholine 50mM Na phosphate pH8 T22C Ariel_1998_Biochem.J_335_95
WT 12 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
WT 0.21 uM - - Acetylthiocholine 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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