Torpedo_number

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Kinetic parameters for torpedo number 288,290

Substrates: Acetylthiocholine, Butyrylthiocholine

Inhibitors: Decamethonium, Edrophonium, HuperzineA, Tacrine

Substrates

Substrate: Acetylthiocholine
Gene_LocusEnzymeKmKcatExp. conditionsReference
human-ACHEF295L/F297V 1300 uM 0.5 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
mouse-ACHEF295L/F297I 200 & 93 uM 12000 & 1000/min 100mM NaP pH7 T22C eq3 sch3 Radic_1993_Biochemistry_32_12074
bunfa-ACHEWT 78.8 & 6.3 uM - T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT - 175000/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
eleel-ACHEWT 130 uM 900000 /min   Salih_1992_Biochem.J_285_451
eleel-ACHEWT - 733333/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
human-ACHEWT 120 uM 420000/min 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 140 uM 4.0 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 140 & 10 uM 400000 & 50000/min 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
human-ACHEWT 140 uM 370000/min IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHEWT 140 uM 400000/min 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHEWT 140 & 50 uM 370000 & 10000/min pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
human-ACHEWT 80 & 10 uM 400000 & 60000/min IS 5mM Shafferman_1994_EMBO.J_13_3448
human-ACHEWT 117 uM 390000 /min 50mM Na phosphate pH8.0 T27C Velan_1991_J.Biol.Chem_266_23977
human-BCHEWT 40 uM 0.5 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 46 uM 140000 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528
mouse-ACHEWT 46 & 3 uM 140000 & 10000/min 100mM NaP pH7 T22C eq3 sch3 Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 23 uM 40000 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528
mouse-BCHEWT 35 & 2 uM 40000 & 7000/min 100mM NaP pH7 T22C eq3 sch3 Radic_1993_Biochemistry_32_12074
ratno-ACHEWT - 220000/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
torca-ACHEWT - 481666/min T25C pH7.8 Taylor_1974_Mol.Pharmacol_10_78
torma-ACHEWT 81.2 & 4.2 uM - T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT - 273333/min 100mM NaP T28C pH7.0 Vigny_1978_Eur.J.Biochem_85_317
human-ACHEWT 0.30 mM - IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 2.5 mM - 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

Substrate: Butyrylthiocholine
Gene_LocusEnzymeKmKcatExp. conditionsReference
human-ACHEF295L/F297V 0.42 mM 0.43 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.30 mM 0.08 10+5/min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 2.5 mM 70000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHEWT 7 & 0.7 uM 24000 & 10000 /min 100mM K phosphate pH7.0 T25C Blong_1997_Biochem.J_327_747
human-BCHEWT 2.2 mM - 100mM Na phosphate pH7.4 T22C Gnatt_1994_J.Neurochem_62_749
human-BCHEWT 0.05 mM 1.1 10+5 /min IS 50mM phosphate pH8 T27C Kaplan_2001_Biochemistry_40_7433
human-BCHEWT 2.8 & 0.7 mM 98000 & 33000 /min 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
mouse-ACHEWT 93 uM 1100 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528
mouse-BCHEWT 55 uM 37000 /min 100mM NaPhosphate Ph7.0 T22C Hosea_1995_Biochemistry_34_11528


Inhibitors

Inhibitor: Decamethonium
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEF295L/F297V 210 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
bunfa-ACHEWT 8.2 & 1.2 uM 47.5 & 3.5 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT 23.6 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 6 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 360 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 6.0 uM 5.7 uM - Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHEWT - - 8.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
human-BCHEWT 2.5 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 3.5 & 1.6 uM 31 & 16 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 10 & 1.1 uM 42 & 25 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
torma-ACHEWT 1.3 & 0.2 uM 7.0 & 1.3 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT 0.34 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-BCHEWT - - 13 uM   Lockridge_1990_Pharmacol.Ther_47_35

Inhibitor: Edrophonium
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEF295L/F297V 2.2 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.6 & 0.1 uM - - 3.3-dimethylbutylthioacetate 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
bunfa-ACHEWT 0.6 & 0.0 uM 9.9 & 4.2 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHEWT 0.23 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 0.75 uM - - Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHEWT 50 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.7 & 0.1 uM - - Acetylthiocholine 50mM NaPhosphate pH8 Kronman_1994_J.Biol.Chem_269_27819
human-ACHEWT 0.3 uM - - Acetylthiocholine IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHEWT 0.6 uM 4.8 uM - Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHEWT - - 1.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
human-ACHEWT 0.32 & 0.05 uM - - Acetylthiocholine IS 5mM Shafferman_1994_EMBO.J_13_3448
human-BCHEWT 50 uM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 0.30 & 0.1O uM 6.4 & 0.6 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 110 & 37 uM 1400 & 700 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
torma-ACHEWT 0.3 & 0.0 uM - - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
torma-ACHEWT 0.15 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHEWT 0.4 uM - - Paranitrophenylacetate IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083
human-ACHEWT 0.24 uM - - S-N-Propylthioacetate IS 50mM phosphate pH8 T27C Ordentlich_1993_J.Biol.Chem_268_17083

Inhibitor: HuperzineA
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEF295L/F297V 50 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 16 & 1 nM 12 & 4 nM - Acetylthiocholine 50mM Na phosphate pH8 T22C Ariel_1998_Biochem.J_335_95
human-ACHEWT 16 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-BCHEWT 50000 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433

Inhibitor: Tacrine
Gene_LocusEnzymeKiKsiIc50SubstrateExp. conditionsReference
human-ACHEF295L/F297V 60 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 85 & 12 nM 90 & 20 nM - Acetylthiocholine 50mM Na phosphate pH8 T22C Ariel_1998_Biochem.J_335_95
human-ACHEWT 12 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
human-ACHEWT 0.21 uM - - Acetylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
human-BCHEWT 12 nM - - Acetylthiocholine T25C IS 50 mM phosphate Kaplan_2001_Biochemistry_40_7433
mouse-ACHEWT 40 & 10 nM 130 & 50 nM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHEWT 17 & 4 nM 47 & 22 nM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
human-BCHEWT 0.06 & 0.03 uM - - Butyrylthiocholine 50mM NaPhosphate pH7.4 Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

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Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
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