Kinetic parameters for torpedo number 129 for human-BCHE

Substrates: Butyrylthiocholine

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

Substrates

Substrate: Butyrylthiocholine

Enzyme	Km	Kcat	Exp. conditions	Reference
V127D	4.9 & 1.0 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

Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
V127D	644 & 32 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: Dibucaine

Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
V127D	18 & 5 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

Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
V127D	4.6 & 0.7 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

Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
V127D	2500 & 800 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

Enzyme	Ki	Ksi	Ic50	Substrate	Exp. conditions	Reference
V127D	0.06 & 0.03 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

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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