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Torpedo_number
Kinetic parameters
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Torpedo_number Report for: 70
bunfa-ACHE
:
(
kinetic parameters
)
Mutation
Kin.
Type
Evaluation system
Effect
Reference
M70Y
kin
sdm
Peripheral Anionic Site
Decrease Ki of PAS ligands
Cousin_1996_J.Biol.Chem_271_15099
M70Y/
K285D
kin
sdm
Peripheral Anionic Site
Decrease Ki of PAS ligands
Cousin_1996_J.Biol.Chem_271_15099
M70Y/
K285D
kin
sdm
Peripheral Anionic Site
Decrease Ki for PAS ligands
Cousin_1996_J.Biol.Chem_271_15099
drome-ACHE
Mutation
Kin.
Type
Evaluation system
Effect
Reference
E107A
sdm
Insecticide sensitivity
Boublik_2002_Protein.Eng_15_43
E107+A
sdm
Insecticide sensitivity
Boublik_2002_Protein.Eng_15_43
E107del
sdm
Insecticide sensitivity
Boublik_2002_Protein.Eng_15_43
E107Y
sdm
Binding of Triton X-100 studies
mimic the torpedo enzyme, increases afinity for Triton 10 fold, increases inhibition by triton of phosphorylation by malaoxon
Marcel_2000_J.Biol.Chem_275_11603
E107W
sdm
Binding of Triton X-100 studies
increases afinity for Triton 10 fold, increases inhibition by triton of phosphorylation by malaoxon
Marcel_2000_J.Biol.Chem_275_11603
E107K
sdm
Binding of Triton X-100 studies
slightly decreases afinity for Triton
Marcel_2000_J.Biol.Chem_275_11603
E107L
sdm
Binding of Triton X-100 studies
slightly decreases affinity for Triton
Marcel_2000_J.Biol.Chem_275_11603
human-ACHE
:
(
kinetic parameters
)
Mutation
Kin.
Type
Evaluation system
Effect
Reference
Y72N
kin
sdm
Acyl specificity
replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE
Kaplan_2001_Biochemistry_40_7433
Y72N/
Y124Q
kin
sdm
Acyl specificity
replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE
Kaplan_2001_Biochemistry_40_7433
Y72N/
Y124Q/
W286A
kin
sdm
Acyl specificity
replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE
Kaplan_2001_Biochemistry_40_7433
Y72N/
Y124Q/
W286A/
F295L/
F297W/
Y337A
sdm
Acyl specificity
replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE
Kaplan_2001_Biochemistry_40_7433
Y72N/
Y124Q/
W286A/
F295L/
F297V/
Y337A/
V407F
sdm
Acyl specificity
Acyl pocket V407F does not increase kcat of the hexamutant
Barak_2002_Biochemistry_41_8245
Y72D/
Y124H
sdm
Search for phosphotriesterase activity
Phosphotriesterase activity
Trovaslet-Leroy_2011_Toxicol.Lett_206_14_
Y72A
kin
sdm
Omega loop
No effect
Velan_1996_FEBS.Lett_395_22
Y72A
kin
sdm
Peripheral Anionic Site
Increase inhibition by PAS ligands
Barak_1994_J.Biol.Chem_269_6296
Y72A/
Y124A
kin
sdm
Peripheral Anionic Site
small effect on Km and kcat, resistance to inhibition
Barak_1994_J.Biol.Chem_269_6296
,
Shafferman_1995_5th.ChE.Meeting.Madras__189
Y72A/
E285A
kin
sdm
Peripheral Anionic Site
Ki of PAS ligand increased >10X
Barak_1994_J.Biol.Chem_269_6296
,
Shafferman_1995_5th.ChE.Meeting.Madras__189
Y72A/
W286A
kin
sdm
Peripheral Anionic Site
Ki of PAS ligand increased >10X
Barak_1994_J.Biol.Chem_269_6296
,
Shafferman_1995_5th.ChE.Meeting.Madras__189
Y72A/
E285A/
W286A
kin
sdm
Peripheral Anionic Site
Ki of PAS ligand increased up to 400X
Barak_1994_J.Biol.Chem_269_6296
,
Shafferman_1995_5th.ChE.Meeting.Madras__189
Y72N/
Y124Q/
W286A/
F295L/
F297V/
Y337A
kin
sdm
Acyl specificity
replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE
Kaplan_2001_Biochemistry_40_7433
human-BCHE
:
(
kinetic parameters
)
Mutation
Kin.
Type
Evaluation system
Effect
Reference
N68D
kin
sdm
Peripheral Anionic Site
vKi BW284C51
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68K
kin
sdm
Peripheral Anionic Site
^Ki BW284C51
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68R
kin
sdm
Peripheral Anionic Site
^Ki BW284C51
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68Y
kin
sdm
Peripheral Anionic Site
No effect
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
N68A
kin
sdm
Peripheral Anionic Site
No effect
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
mouse-ACHE
:
(
kinetic parameters
)
Mutation
Kin.
Type
Evaluation system
Effect
Reference
Y72N
kin
sdm
Peripheral Anionic Site
increase Ki of PAS ligands/fasciculin
Radic_1993_Biochemistry_32_12074
,
Radic_1994_J.Biol.Chem_269_11233
Y72N
kin
sdm
Aricept~Donepezil~E2020 inhibition
10-fold increase Ki vs WT
Saxena_2003_Eur.J.Biochem_270_4447
Y72N
kin
sdm
oxime interaction
enlargement of the active site of the gorge
Kovarik_2006_Biochem.Biophys.Res.Commun_342_973
Y72N/
Y124Q
kin
sdm
Peripheral Anionic Site
increase Ki of PAS ligands
Radic_1993_Biochemistry_32_12074
,
Radic_1994_J.Biol.Chem_269_11233
Y72N/
W286R
kin
sdm
Peripheral Anionic Site
increase Ki of PAS ligands
Radic_1993_Biochemistry_32_12074
,
Radic_1994_J.Biol.Chem_269_11233
Y72N/
Y124Q/
W286A
kin
sdm
Peripheral Anionic Site
increase Ki of PAS ligands
Radic_1993_Biochemistry_32_12074
Y72N/
Y124Q/
W286A
kin
sdm
oxime interaction
enlargement of the active site of the gorge
Kovarik_2006_Biochem.Biophys.Res.Commun_342_973
Y72N/
Y124Q/
W286R
kin
sdm
Peripheral Anionic Site
increase Ki of PAS ligands
Radic_1993_Biochemistry_32_12074
,
Radic_1994_J.Biol.Chem_269_11233
Y72N/
Y124Q/
W286R
kin
sdm
Peripheral Anionic Site
bisquaternary inhibitors constants equivalent to that in BChE
Radic_1993_Biochemistry_32_12074
,
Radic_1994_J.Biol.Chem_269_11233
Y72N/
Y124Q/
W286R
kin
sdm
Peripheral Anionic Site
fasciculin dissociation constant increases for each mutation
Radic_1993_Biochemistry_32_12074
Y72N/
Y124Q/
W286R
kin
sdm
Aricept~Donepezil~E2020 inhibition
4000-fold increase Ki vs WT
Saxena_2003_Eur.J.Biochem_270_4447
Y72N/
D74N/
Y124Q/
W286A
kin
sdm
Peripheral Anionic Site
increase Ki of PAS ligands
Radic_1993_Biochemistry_32_12074
Y72N/
D74N/
Y124Q/
W286R
kin
sdm
Peripheral Anionic Site
increase Ki of PAS ligands
Radic_1993_Biochemistry_32_12074
nipbr-ACHEB
Mutation
Kin.
Type
Evaluation system
Effect
Reference
T65Y
sdm
Insecticide sensitivity
Schulze_2005_Anal.Chem_77_5823
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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