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Torpedo_number
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Torpedo_number Report for: 121
bunfa-ACHE
Mutation
Kin.
Type
Evaluation system
Effect
Reference
G119H/
Y121Q/
S122T
sdm
OP-hydrolase
OP-hydrolase but 4 fold less kcat/Km for ACh than WT
Poyot_2006_Biochim.Biophys.Acta_1764_1470
drome-ACHE
Mutation
Kin.
Type
Evaluation system
Effect
Reference
M191A
sdm
Insecticide sensitivity
Boublik_2002_Protein.Eng_15_43
human-ACHE
:
(
kinetic parameters
)
Mutation
Kin.
Type
Evaluation system
Effect
Reference
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_
Y124H
sdm
Search for phosphotriesterase activity
Phosphotriesterase activity
Trovaslet-Leroy_2011_Toxicol.Lett_206_14
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
Y124A
kin
sdm
Peripheral Anionic Site
low effect
Barak_1994_J.Biol.Chem_269_6296
,
Shafferman_1995_5th.ChE.Meeting.Madras__189
Y124A/
E285A/
W286A
kin
sdm
Peripheral Anionic Site
low effect on Km Kcat but 400 increase of Ki for PAS inhib
Barak_1994_J.Biol.Chem_269_6296
,
Shafferman_1995_5th.ChE.Meeting.Madras__189
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
Y124F
sdm
oxime interaction
reactivation of tabun-inhibited human AChE. Unable to facilitate HI-6-mediated reactivation of tabun-hAChE. Induced a 2-2.5-fold enhancement of the bimolecular rate constant for K027 and HLo-7
Artursson_2009_Toxicology_265_108
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
Q119X
nat
Silent variant
Natural mutation Silent phenotype
Maekawa_1997_Clin.Chem_43_924
Q119H
kin
sdm
Search for phosphotriesterase activity
Phosphotriesterase activity Identical to WT
Millard_1995_Biochemistry_34_15925
,
Lockridge_1997_Biochemistry_36_786
Q119H
kin
sdm
Peripheral Anionic Site
No significant changes of Km and Kcat on esters
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Q119A
kin
sdm
Peripheral Anionic Site
no significant changes in Km and kcat for esters
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Q119E
kin
sdm
Peripheral Anionic Site
vKi BW284C51
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Q119G
kin
sdm
Peripheral Anionic Site
no significant changes in Km and kcat for esters
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Q119K
kin
sdm
Peripheral Anionic Site
No effect
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Q119R
kin
sdm
Peripheral Anionic Site
No effect
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Q119Y
kin
sdm
Peripheral Anionic Site
vKi BW284C51
Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423
Q119Y
kin
sdm
Peripheral Anionic Site
no role in substrate binding
Masson_1995_5th.ChE.Meeting.Madras__230
mouse-ACHE
:
(
kinetic parameters
)
Mutation
Kin.
Type
Evaluation system
Effect
Reference
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/
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
Y124C
sdm
Peripheral Anionic Site
Omega loop conformation test incorporation of the fluorophore acrylodan
Boyd_2000_J.Biol.Chem_275_22401
,
Shi_2001_J.Biol.Chem_276_42196
Y124Q
kin
sdm
Peripheral Anionic Site
Y124 stabilize bisquaternary inhibitors constants
Radic_1993_Biochemistry_32_12074
,
Radic_1994_J.Biol.Chem_269_11233
Y124Q
kin
sdm
Aricept~Donepezil~E2020 inhibition
10-fold increase Ki vs WT
Saxena_2003_Eur.J.Biochem_270_4447
Y124Q
kin
sdm
oxime interaction
enlargement of the active site of the gorge
Kovarik_2006_Biochem.Biophys.Res.Commun_342_973
Y124Q/
W286R
kin
sdm
Peripheral Anionic Site
additive effects on bisquaternary inhibitors constants
Radic_1993_Biochemistry_32_12074
,
Radic_1994_J.Biol.Chem_269_11233
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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