Torpedo_number
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Torpedo_number Report for: 279

drome-ACHE
MutationKin.TypeEvaluation systemEffectReference
W359A sdmInsecticide sensitivityBoublik_2002_Protein.Eng_15_43
W359A sdmInsecticide sensitivityStojan_2016_Chem.Biol.Interact_259_110
W121A/
W359A		 sdmInsecticide sensitivityStojan_2016_Chem.Biol.Interact_259_110
W359+A sdmInsecticide sensitivityBoublik_2002_Protein.Eng_15_43
W359del sdmInsecticide sensitivityBoublik_2002_Protein.Eng_15_43
W359L sdmBinding of Triton X-100 studiesincreases affinity for Triton but slightly decreased maloxon phosphorylationMarcel_2000_J.Biol.Chem_275_11603

human-ACHE : (kinetic parameters)
MutationKin.TypeEvaluation systemEffectReference
Y72N/
Y124Q/
W286A		kinsdmAcyl specificityreplacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHEKaplan_2001_Biochemistry_40_7433
Y72N/
Y124Q/
W286A/
F295L/
F297W/
Y337A		 sdmAcyl specificityreplacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHEKaplan_2001_Biochemistry_40_7433
Y72N/
Y124Q/
W286A/
F295L/
F297V/
Y337A/
V407F		 sdmAcyl specificity Acyl pocket V407F does not increase kcat of the hexamutantBarak_2002_Biochemistry_41_8245
Y72A/
W286A		kinsdmPeripheral Anionic SiteKi of PAS ligand increased >10XBarak_1994_J.Biol.Chem_269_6296,
Shafferman_1995_5th.ChE.Meeting.Madras__189
Y72A/
E285A/
W286A		kinsdmPeripheral Anionic SiteKi of PAS ligand increased up to 400XBarak_1994_J.Biol.Chem_269_6296,
Shafferman_1995_5th.ChE.Meeting.Madras__189
D74N/
W286A		 sdmPeripheral Anionic Sitecooperativity of mutations D74 W286 10+4 increase KiShafferman_1995_5th.ChE.Meeting.Madras__189
D74N/
W286A/
Y341A		 sdmPeripheral Anionic Sitecooperativity of mutations on D74 W286 for bisquaternary PAS inhibShafferman_1995_5th.ChE.Meeting.Madras__189
Y124A/
E285A/
W286A		kinsdmPeripheral Anionic Sitelow effect on Km Kcat but 400 increase of Ki for PAS inhibBarak_1994_J.Biol.Chem_269_6296,
Shafferman_1995_5th.ChE.Meeting.Madras__189
E285A/
W286A		kinsdmPeripheral Anionic Site10 to 200fold increase of inhibition K for PAS ligandsBarak_1994_J.Biol.Chem_269_6296,
Shafferman_1995_5th.ChE.Meeting.Madras__189
W286AkinsdmPeripheral Anionic Site Substrate inhibition10 fold increase of inhibition K for PAS ligandsShafferman_1992_EMBO.J_11_3561,
Shafferman_1992_4th.ChE.Meeting.Eilat__165,
Ordentlich_1993_J.Biol.Chem_268_17083,
Shafferman_1993_Proc.Med.Def.Biosci.Rev_3_1097,
Ashani_1994_Mol.Pharmacol_45_555,
Barak_1994_J.Biol.Chem_269_6296,
Shafferman_1995_5th.ChE.Meeting.Madras__189
W286AkinsdmAcyl specificityreplacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHEKaplan_2001_Biochemistry_40_7433
W286A/
Y341A		 sdmPeripheral Anionic Sitesynergetic effects on PAS ligands inhibitionShafferman_1995_5th.ChE.Meeting.Madras__189
Y72N/
Y124Q/
W286A/
F295L/
F297V/
Y337A		kinsdmAcyl specificityreplacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHEKaplan_2001_Biochemistry_40_7433

human-BCHE
MutationKin.TypeEvaluation systemEffectReference
A277V sdmp.A277V Ala277Val Cationic triarylmethane dyesBiberoglu_2011_Arch.Biochem.Biophys_511_64
A277H sdmPeripheral Anionic SiteA277 plays no role in catalytic activityMasson_1995_5th.ChE.Meeting.Madras__230,
Masson_1996_Eur.J.Biochem_235_36
A277W sdmPeripheral Anionic SiteA277 plays no role in catalytic activityMasson_1995_5th.ChE.Meeting.Madras__230,
Masson_1996_Eur.J.Biochem_235_36
A277W/
G283D		 sdmPeripheral Anionic SiteA277 G283 play no role in catalytic activityMasson_1995_5th.ChE.Meeting.Madras__230,
Masson_1996_Eur.J.Biochem_235_36

mouse-ACHE : (kinetic parameters)
MutationKin.TypeEvaluation systemEffectReference
Y72N/
W286R		kinsdmPeripheral Anionic Siteincrease Ki of PAS ligandsRadic_1993_Biochemistry_32_12074,
Radic_1994_J.Biol.Chem_269_11233
W286A sdmPeripheral Anionic SiteRadic_1999_Chem.Biol.Interact_119-120_111
W286A sdmAricept~Donepezil~E2020 inhibition1400-fold increase Ki vs WTSaxena_2003_Eur.J.Biochem_270_4447
W286A sdmoxime interactionenlargement of the active site of the gorgeKovarik_2006_Biochem.Biophys.Res.Commun_342_973
Y72N/
Y124Q/
W286A		kinsdmPeripheral Anionic Siteincrease Ki of PAS ligandsRadic_1993_Biochemistry_32_12074
Y72N/
Y124Q/
W286A		kinsdmoxime interactionenlargement of the active site of the gorgeKovarik_2006_Biochem.Biophys.Res.Commun_342_973
Y72N/
Y124Q/
W286R		kinsdmPeripheral Anionic Siteincrease Ki of PAS ligandsRadic_1993_Biochemistry_32_12074,
Radic_1994_J.Biol.Chem_269_11233
Y72N/
Y124Q/
W286R		kinsdmPeripheral Anionic Sitebisquaternary inhibitors constants equivalent to that in BChERadic_1993_Biochemistry_32_12074,
Radic_1994_J.Biol.Chem_269_11233
Y72N/
Y124Q/
W286R		kinsdmPeripheral Anionic Sitefasciculin dissociation constant increases for each mutationRadic_1993_Biochemistry_32_12074
Y72N/
Y124Q/
W286R		kinsdmAricept~Donepezil~E2020 inhibition4000-fold increase Ki vs WTSaxena_2003_Eur.J.Biochem_270_4447
Y72N/
D74N/
Y124Q/
W286A		kinsdmPeripheral Anionic Siteincrease Ki of PAS ligandsRadic_1993_Biochemistry_32_12074
Y72N/
D74N/
Y124Q/
W286R		kinsdmPeripheral Anionic Siteincrease Ki of PAS ligandsRadic_1993_Biochemistry_32_12074
Y124Q/
W286R		kinsdmPeripheral Anionic Siteadditive effects on bisquaternary inhibitors constantsRadic_1993_Biochemistry_32_12074,
Radic_1994_J.Biol.Chem_269_11233
W286RkinsdmPeripheral Anionic SiteR in BChE additional positive charge near the lip of the gorgereduces binding energy by 0.8 kcalRadic_1993_Biochemistry_32_12074,
Radic_1994_J.Biol.Chem_269_11233

torma-ACHE
MutationKin.TypeEvaluation systemEffectReference
W279A sdmPeripheral Anionic Sitestrongly reduced inhibition by PAS ligand but inhib active site unaffectedHarel_1992_Proc.Natl.Acad.Sci.U.S.A_89_10827
W279A sdmPeripheral Anionic SiteIncreased thermal inactivation Increased reactivity of C231Morel_1999_Mol.Pharmacol_55_982
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