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Mutation Report for: A328Y_human-BCHE
Name
Class
A328Y_human-BCHE
Gene_locus
human-BCHE
Torpedo_number
330
AA_Change
A328Y
Mode_of_mutation
Site directed mutagenesis
Modification
Acyl specificity
Substrate activation
Cocaine hydrolysis
Aricept~Donepezil~E2020 inhibition
Summary
Cocaine hydrolysis;4-fold improvement in catalytic efficiency kcat/Km;Xie_1999_Mol.Pharmacol_55_83
Binding of inhibitors;smaller dimension of the active-site gorge;Saxena_1999_Chem.Biol.Interact_119-120_61
Substrate activation;substrate activation;Masson_2001_Biochim.Biophys.Acta_1544_166
Aricept~Donepezil~E2020 inhibition;small increase Ki vs WT;Saxena_2003_Eur.J.Biochem_270_4447
Paper (6)
Comment
p.A328Y Ala328Tyr (p.A356Y Ala356Tyr in primary sequence with 28 amino-acids signal peptide)Cocaine hydrolysis;4-fold improvement in catalytic efficiency kcat/Km Substrate activation, Aricept~Donepezil~E2020 inhibition;small increase Ki vs WT
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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