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Mutation Report for: A328Y_human-BCHE

Mode of mutation|Site directed mutagenesis
Amino Acid change|A328Y
Torpedo number|330
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
Kinetic parameters|none

    Title: Probing the peripheral site of human butyrylcholinesterase
    Macdonald IR, Martin E, Rosenberry TL, Darvesh S
    Ref: Biochemistry, 51:7046, 2012 : PubMed


    Title: Aromatic amino-acid residues at the active and peripheral anionic sites control the binding of E2020 (Aricept) to cholinesterases
    Saxena A, Fedorko JM, Vinayaka CR, Medhekar R, Radic Z, Taylor P, Lockridge O, Doctor BP
    Ref: European Journal of Biochemistry, 270:4447, 2003 : PubMed


    Title: Concentration-dependent reversible activation-inhibition of human butyrylcholinesterase by tetraethylammonium ion
    Stojan J, Golicnik M, Froment MT, Estour F, Masson P
    Ref: European Journal of Biochemistry, 269:1154, 2002 : PubMed


    Title: Effects of mutations of active site residues and amino acids interacting with the Omega loop on substrate activation of butyrylcholinesterase
    Masson P, Xie W, Froment MT, Lockridge O
    Ref: Biochimica & Biophysica Acta, 1544:166, 2001 : PubMed


    Title: Differences in active-site gorge dimensions of cholinesterases revealed by binding of inhibitors to human butyrylcholinesterase
    Saxena A, Redman AM, Jiang X, Lockridge O, Doctor BP
    Ref: Chemico-Biological Interactions, 119-120:61, 1999 : PubMed


    Title: An improved cocaine hydrolase: the A328Y mutant of human butyrylcholinesterase is 4-fold more efficient
    Xie W, Altamirano CV, Bartels CF, Speirs RJ, Cashman JR, Lockridge O
    Ref: Molecular Pharmacology, 55:83, 1999 : PubMed


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Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
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