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Mutation Report for: F295L/F297V_human-ACHE

Mode of mutation|Site directed mutagenesis
Amino Acid change|F295L/F297V
Torpedo number|288,290//290//288
Comment|p.F295L/F297V Phe295Leu/Phe297Val (p.F326L/F328V Phe326Leu/Phe328Valin primary sequence with 31 amino-acids signal peptide) Acyl pocket, Increases hydrolysis of BTC OP-specificity: increases reactivity towards DFP DEFP and paraoxon;replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE
Kinetic parameters|Acetylthiocholine_F295L/F297V_human-ACHE,

    Title: Stereoselectivity toward VX is determined by interactions with residues of the acyl pocket as well as of the peripheral anionic site of AChE
    Ordentlich A, Barak D, Sod-Moriah G, Kaplan D, Mizrahi D, Segall Y, Kronman C, Karton Y, Lazar A and Shafferman A <2 more author(s)>
    Ref: Biochemistry, 43:11255, 2004 : PubMed


    Title: Does butyrylization of acetylcholinesterase through substitution of the six divergent aromatic amino acids in the active center gorge generate an enzyme mimic of butyrylcholinesterase?
    Kaplan D, Ordentlich A, Barak D, Ariel N, Kronman C, Velan B, Shafferman A
    Ref: Biochemistry, 40:7433, 2001 : PubMed


    Title: The architecture of human acetylcholinesterase active center probed by interactions with selected organophosphate inhibitors
    Ordentlich A, Barak D, Kronman C, Ariel N, Segall Y, Velan B, Shafferman A
    Ref: Journal of Biological Chemistry, 271:11953, 1996 : PubMed


    Title: Role of tyrosine 337 in the binding of huperzine A to the active site of human acetylcholinesterase
    Ashani Y, Grunwald J, Kronman C, Velan B, Shafferman A
    Ref: Molecular Pharmacology, 45:555, 1994 : PubMed


    Title: Dissection of the human acetylcholinesterase active center determinants of substrate specificity. Identification of residues constituting the anionic site, the hydrophobic site, and the acyl pocket
    Ordentlich A, Barak D, Kronman C, Flashner Y, Leitner M, Segall Y, Ariel N, Cohen S, Velan B, Shafferman A
    Ref: Journal of Biological Chemistry, 268:17083, 1993 : PubMed


    Title: Recombinant human acetylcholinesterase - Enzyme engineering
    Shafferman A, Velan B, Barak D, Kronman C, Ordentlich A, Flashner Y, Leitner M, Segal Y, Grosfeld H and Ariel N <1 more author(s)>
    Ref: Medical Defense Bioscience Review, 3:1097, 1993 : PubMed


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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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