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Mutation Report for: W86A_mouse-ACHE

Mode of mutation|Site directed mutagenesis
Amino Acid change|W86A
Torpedo number|84
Comment|p.W86A Trp86Ala Fasciculin becomes an allosteric activator instead of an inhibitor for certain substrates; Aricept~Donepezil~E2020 inhibition;300-fold increase in Ki vs WT
Kinetic parameters|none

    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: Amino Acid Residues that Control Mono- and Bisquaternary Oxime-Induced Reactivation of O-Ethyl Methylphosphonylated Cholinesterases
    Ashani Y, Radic Z, Tsigelny I, Vellom DC, Pickering NA, Quinn DM, Doctor BP, Taylor P
    Ref: In Enzyme of the Cholinesterase Family - Proceedings of Fifth International Meeting on Cholinesterases, (Quinn, D.M., Balasubramanian, A.S., Doctor, B.P., Taylor, P., Eds) Plenum Publishing Corp.:133, 1995 : PubMed


    Title: Allosteric control of acetylcholinesterase catalysis by fasciculin
    Radic Z, Quinn DM, Vellom DC, Camp S, Taylor P
    Ref: Journal of Biological Chemistry, 270:20391, 1995 : 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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