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  • Title: Synthesis and evaluation of curcumin derivatives toward an inhibitor of beta-site amyloid precursor protein cleaving enzyme 1.
    Author: Konno H, Endo H, Ise S, Miyazaki K, Aoki H, Sanjoh A, Kobayashi K, Hattori Y, Akaji K.
    Journal: Bioorg Med Chem Lett; 2014 Jan 15; 24(2):685-90. PubMed ID: 24360557.
    Abstract:
    To research a new non-peptidyl inhibitor of beta-site amyloid precursor protein cleaving enzyme 1, we focused on the curcumin framework, two phenolic groups combined with an sp2 carbon spacer for low-molecular and high lipophilicity. The structure-activity relationship study of curcumin derivatives is described. Our results indicate that phenolic hydroxy groups and an alkenyl spacer are important structural factors for the inhibition of beta-site amyloid precursor protein cleaving enzyme 1 and, furthermore, non-competitive inhibition of enzyme activity is anticipated from an inhibitory kinetics experiment and docking simulation.
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