Synthesis of a Tau Aggregation Inhibitor in Relation to Alzheimer’s Disease

Overview

A multitargeted approach is suggested to be most effective in inhibiting the formation of tau aggregates in Alzheimer’s disease. Two promising targets for treatment of Alzheimer’s are the initial hyperphosphorylation of tau, which is caused by an overexpression of the GSK-3beta protein, and early tau aggregation itself. To improve drug effectiveness, the structure of a known inhibitor molecule targeting both of these stages of tau aggregation was adjusted to increase binding affinity with the GSK-3beta enzyme. These adjusted molecules were screened using Molegro. The candidate molecules with the highest calculated binding affinities were further evaluated. One of these novel compounds was then synthesized and assayed for its ability to inhibit the GSK-3beta protein, resulting in a comparable efficacy to the original known molecule’s multitargeted structure. The novel molecule has promising GSK-3beta inhibition results and maintained structural features to attack early tau aggregation. This indicates possible effectiveness in inhibiting the future stages of tau aggregation indicative of Alzheimer’s disease.

Awards (1)

• 1st Place Chemistry

Competition history

• JSHS 2020 Category not listed

Resources

• National JSHS abstract book ↗

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