Mechanistic basis of phenothiazine‐driven inhibition of Tau aggregation

Akoury, Elias; Pickhardt, Marcus; Gajda, Michal; Biernat, Jacek; Mandelkow, Eckhard; Zweckstetter, Markus

Mechanistic basis of phenothiazine‐driven inhibition of Tau aggregation

Akoury, Elias; Pickhardt, Marcus; Gajda, Michal; Biernat, Jacek; Mandelkow, Eckhard; Zweckstetter, Markus

URI: http://hdl.handle.net/10725/10249

URL: https://onlinelibrary.wiley.com/doi/full/10.1002/anie.201208290

DOI: https://doi.org/10.1002/anie.201208290

Date: 2019-03-21

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Abstract:

Blues brothers: Aggregation of the Tau protein is a key event in Alzheimer's disease and Tau aggregation inhibitors are important as potential drugs. Phenothiazines, such as methylene blue and its azure derivatives, have a unique mechanism, specifically modifying the Tau cysteine residues. The modification keeps Tau in a monomeric disordered conformation preventing the formation of filaments and their toxic precursors.

Citation:

Akoury, E., Pickhardt, M., Gajda, M., Biernat, J., Mandelkow, E., & Zweckstetter, M. (2013). Mechanistic basis of phenothiazine‐driven inhibition of Tau aggregation. Angewandte Chemie International Edition, 52(12), 3511-3515.