4.7 Article

Synthesis and evaluation of gallocyanine dyes as potential agents for the treatment of Alzheimer's disease and related neurodegenerative tauopathies

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 108, Issue -, Pages 28-38

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.11.024

Keywords

Gallocyanine; Phenoxazine; DKK1 inhibitors; DKK1/LRP6 interaction inhibitors; Tau phosphorylation inhibition; Alzheimer's disease; Tauopathies

Funding

  1. European Union

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In search of safe and effective anti-Alzheimer disease agents a series of gallocyanine dyes have been synthesized and evaluated for their ability to inhibit LRPs/DKK1 interactions. Modulation of the interactions between LRPs and DKK1, regulate Wnt signaling pathway and affect Tau phosphorylation. The current efforts resulted in the identification of potent DKK1 inhibitors which are able to inhibit prostaglandin J2-induced tau phosphorylation at serine 396. (C) 2015 Elsevier Masson SAS. All rights reserved.

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