2. Academic Validation
  3. Synthesis and evaluation of gallocyanine dyes as potential agents for the treatment of Alzheimer's disease and related neurodegenerative tauopathies

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

  • Eur J Med Chem. 2016 Jan 27;108:28-38. doi: 10.1016/j.ejmech.2015.11.024.
Spyros Mpousis 1,  Savvas Thysiadis 1,  Nicolaos Avramidis 2,  Sotirios Katsamakas 3,  Spiros Efthimiopoulos 4,  Vasiliki Sarli 5
Affiliations

Affiliations

  • 1 Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
  • 2 Division of Animal and Human Physiology, Department of Biology, National & Kapodistrian University of Athens, Panepistimiopolis, Ilisia, Greece.
  • 3 Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
  • 4 Division of Animal and Human Physiology, Department of Biology, National & Kapodistrian University of Athens, Panepistimiopolis, Ilisia, Greece. Electronic address: [email protected].
  • 5 Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece. Electronic address: [email protected].
PMID: 26629858 DOI: 10.1016/j.ejmech.2015.11.024
Abstract

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.

Keywords

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

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