title: Synthesis and evaluation of gallocyanine dyes as potential agents for the treatment of Alzheimer's disease and related neurodegenerative tauopathies.
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.
authors.affiliation: Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
authors.forename: Spyros
authors.initials: S
authors.lastname: Mpousis
authors.affiliation: Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
authors.forename: Savvas
authors.initials: S
authors.lastname: Thysiadis
authors.affiliation: Division of Animal and Human Physiology, Department of Biology, National & Kapodistrian University of Athens, Panepistimiopolis, Ilisia, Greece.
authors.forename: Nicolaos
authors.initials: N
authors.lastname: Avramidis
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
authors.forename: Sotirios
authors.initials: S
authors.lastname: Katsamakas
authors.affiliation: Division of Animal and Human Physiology, Department of Biology, National & Kapodistrian University of Athens, Panepistimiopolis, Ilisia, Greece. Electronic address: efthis@biol.uoa.gr.
authors.forename: Spiros
authors.initials: S
authors.lastname: Efthimiopoulos
authors.affiliation: Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece. Electronic address: sarli@chem.auth.gr.
authors.forename: Vasiliki
authors.initials: V
authors.lastname: Sarli
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy*; D004396:Coloring Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins / Q000378:metabolism; D026503:Low Density Lipoprotein Receptor-Related Protein-1 / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D010078:Oxazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D010766:Phosphorylation / Q000187:drug effects; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship; D024801:Tauopathies / Q000188:drug therapy*; D016875:tau Proteins / Q000378:metabolism
chemical_list: D004396:Coloring Agents; C501126:DKK1 protein, human; D036341:Intercellular Signaling Peptides and Proteins; D026503:Low Density Lipoprotein Receptor-Related Protein-1; D010078:Oxazines; D016875:tau Proteins; C007062:gallocyanine
keywords: Alzheimer's disease; DKK1 inhibitors; DKK1/LRP6 interaction inhibitors; Gallocyanine; Phenoxazine; Tau phosphorylation inhibition; Tauopathies