Abstract
Amino derivatives of NCI8642 were synthesized and evaluated as inhibitors of DKK1/LRP6 interactions. The new inhibitors were able to activate the Wnt signaling pathway as indicated by the increased levels of β-catenin, and decrease the DKK1-induced Tau phosphorylation at serine 396.
Keywords:
DKK1/LRP6 interaction inhibitors; NCI8642; Phenoxazinone; Tau phosphorylation inhibitors; Wnt signaling.
Copyright © 2016 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
HEK293 Cells
-
Humans
-
Intercellular Signaling Peptides and Proteins / metabolism*
-
Low Density Lipoprotein Receptor-Related Protein-6 / metabolism*
-
Models, Molecular
-
Oxazines / chemical synthesis
-
Oxazines / chemistry*
-
Oxazines / pharmacology*
-
Phosphorylation / drug effects
-
Protein Interaction Maps / drug effects*
-
Signal Transduction / drug effects
-
Structure-Activity Relationship
-
Wnt Proteins / metabolism
-
beta Catenin / metabolism
Substances
-
DKK1 protein, human
-
Intercellular Signaling Peptides and Proteins
-
LRP6 protein, human
-
Low Density Lipoprotein Receptor-Related Protein-6
-
Oxazines
-
Wnt Proteins
-
beta Catenin
-
phenoxazinone