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Discovery of novel phenoxazinone derivatives as DKK1/LRP6 interaction inhibitors: Synthesis, biological evaluation and structure-activity relationships.

Bioorg. Med. Chem.. 2016-03; 
ThysiadisSavvas,MpousisSpyros,AvramidisNicolaos,KatsamakasSotirios,BalomenosAthanasios,RemelliRosaria,EfthimiopoulosSpyros,SarliVasi
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Proteins, Expression, Isolation and Analysis Following washing with TBS-T, proteins were detected by chemiluminescence using the enhanced chemiluminescence system (GenScript Piscataway, NJ, USA) on a Fluorochem 8800 imaging station (Alpha Innotech, CA, USA). Get A Quote

摘要

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.

关键词

DKK1/LRP6 interaction inhibitors,NCI8642,Phenoxazinone,Tau phosphorylation inhibitors,Wnt signa