1.
Bioorg Med Chem
; 24(5): 1014-22, 2016 Mar 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-26819000
RESUMEN
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 ß-catenin, and decrease the DKK1-induced Tau phosphorylation at serine 396.
Asunto(s)
Péptidos y Proteínas de Señalización Intercelular/metabolismo , Proteína-6 Relacionada a Receptor de Lipoproteína de Baja Densidad/metabolismo , Oxazinas/química , Oxazinas/farmacología , Mapas de Interacción de Proteínas/efectos de los fármacos , Células HEK293 , Humanos , Modelos Moleculares , Oxazinas/síntesis química , Fosforilación/efectos de los fármacos , Transducción de Señal/efectos de los fármacos , Relación Estructura-Actividad , Proteínas Wnt/metabolismo , beta Catenina/metabolismo
2.
Eur J Med Chem
; 108: 28-38, 2016 Jan 27.
Artículo
en Inglés
| MEDLINE
| ID: mdl-26629858
RESUMEN
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.