Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen

NOTUM is a carboxylesterase that has been shown to act by mediating the O-depalmitoleoylation of Wnt proteins resulting in suppression of Wnt signaling. Here, we describe the development of NOTUM inhibitors that restore Wnt signaling for use in in vitro disease models where NOTUM over activity is an...

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Detalhes bibliográficos
Publicado no:Medchemcomm
Main Authors: Atkinson, Benjamin N., Steadman, David, Zhao, Yuguang, Sipthorp, James, Vecchia, Luca, Ruza, Reinis R., Jeganathan, Fiona, Lines, Georgie, Frew, Sarah, Monaghan, Amy, Kjær, Svend, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V.
Formato: Artigo
Idioma:Inglês
Publicado em: Royal Society of Chemistry 2019
Assuntos:
Chemistry
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6727465/
https://ncbi.nlm.nih.gov/pubmed/31534655
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c9md00096h
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