Cargando…
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...
Autores principales: | 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: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Royal Society of Chemistry
2019
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6727465/ https://www.ncbi.nlm.nih.gov/pubmed/31534655 http://dx.doi.org/10.1039/c9md00096h |
Ejemplares similares
-
Structural Analysis and Development of Notum Fragment
Screening Hits
por: Zhao, Yuguang, et al.
Publicado: (2022) -
Design of a Potent,
Selective, and Brain-Penetrant
Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic
Fragment Hit
por: Willis, Nicky J., et al.
Publicado: (2022) -
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors
por: Atkinson, Benjamin N., et al.
Publicado: (2020) -
Structural Insights
into Notum Covalent Inhibition
por: Zhao, Yuguang, et al.
Publicado: (2021) -
Carboxylesterase
Notum Is a Druggable Target to Modulate
Wnt Signaling
por: Bayle, Elliott D., et al.
Publicado: (2021)