Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity

N-Acyl indolines 4 are potent, non-covalent Notum inhibitors developed from a covalent virtual screening hit 2a. The lead compounds were simple to synthesise, achieved excellent potency in a biochemical Notum-OPTS assay and restored Wnt signalling in a cell-based TCF/LEF reporter assay. Multiple hig...

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Detalles Bibliográficos
Autores principales: Atkinson, Benjamin N., Willis, Nicky J., Zhao, Yuguang, Patel, Chandni, Frew, Sarah, Costelloe, Kathryn, Magno, Lorenza, Svensson, Fredrik, Jones, E. Yvonne, Fish, Paul V.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Editions Scientifiques Elsevier 2023
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10626578/
https://www.ncbi.nlm.nih.gov/pubmed/36934521
http://dx.doi.org/10.1016/j.ejmech.2023.115132

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