Ontology highlight
ABSTRACT:
SUBMITTER: Atkinson BN
PROVIDER: S-EPMC6961116 | biostudies-literature | 2020 Feb
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20191028 3
The carboxylesterase Notum is a key negative regulator of the Wnt signaling pathway by mediating the depalmitoleoylation of Wnt proteins. Our objective was to discover potent small molecule inhibitors of Notum suitable for exploring the regulation of Wnt signaling in the central nervous system. Scaffold-hopping from thienopyrimidine acids 1 and 2, supported by X-ray structure determination, identified 3-methylimidazolin-4-one amides 20-24 as potent inhibitors of Notum with activity across three ...[more]