Porcupine is a member of the membrane-bound O-acyltransferase family of proteins. It catalyzes the palmitoylation of Wnt proteins, a process required for their secretion and activity. We recently disclosed a class of small molecules (IWPs) as the first reported Porcn inhibitors. We now describe the structure-activity relationship studies and the identification of subnanomolar inhibitors. We also report herein the effects of IWPs on Wnt-dependent developmental processes, including zebrafish posterior axis formation and kidney tubule formation.
|Original language||English (US)|
|Number of pages||5|
|Journal||Journal of Medicinal Chemistry|
|State||Published - Mar 28 2013|
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery