Abstract
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) |
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Pages (from-to) | 2700-2704 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 56 |
Issue number | 6 |
DOIs | |
State | Published - Mar 28 2013 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery