Preferred Label : Porcupine Inhibitor WNT974;
NCIt synonyms : PORCN inhibitor LGK974; 2-(2,3-Dimethyl-[2,4-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide;
NCIt related terms : WNT-974;
NCIt definition : An orally available inhibitor of porcupine (PORCN), with potential antineoplastic
activity. Upon oral administration, WNT974 binds to and inhibits PORCN in the endoplasmic
reticulum (ER), which blocks post-translational acylation of Wnt ligands and inhibits
their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated
signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine, a membrane-bound
O-acyltransferase (MBOAT), is required for the palmitoylation of Wnt ligands, and
plays a key role in Wnt ligand secretion and activity. Wnt signaling is dysregulated
in a variety of cancers.;
UNII : U27F40013Q;
CAS number : 1243244-14-5;
Molecule name : WNT974; WNT 974; LGK 974; LGK-974;
Origin ID : C116860;
UMLS CUI : C4519143;
Semantic type(s)
- concept_is_in_subset
- has_target
