NCIt definition : An orally bioavailable inhibitor of the membrane-bound O-acyltransferase (MBOAT) porcupine
(PORCN), with potential antineoplastic activity. Upon oral administration, ETC-1922159
binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational
palmitoylation 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 catalyzes the palmitoylation of Wnt ligands, and plays
a key role in Wnt ligand secretion. Wnt signaling is dysregulated in a variety of
cancers.;
Semantic type(s)