Preferred Label : Zamaporvint;
NCIt synonyms : RXC 004; RXC-004; Porcupine Inhibitor RXC004;
NCIt definition : An orally available inhibitor of porcupine (PORCN), with potential antineoplastic
activity. Upon oral administration, zamaporvint 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 : M56M7CHN8E;
CAS number : 1900754-56-4;
Molecule name : RXC004;
NCI Metathesaurus CUI : CL935870;
Origin ID : C156701;
UMLS CUI : C5908081;
Semantic type(s)
concept_is_in_subset