PORCN

Porcupine (PORCN) is a membrane bound O-acyltransferase (MBOAT) that is involved in the acylation (palmitoylation) of Wnt proteins. Palmitoylation is essential for Wnt secretion and signaling, with PORCN inhibitors showing efficacy in inhibiting Wnt-driven tumorigenesis.

Palmitoylation is a post-translational modification where fatty acids, such as palmitic acid, are transferred to target proteins. PORCN selectively catalyzes the palmitoylation of Wnt proteins in the endoplasmic reticulum, a process which is essential for Wnt secretion and thus the induction of Wnt signaling. Interestingly PORCN has been shown to be the first acyltransferase that is itself palmitoylated. Palmitoylation of PORCN is thought to have a negative regulatory effect on Wnt secretion.

Loss of PORCN function is associated with the disruption of Wnt signaling pathways, and pharmacological inhibition of Wnt has been shown to induce tumor regression in Wnt-dependent mammary tumors in mice. Therefore PORCN inhibitors have been postulated as therapeutics for the treatment of Wnt-driven cancers.

External sources of pharmacological information for PORCN :

• BJP Guide

PORCN Gene Data