title: The use of porcupine inhibitors to target Wnt-driven cancers.
abstract: Over the past decade, academic groups and pharmaceutical companies have uncovered several components and targets for intervention in the Wnt pathway. One approach is to block Wnt signalling through the use of orally bioavailable small molecules that prevent Wnt ligand secretion. In recent years, the membrane bound O-acyl transferase (MBOAT) porcupine (PORCN) has emerged as a molecular target of interest in the search for clinical options to treat Wnt-driven cancers. This review shall provide an overview of the reported small molecule inhibitors for PORCN and discuss the progress made in identifying human disease models that are responsive to PORCN inhibitors.
authors.affiliation: Experimental Therapeutics Centre, 31 Biopolis Way, #03-01 Nanos, Singapore 138669, Singapore. Electronic address: syho@etc.a-star.edu.sg.
authors.forename: Soo Yei
authors.initials: SY
authors.lastname: Ho
authors.affiliation: Experimental Therapeutics Centre, 31 Biopolis Way, #03-01 Nanos, Singapore 138669, Singapore.
authors.forename: Thomas H
authors.initials: TH
authors.lastname: Keller
mesh_terms: D000217:Acyltransferases; D000818:Animals; D052160:Benzothiazoles / Q000737:chemistry* / Q000494:pharmacology; D057809:HEK293 Cells; D006801:Humans; D008565:Membrane Proteins / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D060449:Wnt Signaling Pathway
chemical_list: D052160:Benzothiazoles; C000611185:IWP-1 compound; C000611186:IWP-2 compound; D008565:Membrane Proteins; D000217:Acyltransferases; C491188:PORCN protein, human
keywords: Acyltransferase; Palmitoleation; Phenotypic assays; Porcupine inhibitors; Wnt-driven cancers; Wnt-signalling pathway