2. Academic Validation
  3. The use of porcupine inhibitors to target Wnt-driven cancers

The use of porcupine inhibitors to target Wnt-driven cancers

  • Bioorg Med Chem Lett. 2015 Dec 1;25(23):5472-6. doi: 10.1016/j.bmcl.2015.10.032.
Soo Yei Ho 1,  Thomas H Keller 2
Affiliations

Affiliations

  • 1 Experimental Therapeutics Centre, 31 Biopolis Way, #03-01 Nanos, Singapore 138669, Singapore. Electronic address: syho@etc.a-star.edu.sg.
  • 2 Experimental Therapeutics Centre, 31 Biopolis Way, #03-01 Nanos, Singapore 138669, Singapore.
PMID: 26522946 DOI: 10.1016/j.bmcl.2015.10.032
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.

Keywords

Acyltransferase; Palmitoleation; Phenotypic assays; Porcupine inhibitors; Wnt-driven cancers; Wnt-signalling pathway.

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