Chemical Modulation of WNT Signaling in Cancer

Li shu Zhang, Lawrence Lum

Research output: Chapter in Book/Report/Conference proceedingChapter

16 Scopus citations


Genetically based observations stemming from defects in development and in regeneration form the foundation of our understanding regarding how the secreted WNT proteins control coordinated cell fate decision-making in adult tissues. At the same time, our anticipation of potential benefits and unwanted toxicities associated with candidate anticancer agents targeting WNT signal transduction are also reliant upon this blueprint of WNT-associated physiology. Despite the long established role of WNT signaling in cancer, the emergence of WNT signaling as a suppressor of immunological attack in melanoma reveals an unanticipated anticancer potential in targeting WNT signaling. Here we review the literature associated with WNT signaling in cancer and discuss potential challenges that may be associated with the chemical attack of this important cellular process in achieving therapeutic goals. Although a number of small molecules targeting WNT signaling are introduced here, we center our discussion on antagonists of the WNT acyltransferase porcupine (PORCN) given the recent entry of two candidate molecules in clinical testing.

Original languageEnglish (US)
Title of host publicationProgress in Molecular Biology and Translational Science
PublisherElsevier B.V.
Number of pages25
StatePublished - Jan 2018

Publication series

NameProgress in Molecular Biology and Translational Science
ISSN (Print)1877-1173
ISSN (Electronic)1878-0814


  • APC
  • RNF43
  • TCF7L2
  • WNT
  • colorectal cancer
  • dysgeusia
  • hepatocellular cancer
  • immunooncology
  • pancreatic cancer
  • porcupine
  • β-catenin

ASJC Scopus subject areas

  • Molecular Medicine
  • Molecular Biology


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