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Updated: Oct 22, 2025

Modeling Paracrine Noncanonical Wnt Signaling In Vitro
Published on: December 10, 2021
An Overview of Potential Therapeutic Agents Targeting WNT/PCP Signaling
1School of Biomedical Sciences, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Pokfulam, Hong Kong SAR, China.
Abstract:
Since the discovery of the proto-oncogene Wnt1 (Int1) in 1982, WNT signaling has been identified as one of the most important pathways that regulates a wide range of fundamental developmental and physiological processes in multicellular organisms. The canonical WNT signaling pathway depends on the stabilization and translocation of β-catenin and plays important roles in development and homeostasis. The WNT/planar cell polarity (WNT/PCP) signaling, also known as one of the β-catenin-independent WNT pathways, conveys directional information to coordinate polarized cell behaviors. Similar to WNT/β-catenin signaling, disruption or aberrant activation of WNT/PCP signaling also underlies a variety of developmental defects and cancers. However, the pharmacological targeting of WNT/PCP signaling for therapeutic purposes remains largely unexplored. In this review, we briefly discuss WNT/PCP signaling in development and disease and summarize the known drugs/inhibitors targeting this pathway.
Insights
WNT/planar cell polarity (PCP) signaling regulates cell behavior during development and in disease. This review discusses WNT/PCP pathways and explores potential therapeutic drugs and inhibitors for targeting this signaling.
Area of Science:
- Molecular Biology
- Developmental Biology
- Cell Biology
Background:
- WNT signaling pathways are crucial for multicellular organism development and physiology.
- Canonical WNT/β-catenin signaling involves β-catenin stabilization and translocation.
- WNT/planar cell polarity (PCP) signaling, a β-catenin-independent pathway, directs cell polarization.
Purpose of the Study:
- To review the roles of WNT/PCP signaling in development and disease.
- To summarize existing drugs and inhibitors targeting WNT/PCP signaling.
- To highlight the largely unexplored therapeutic potential of targeting WNT/PCP signaling.
Main Methods:
- Literature review of WNT/PCP signaling.
- Analysis of WNT/PCP roles in developmental processes.
- Summary of WNT/PCP involvement in various cancers and diseases.
Main Results:
- WNT/PCP signaling disruption is linked to developmental defects and cancers.
- Pharmacological targeting of WNT/PCP signaling remains an underexplored therapeutic avenue.
- Existing drugs and inhibitors targeting WNT/PCP pathways are summarized.
Conclusions:
- WNT/PCP signaling is vital for coordinating polarized cell behaviors.
- Aberrant WNT/PCP signaling contributes to disease pathogenesis.
- Further research into WNT/PCP targeting offers therapeutic promise.
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