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An Overview of Potential Therapeutic Agents Targeting WNT/PCP Signaling

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Pharmacology of the WNT Signaling System

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 269))

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.

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Acknowledgments

This work was supported by grants from the Hong Kong Research Grants Council (ECS_27115317, GRF_17122119, and GRF_17118120) and grant from National Natural Science Foundation (general program_31771561) to Bo GAO.

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Correspondence to Bo Gao .

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Wang, J., Feng, D., Gao, B. (2021). An Overview of Potential Therapeutic Agents Targeting WNT/PCP Signaling. In: Schulte, G., Kozielewicz, P. (eds) Pharmacology of the WNT Signaling System. Handbook of Experimental Pharmacology, vol 269. Springer, Cham. https://doi.org/10.1007/164_2021_533

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