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Activating Wnt/β-catenin signaling pathway for disease therapy: Challenges and opportunities

Piao Huang1, Rong Yan1, Xue Zhang1

  • 1Center for Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, P.R. China.

Pharmacology & Therapeutics
|November 24, 2018
PubMed

Insights

Small molecules that activate the Wnt/β-catenin signaling pathway are crucial for development and tissue repair. This review details Wnt activators, their therapeutic potential in diseases like hair loss and neurodegeneration, and future development challenges.

Area of Science:

  • Molecular Biology
  • Biochemistry
  • Pharmacology

Background:

  • The Wnt/β-catenin signaling pathway is vital for embryonic development, tissue homeostasis, and regeneration.
  • Dysregulation of this pathway is linked to various diseases, making it a key therapeutic target.
  • While Wnt inhibitors are well-studied, small molecules that activate Wnt signaling remain less explored.

Purpose of the Study:

  • To review diseases associated with Wnt/β-catenin signaling pathway disruption.
  • To comprehensively summarize small molecules that activate Wnt/β-catenin signaling.
  • To evaluate the therapeutic potential of Wnt activators by focusing on discovery, characterization, and target identification.

Main Methods:

  • Literature review of diseases linked to Wnt/β-catenin signaling.
  • Comprehensive summary of small molecules activating Wnt/β-catenin signaling in vitro and in vivo models.
  • Analysis of Wnt activator discovery strategies, phenotypic characterization, and target identification.

Main Results:

  • Identified numerous diseases associated with Wnt/β-catenin pathway disruption, including hair loss, pigmentary disorders, wound healing, bone diseases, neurodegenerative diseases, and COPD.
  • Compiled a comprehensive list of small molecules known to activate Wnt/β-catenin signaling.
  • Evaluated the therapeutic potential and discovery approaches for these Wnt activators.

Conclusions:

  • Wnt/β-catenin signaling activators hold significant therapeutic promise for a range of diseases.
  • Further research is needed to address challenges in targeting safety and selectivity for pharmacological development.
  • This review provides a foundation for future drug development targeting Wnt pathway activation.
Keywords:
DiseasesDrug discoverySafetySelectivityTarget proteinsWnt activator

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