Activating Wnt/β-Catenin Signaling Pathway for Disease Therapy: Challenges and Opportunities

The document from 2019 discussed the Wnt/β-catenin signaling pathway, an essential regulator of embryo development and adult tissue homeostasis. Abnormal activation or disruption of this pathway was found to be associated with many types of diseases, including cancer, hair loss, wound healing, and osteoporosis. The authors reviewed diseases associated with abnormal inactivation of the Wnt/β-catenin signaling pathway and small molecules that activate this pathway. They emphasized the discovery strategies, models, phenotype, and target proteins of these Wnt activators. They also discussed the challenges and opportunities in the development of Wnt activators for disease therapy. Over the past decades, several small molecules have been reported to activate Wnt/β-catenin signaling in various in vitro and in vivo models, some of which showed promising therapeutic effects for several types of diseases in preclinical models.