Targeting the β-catenin signaling for cancer therapy

β-catenin is the key transducer of the canonical Wnt signaling. Aberrant activation of β-catenin has been tightly connected to the initiation and progression of various cancers, and blocking β-catenin signaling is very attractive for cancer therapy. In this article, we dissect the regulatory mechanisms of β-catenin stabilization and transcriptional activity, with emphasis on the enzymes and partners for post-translational modifications and protein-protein interactions, and review the small molecules and peptides targeting β-catenin for cancer therapy. Finally, we discuss the challenges of the present targeting approaches, and propose new strategies for β-catenin-based anti-cancer drug discovery.