Targeting the β-Catenin Signaling for Cancer Therapy

beta-catenin is the key transducer of the canonical Wnt signaling. Aberrant activation of beta-catenin has been tightly connected to the initiation and progression of various cancers, and blocking beta-catenin signaling is very attractive for cancer therapy. In this article, we dissect the regulatory mechanisms of beta-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 beta-catenin for cancer therapy. Finally, we discuss the challenges of the present targeting approaches, and propose new strategies for beta-catenin-based anti-cancer drug discovery.