Aberrant activation of the Wnt pathway is implicated in driving the formation of various
human cancers, particularly those of the digestive tract. Inhibition of aberrant Wnt pathway
activity in cancer cell lines efficiently blocks their growth, highlighting the great potential of
therapeutics designed to achieve this in cancer patients. Here we provide an overview of the
promise and pitfalls of current drug development strategies striving to inhibit the Wnt
pathway and present new opportunities for therapeutic intervention.