The Wnt Pathway as a Target for Small Synthetic Anti-Cancer Molecules

The Wnt signaling pathway regulates embryonic development, cell proliferation and cellular morphology. Deregulation and inappropriate activation of the pathway are associated with several diseases including cancer as well as bone and cartilage diseases such as arthritis. The high medical relevance of the Wnt pathway turns it into a tempting target for drug intervention. In this review we will summarize the major functions of the classical Wnt pathway with focus on its role in tumorigenesis. The proto-oncoproteins and tumor suppressor proteins of the Wnt pathway, which might serve as targets for therapeutic intervention, will be introduced. Despite many difficulties, a few promising achievements have been made over the last few years. Remarkable technical developments allowed the screening for compounds, which interfere with components and the activity of the Wnt pathway. We will describe several small synthetic compounds with inhibitory effects on the Wnt pathway and their effectiveness in biochemical and cell biological assays will be summarized.