Wnt Signaling Inhibitors

Wnt proteins (Wnt name derived from wingless phenotype in Drosophila) are highly conserved secreted glycoproteins acting as short- or long-range signaling molecules functioning primarily in embryogenesis. Wnt proteins trigger and relay cellular responses that establish body axis, positions of organs and so on. The relay of information is carried out by precisely-timed activation of an intricately interconnected set of intracellular signal transduction networks starting with the binding of Wnt proteins to receptors of the Frizzled family. In humans, 19 members of the Wnt family and 10 Frizzled receptors are known. There are three major ways Wnt signaling has been proposed to work. In the canonical pathway, Wnt binding leads to the stabilization of the transcription factor β-catenin, which enters the nucleus to regulate a set of target genes. However, Wnt-binding also acts through β-catenin-independent, non-canonical pathways such as the planar cell polarity (PCP) pathway and a pathway involving Ca2+ signaling. Wnts have important functions in stem cell biology, organ development, cell differentiation, cell migration, angiogenesis and aging to name a few. Over-activation of Wnt signaling due to mutations is a major factor in oncogenesis in the human colon, liver, skin, prostrate, breast and other tissues. Due to its capacity to influence basic cellular behavior mis-regulation of which can even lead to an "unviable" fate for a developing embryo, the Wnt signaling cascade holds excellent potential as a therapeutic target for treating myriad of human diseases like cancers and various developmental abnormalities. Despite academic and industrial pursuits, clinically relevant and selective inhibitors of the pathway remain elusive, requiring continuous dedicated effort to come up with novel approaches. BioVision's product catalog includes a wholesome collection of currently-known Wnt signaling inhibitors.