Fig. 2

Therapeutic targets in Wnt/β-catenin pathway and developmental therapeutics. Multiple strategies have been under investigation to counteract the canonical pathway of Wnt signaling. a, b Wnt soluble receptors and antibodies directed to Frizzled receptors impair the interaction ligand/receptor and its conveyed signal. c COX inhibitors reduces β-catenin cytoplasmic levels through different ways. PGE2, the main product of COX2 enzyme, is thought to mediate β-catenin transcription. Also, COX inhibitors such as aspirin were related to increase β-catenin ubiquitination and proteasomal destruction. d Tankyrase activates axin through induction of PARsylation and proteasomal degradation; tankyrase inhibitors increase the levels of axin, facilitating the formation of the β-catenin destruction complex and reducing β-catenin availability. e CBP inhibitors reduce the interaction between CBP and Tcf/Lef, reducing Tcf/Lef activity. f. PORCN inhibitors reduce the essential palmitoylation of Wnt, precluding its release to the extracellular space. g SAM68 is a regulator of alternative splicing of Tcf and impairs β-catenin/Tcf/Lef interaction