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. Author manuscript; available in PMC: 2018 Mar 15.
Published in final edited form as: Crit Rev Oncol Hematol. 2015 Dec 24;99:141–149. doi: 10.1016/j.critrevonc.2015.12.005

Figure 3. Schematic of Wnt inhibitors currently in clinical trials.

Figure 3

This figure summarizes the different Wnt pathway modulators with variable specificities and at different stages of development (fully described in the main text). The current agents in clinical trials are the porcupine inhibitor LGK974, which inhibits Wnt posttranslational palmitoylation and secretion. OMP18R5, is a fully humanized monoclonal antibody specifically binding to multiple Frizzled (Fzd) receptors and OMP-54F28 is a Fc fusion protein with Fzd8, which binds all Wnt ligands. Both inhibit the intracellular transduction of the Wnt signal. PRI-724 specifically targets the β-catenin transcriptional co-activator CBP thereby blocking their interaction. UC-961 (cirmtuzumab) is a humanized antibody targeting the targeting specifically the Wnt receptor ROR1. Arrows indicate activation/induction, blunt ended lines indicate inhibition/blockade.