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PLoS One. 2012;7(12):e50457. doi: 10.1371/journal.pone.0050457. Epub 2012 Dec 5.

WIKI4, a novel inhibitor of tankyrase and Wnt/ß-catenin signaling.

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  • 1Department of Pharmacology, Seattle, Washington, United States of America ; Institute for Stem Cell and Regenerative Medicine, Seattle, Washington, United States of America.


The Wnt/ß-catenin signaling pathway controls important cellular events during development and often contributes to disease when dysregulated. Using high throughput screening we have identified a new small molecule inhibitor of Wnt/ß-catenin signaling, WIKI4. WIKI4 inhibits expression of ß-catenin target genes and cellular responses to Wnt/ß-catenin signaling in cancer cell lines as well as in human embryonic stem cells. Furthermore, we demonstrate that WIKI4 mediates its effects on Wnt/ß-catenin signaling by inhibiting the enzymatic activity of TNKS2, a regulator of AXIN ubiquitylation and degradation. While TNKS has previously been shown to be the target of small molecule inhibitors of Wnt/ß-catenin signaling, WIKI4 is structurally distinct from previously identified TNKS inhibitors.

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