XAV939 binds tankyrase to stabilize axin and inhibit WNT signaling

Stable Identifier
Reaction [binding]
Homo sapiens
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XAV939 binds to the catalytic sites of tankyrase 1 and 2 and inhibits the ADP-ribosylation of AXIN1 and 2. Treatment of cells with XAV939 significantly increases the protein, but not the mRNA levels of AXIN1 and 2 and supports a strong increase in the level of GSK3beta-AXIN complexes. These cells also show increased phosphorylation of beta-catenin, decreased beta-catenin protein levels and a corresponding decrease in beta-catenin dependent transcription. Treatment of DLD-1 cells with XAV939 has also been shown to inhibit proliferation (Huang et al, 2009). XAV939 has not been tested in a clinical setting.
Literature References
PubMed ID Title Journal Year
19759537 Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

Mickanin, C, Zhang, Y, Fawell, S, Mishina, YM, Fazal, A, Myer, V, Wiellette, E, Michaud, GA, Wiessner, S, Hild, M, Bauer, A, Porter, JA, Rau, C, Huang, SM, Lengauer, C, Finan, PM, Ghidelli, S, Serluca, F, Shao, W, Bouwmeester, T, Shi, X, Stegmeier, F, Shultz, M, Charlat, O, Kirschner, MW, Cong, F, Schirle, M, Schlegl, J, Curtis, D, Wilson, CJ, Tallarico, JA, Cheng, H, Cheung, A, Liu, S, Lu, C, Tomlinson, R

Nature 2009
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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