Tankyrase inhibitors

Inside the plate · In Wnt and β-catenin

Chemical structure of Xav-939
Structure: Xav-939, one of the class, PubChem CID 135418940

Cells and tissue onlyNot measured in peopleResearch onlySmall moleculeAlso XAV939, IWR-1

Research chemicals that turn the cartilage-building signal down rather than up.

Two chemically unrelated small molecules that inhibit the enzymes tankyrase 1 and 2. Those enzymes tag axin for destruction, so inhibiting them stabilises axin, which is the limiting part of the complex that degrades β-catenin. The result is less Wnt signalling, not more.

Nature, 2009Bioorg Med Chem Lett, 2009

Risks. In growing mice the class caused bone loss, and gut damage limits how much can be given.

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