• Biomedical Science Letters
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• v.24 no.3
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• pp.150-156
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• 2018

Tankyrases are multifunctional poly (ADP-ribose) polymerases that regulate a variety of cellular processes including WNT signaling, telomere maintenance, regulation of mitosis, and many others. Tankyrases interact with target proteins and regulate their interactions and stability through poly (ADP-ribosyl) ation. In addition to their roles in telomere maintenance and regulation of mitosis, tankyrase proteins regulate tumor suppressors such as AXIN, PTEN, and AMOT. Therefore, tankyrases can be effective targets for cancer treatment. Tankyrase inhibitors could affect a variety of pathways that are carcinogenic (essential for the unlimited proliferation of human cancer cells), including WNT, AKT, YAP, telomere maintenance, and regulation of mitosis. Recently, new aspects of the function and mechanism of tankyrases have been reported and several tankyrase inhibitors have been identified. Also, it has been proposed that the combination of conventional chemotherapy agents with tankyrase inhibitors may have synergistic anti-cancer effects. Based on this, it is expected that more advanced and improved tankyrase inhibitors will be developed, enabling new therapeutic strategies against cancer and other tankyrase linked diseases. This review discusses tankyrase function and the role of tankyrase inhibitors in the treatment of cancer.