Tankyrases are multifunctional
poly(ADP-ribose) polymerases that regulate a variety of cellular processes, including Wnt signaling, telomere maintenance and mitosis regulation.
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, including AXIN,
phosphatase and
tensin homolog and
angiomotin. Therefore,
tankyrases may be effective targets for
cancer treatment.
Tankyrase inhibitors could affect a variety of carcinogenic pathways that promote uncontrolled proliferation, including Wnt, AKT, yes-associated
protein, telomere maintenance and mitosis regulation. Recently, novel aspects of the function and mechanism of
tankyrases have been reported, and a number of
tankyrase inhibitors have been identified. A combination of conventional
chemotherapy agents with
tankyrase inhibitors may have synergistic anticancer effects. Therefore, it is expected that more advanced and improved
tankyrase inhibitors will be developed, enabling novel therapeutic strategies against
cancer and other
tankyrase-associated diseases. The present review discusses
tankyrase function and the role of
tankyrase inhibitors in the treatment of
cancer.