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Tankyrase TRF1-interacting ankyrin-related ADP-ribose polymerase (TNKS); TNKS2

In vitro and mouse studies suggest dual inhibitors of TNKS and TNKS2 could help treat cancer. Tankyrase inhibition blocks wingless-type MMTV integration site (WNT) signaling, which is activated in some cancers. Structural-, potency- and lipophilicity-based assays led to an optimized dual TNKS and TNKS2 inhibitor. In mice with Wnt-activated mouse mammary carcinoma allografts, the most optimized inhibitor had high oral bioavailability and stability compared with vehicle and inhibited Wnt pathway signaling. Next steps could include assessing the therapeutic effects of the inhibitors in additional disease models.

SciBX 6(32); doi:10.1038/scibx.2013.858
Published online Aug. 22, 2013

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Shultz, M.D. et al. J. Med. Chem.; published online July 11, 2013;
Contact: Michael D. Shultz, Novartis Institutes for BioMedical Research, Cambridge, Mass.