Insights into the binding of PARP inhibitors to the catalytic domain of human tankyrase-2

The high-resolution crystal structures of the human tankyrase 2 poly(ADP-ribose) polymerase (PARP) domain in complex with 16 various PARP inhibitors are reported, including the compounds BSI-201, AZD-2281 and ABT-888, which are currently in Phase 2 or 3 clinical trials.