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ADP-ribosyltransferase ARTD1/PARP1 is a target for cancer and ischemia drug development. Several other ARTD-family enzymes have been characterized in recent years, and it has become clear that their inhibition might also have therapeutic value. This minireview series summarizes current knowledge of pharmacological inhibition of ADP-ribosyltransferases by a compound class called PARP inhibitors and the prospects for drug development.