Poly (ADP-ribosyl)ation of proteins is a posttranslational modification mediated by
poly (ADP-ribose) polymerases (PARPs) that uses NAD(+) as substrate to form the negatively
charged polymer of poly (ADP-ribose) (PAR). After DNA damage, PARP-1 is responsible
for approximately 90% of the total cellular PARylation activity. Numerous studies
showed activation of PARP-1 in various conditions associated with oxidative and nitrosative
stress, such as ischemia-reperfusion injury, diabetes mellitus, and inflammation,
and also proved the beneficial effects of PARP inhibitors. Pharmacological inhibitors
of PARP move toward clinical testing for a variety of indications, including cardioprotection
and malignant tumors. Some of the compounds are already in clinical trials. These
advances necessitate the detection of PARP activation in human tissues. In the present
chapter, we review specific methods used to detect PARP activation in human circulating
leukocytes and human tissue sections.