PAC-1 works by chelating inhibitory zinc ions that normally bind to procaspase-3 and prevent its activation. Once these zinc ions are removed, the procaspase-3 undergoes a conformational change to become active caspase-3. The active caspase-3 then initiates a cascade of proteolytic activities that lead to apoptosis. This mechanism is particularly advantageous because it targets a fundamental process in cancer cell survival.