Prostate apoptosis response-4 (Par-4) is a unique pro-apoptotic protein that selectively induces apoptosis in cancer cells. Moreover, Par-4 sensitizes cells to the action of diverse apoptotic stimuli and causes tumor regression. This review discusses the prominent structural and functional features of Par-4 and the multiple levels of regulation of its apoptotic function, all of which can be utilized to develop targeted cancer therapy.