The present invention discloses compositions and methods for selectively delivering apoptosis inducing agents (referred to as apoptogens) to the tumor prior to conventional therapeutic treatment protocol. We refer to this technology as a priori activation of apoptosis pathways of tumors (AAAPT). Specifically, the present invention relates to an ensemble (or bioconjugate) comprising of an apoptogen (A) and a tumor targeting group (or vector) (T), wherein the apoptogen is either connected directly to the targeting group or optionally attached through an intervening linker (L). Thus, a AAAPT bioconjugate bearing a linker is capable of being cleaved by enzymes and is expected to induce much higher death of tumor cells compared to normal cells. The AAAPT conjugates of the present invention induce large synergistic and selective cancer cell death response in combination with therapeutic agents.
