Identifying the binding determinants for anti-cancer BH3 mimetic

Abstract

One of the many hallmarks of cancer is the evasion of cell death. While this is accomplished through several approaches, one strategy is to interrupt the intrinsic apoptotic pathway regulated by the Bcl-2 protein family by interfering with the initiation of apoptosis through the upregulated expression of pro-survival Bcl-2 proteins and inhibiting cell death effectors BAX and BAK. In normal cells, apoptosis can occur through pro-apoptotic BH3-only proteins directly binding and inhibiting pro-survival Bcl-2 proteins.