Targeting Apoptosis in Cancer

Purpose of Review Apoptosis is a major mechanism of cancer cell death. Thus, evasion of apoptosis results in therapy resistance. Here, we review apoptosis modulators in cancer and their recent developments, including MDM2 inhibitors and kinase inhibitors that can induce effective apoptosis. Recent Findings Both extrinsic pathways (external stimuli through cell surface death receptor) and intrinsic pathways (mitochondrial-mediated regulation upon genotoxic stress) regulate the complex process of apoptosis through orchestration of various proteins such as members of the BCL-2 family. Dysregulation within these complex steps can result in evasion of apoptosis. However, via the combined evolution of medicinal chemistry and molecular biology, omics assays have led to innovative inducers of apoptosis and inhibitors of anti-apoptotic regulators. Many of these agents are now being tested in cancer patients in early-phase trials. We believe that despite a sluggish speed of development, apoptosis targeting holds promise as a relevant strategy in cancer therapeutics.

Automated summary

This review discusses apoptosis modulators in cancer and their recent developments. Through the combined evolution of medicinal chemistry and molecular biology, innovative inducers of apoptosis and inhibitors of anti-apoptotic regulators have been discovered. Many of these agents are now being tested in early-phase trials in cancer patients. We believe that apoptosis targeting holds promise as a relevant strategy in cancer therapeutics.