A BH3 Mimetic for Killing Cancer Cells

Cell. 2016 Jun 16;165(7):1560. doi: 10.1016/j.cell.2016.05.080.

Abstract

Venetoclax is a BH3 mimetic approved for treating chronic lymphocytic leukemia. Cancer cells are resistant to apoptosis but "primed for death" by elevated BCL-2, which binds to pro-apoptotic proteins and holds them in check. Venetoclax releases this antagonism and is the first approved drug to target a protein-protein interaction.

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects
  • Apoptosis Regulatory Proteins / antagonists & inhibitors
  • Apoptosis Regulatory Proteins / metabolism
  • Bridged Bicyclo Compounds, Heterocyclic / therapeutic use*
  • Drug Approval*
  • Humans
  • Leukemia, Lymphocytic, Chronic, B-Cell / drug therapy*
  • Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Sulfonamides / therapeutic use*

Substances

  • Antineoplastic Agents
  • Apoptosis Regulatory Proteins
  • BCL2 protein, human
  • Bridged Bicyclo Compounds, Heterocyclic
  • Proto-Oncogene Proteins c-bcl-2
  • Sulfonamides
  • venetoclax