Targeting mitochondria for cancer therapy

Nat Rev Drug Discov. 2010 Jun;9(6):447-64. doi: 10.1038/nrd3137. Epub 2010 May 14.


Mitochondria are the cells' powerhouse, but also their suicidal weapon store. Dozens of lethal signal transduction pathways converge on mitochondria to cause the permeabilization of the mitochondrial outer membrane, leading to the cytosolic release of pro-apoptotic proteins and to the impairment of the bioenergetic functions of mitochondria. The mitochondrial metabolism of cancer cells is deregulated owing to the use of glycolytic intermediates, which are normally destined for oxidative phosphorylation, in anabolic reactions. Activation of the cell death machinery in cancer cells by inhibiting tumour-specific alterations of the mitochondrial metabolism or by stimulating mitochondrial membrane permeabilization could therefore be promising therapeutic approaches.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Cell Membrane Permeability / drug effects
  • HSP90 Heat-Shock Proteins / antagonists & inhibitors
  • Humans
  • Indoles
  • Mitochondria / drug effects*
  • Mitochondria / metabolism
  • Mitochondrial Membrane Transport Proteins / drug effects
  • Mitochondrial Permeability Transition Pore
  • Pyrroles / pharmacology
  • Reactive Oxygen Species / metabolism
  • Resveratrol
  • Stilbenes / pharmacology


  • Antineoplastic Agents
  • HSP90 Heat-Shock Proteins
  • Indoles
  • Mitochondrial Membrane Transport Proteins
  • Mitochondrial Permeability Transition Pore
  • Pyrroles
  • Reactive Oxygen Species
  • Stilbenes
  • Resveratrol
  • obatoclax